apomorphine

American Heritage Dictionary:

ap·o·mor·phine

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(ăp'ə-môr'fēn') pronunciation

n.
A poisonous white crystalline alkaloid, C₁₇H₁₇NO₂, derived from morphine and used medicinally to induce vomiting.

Apomorphine

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Brand names: Apokyn®, Uprima™

Chemical formula:

Drug Forms:

Apomorphine Hydrochloride Solution for injection (below)
Apomorphine injection

Espa�ol:

Apomorphine Hydrochloride Solution for injection

What is this medicine?

APOMORPHINE (a poe MOR feen) is used to treat 'off' episodes in advanced Parkinson's disease. These episodes affect your ability to move or perform tasks.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•asthma or other breathing problems
•heart disease
•history of alcohol or drug abuse
•kidney or liver disease
•low blood pressure
•mental illness
•sleep disorder
•stroke
•an unusual or allergic reaction to apomorphine, sulfites, other medicines foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

This medicine is for injection under the skin. You will be taught how to prepare and give this medicine. You will also need to take a medicine to prevent nausea and vomiting for at least the first two months of therapy. Use exactly as directed. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.

It is important that you put your used needles and syringes in a special sharps container. Do not put them in a trash can. If you do not have a sharps container, call your pharmacist or healthcare provider to get one.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

If you miss a dose, use it as soon as you can. If it is almost time for your next dose, use only that dose. Do not use double or extra doses.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•certain antibiotics like grepafloxacin and sparfloxacin
•cisapride
•medicines for irregular heart beat like amiodarone, disopyramide, dofetilide, flecainide, ibutilide, procainamide, quinidine, sotalol
•droperidol
•halofantrine
•levomethadyl
•pimozide
•some medicines for nausea like alosetron, dolasetron, dronabinol, droperidol, granisetron, ondansetron, palonosetron
•ziprasidone

This medicine may also interact with the following medications:
•alfuzosin
•certain antibiotics like clarithromycin, erythromycin, gatifloxacin, gemifloxacin, levofloxacin, moxifloxacin, troleandomycin
•medicines for high blood pressure or chest pain (angina)
•medicines to treat or prevent malaria like chloroquine or mefloquine
•metoclopramide
•phenothiazines like chlorpromazine, mesoridazine, prochlorperazine, thioridazine
•some medicines for depression like amitriptyline, amoxapine, maprotiline, mirtazapine, nefazodone, nortriptyline
•some medicines for mental disturbances like clozapine, haloperidol, molindone, olanzapine, pimozide, quetiapine, risperidone, ziprasidone

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. You may experience flushing, nausea, vomiting, pale skin, or sweating before dizziness or fainting occurs. Do not get up too quickly from a lying or sitting position. Report any dizziness or related symptoms to your health care provider as soon as possible. Alcohol may increase dizziness and drowsiness. Avoid alcoholic drinks. Do not take any medications that cause drowsiness without first checking with your health care provider.

If you find that you have sudden feelings of wanting to sleep during normal activities, like cooking, watching television, or while driving or riding in a car, you should contact your health care professional.

This medicine may cause severe nausea and vomiting. Your doctor may prescribe a medication to prevent these symptoms. Do not treat yourself. Not all medicines for nausea and vomiting can be used with this medicine. Talk to your doctor about which one may be right for you.

There have been reports of increased sexual urges or other strong urges such as gambling while taking some medicines for Parkinson's disease. If you experience any of these urges while taking this medicine, you should report it to your health care provider as soon as possible.

You should check your skin often for changes to moles and new growths while taking this medicine. Call your doctor if you notice any of these changes.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•abnormal or unusual body movements
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•blood pressure changes
•confusion, hallucinations (seeing or hearing things that are not really there)
•depression or depressed mood
•difficulty breathing or swallowing
•dizziness or lightheadedness
•excess sweating
•fainting spells
•falling asleep during normal activities like driving
•irregular or fast, pounding heartbeat, palpitations
•swelling in arms, hands, legs, or feet
•unusually weak or tired
•vomiting

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•drowsiness
•headache
•nausea
•yawning

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees). Throw away any unused medicine after the expiration date.

Last updated: 5/11/2004 11:36:00 AM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Oxford Dictionary of Biochemistry:

apomorphine

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6aβ-aporphine-10,11-diol; 5,6,6a,7-tetrahydro-6-methyl-4H-dibenzo[de,g]quinoline-10,11-diol; a synthetic opiate. The (R)-enantiomer is a potent dopamine receptor agonist, noted for its powerful emetic effects

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Saunders Veterinary Dictionary:

apomorphine

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An alkaloid from morphine. Used as the hydrochloride; administered parenterally it causes vomiting within 3 to 10 minutes but can also be administered orally. Stimulates receptors in the chemoreceptor trigger zone of the medulla oblongata.

Wikipedia on Answers.com:

Apomorphine

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Home > Library > Miscellaneous > Wikipedia

Apomorphine


Systematic (IUPAC) name
(6aR)-6-methyl-5,6,6a,7-tetrahydro-4H-dibenzo[de,g]quinoline-10,11-diol
Clinical data
Trade names	Apokyn
AHFS/Drugs.com	monograph
MedlinePlus	a604020
Pregnancy cat.	C
Legal status	℞ Prescription only
Routes	Oral, SC
Pharmacokinetic data
Bioavailability	100% following sc injection
Protein binding	~50%
Metabolism	Hepatic
Half-life	40 minutes (range 30-60 minutes)
Identifiers
CAS number	41372-20-7^Y
ATC code	G04BE07 N04BC07
PubChem	CID 6005
IUPHAR ligand	33
DrugBank	DB00714
ChemSpider	5783^Y
UNII	F39049Y068^Y
KEGG	D07460^Y
ChEBI	CHEBI:48538^Y
ChEMBL	CHEMBL53^N
Chemical data
Formula	C₁₇H₁₇N O₂
Mol. mass	267.322 g/mol
SMILES	eMolecules & PubChem
InChI InChI=1S/C17H17NO2/c1-18-8-7-10-3-2-4-12-15(10)13(18)9-11-5-6-14(19)17(20)16(11)12/h2-6,13,19-20H,7-9H2,1H3/t13-/m1/s1^Y Key:VMWNQDUVQKEIOC-CYBMUJFWSA-N^Y
N (what is this?) (verify)

Apomorphine (Apokyn, Ixense, Spontane, Uprima) is a non-selective dopamine agonist which activates both D₁-like and D₂-like receptors, with some preference for the latter subtypes.^[1] It is historically a morphine decomposition product by boiling with concentrated acid, hence the -morphine suffix. Apomorphine does not actually contain morphine or its skeleton, or bind to opioid receptors. The apo- prefix relates to it being an aporphine derivative.

Historically, apomorphine has been tried for a variety of uses including psychiatric treatment of homosexuality in the early 20th century, and more recently in treating erectile dysfunction. Currently, apomorphine is used in the treatment of Parkinson's disease. It is a potent emetic (i.e., it induces vomiting) and should not be administered without an antiemetic such as domperidone. The emetic properties of apomorphine are exploited in veterinary medicine to induce therapeutic emesis in canines that have recently ingested toxic or foreign substances.

It was also successfully used as an unofficial treatment of heroin addiction, a purpose for which it was championed by the author William S. Burroughs. A recent study indicates that apomorphine might be a suitable marker for assessing central dopamine system alterations associated with chronic heroin consumption.^[2] There is, however, no clinical evidence that apomorphine is an effective and safe treatment regimen for opiate addiction. Early studies involved aversion therapy in alcoholism and anxiety, and modern reports are rather anecdotal.^[3]

For treatment of erectile dysfunction, it is believed that dopamine receptors in the hypothalamic region of the brain are the main target, as although dopamine receptors in the penis do facilitate erection, they do so far more weakly than those in the brain.^[4]

Contents

1 Uses
2 Pharmacology
3 Chemistry
- 3.1 Properties
- 3.2 Synthesis
4 See also
5 References
6 External links

Uses

Alcoholism

Apomorphine was used with some notable success as a treatment for alcohol and morphine addiction. Its chief practitioner in the 1950s was Dr John Yerbury Dent 1888-1961 who, early on in his research, mistakenly believed that it was the emetic properties of apomorphine which was efficacious.

Parkinson's disease

First mooted as a treatment for Parkinson's disease as early as 1951,^[5] its clinical use was first reported in 1970 by Cotzias et al.,^[6] although its emetic properties and short half-life made oral use impractical. A later study found that combining the drug with the antiemetic domperidone improved results significantly.^[7]

Therapeutic use in Parkinson's disease is effective because of the drug's strong dopaminergic action. When administered subcutaneously, apomorphine is the most effective dopamine agonist. Within 3–20 minutes of injection apomorphine demonstrates a magnitude of effect (ability to convert the patient with Parkinson's disease to the "on" state) that is comparable to l-dopa. A single subcutaneous injection lasts for up to 90 minutes.^[8] While apomorphine can be used in combination with l-dopa, the intention is usually to reduce the l-dopa dosing, as by this stage the patient with Parkinson's disease will probably be experiencing a great deal of dopa-induced dyskinesias and "off" periods.^[8] Following a successful apomorphine challenge, training of patient and caregiver, and careful dose titration, the patient can be maintained in the "on" state by the use of an apomorphine pump as an effective monotherapy.^[8]

Erectile dysfunction

Apomorphine hydrochloride (trade name "Uprima", "Ixense") was a therapy used in the treatment of erectile dysfunction (male impotence). It is its mode of stimulating dopamine in the brain which is believed to enhance the sexual response. It was found to be of poor efficacy^[9] in a large-scale study by Researchers at the UK's Drug Safety Research Unit and University of Portsmouth and discontinued in the UK in January 2006.^[9] Around 65-70% of doctors felt it was ineffective, with 60% of over 11,000 patients (avg age 61) discontinuing in month 1 and a further 23% in month 2.^[9]^[10] UK studies concentrated on males with generalized erectile dysfunction. Uprima effects desire and is not meant to produce an overall effect as say Viagra which works on blood flow. In those males who have problems with desire as opposed to generalized erectile dysfunction it works as expected.

Alzheimer's disease

Apomorphine has been reported to be an inhibitor of Beta amyloid fibril formation, and may thus have potential as a therapeutic for Alzheimer's disease.^[11]

Opiate addiction

In his Deposition: Testimony Concerning a Sickness in the introduction to later editions of Naked Lunch, William S. Burroughs wrote that apomorphine treatment was the only effective cure to opiate addiction he has encountered. "The apomorphine cure is qualitatively different from other methods of cure. I have tried them all. Short reduction, slow reduction, cortisone, antihistamines, tranquilizers, sleeping cures, tolserol, reserpine. None of these cures lasted beyond the first opportunity to relapse. I can say that I was never metabolically cured until I took the apomorphine cure... The doctor explained to me that apomorphine acts on the back brain to regulate the metabolism and normalize the blood stream in such a way that the enzyme stream of addiction is destroyed over a period of four to five days. Once the back brain is regulated apomorphine can be discontinued and only used in case of relapse. (No one would take apomorphine for kicks. Not one case of addiction to apomorphine has ever been recorded.)" He goes on to lament the fact that as of his writing, little to no research has been done on apomorphine or variations of the drug to study its effects on curing addiction, and perhaps the possibility of retaining the positive effects while removing the side effect of vomiting.

Pharmacology

Apomorphine possesses affinity for the following receptors:^[1]

D₁ (K_i = 372 nM)
D_2S (K_i = 35 nM)
D_2L (K_i = 83 nM)
D₃ (K_i = 26 nM)
D₄ (K_i = 4.4 nM)
D₅ (K_i = 15 nM)

5-HT_1A (K_i = 117 nM)
5-HT_2A (K_i = 120 nM)
5-HT_2B (K_i = 132 nM)
5-HT_2C (K_i = 102 nM)

α_1B-adrenergic (K_i = 676 nM)
α_1D-adrenergic (K_i = 65 nM)
α_2A-adrenergic (K_i = 141 nM)
α_2B-adrenergic (K_i = 66 nM)
α_2C-adrenergic (K_i = 36 nM)

It has > 1,000 nM affinity for 5-HT_1B, 5-HT_1D, and α_1A-adrenergic, and > 10,000 nM affinity for β-adrenergic, H₁, and mACh.^[1]

Apomorphine behaves as a partial agonist at D_2S ( IA = 79%), D_2L (IA= 53%), D₃ (IA = 82%), and D₄ (IA = 45%), and as an antagonist at 5-HT_1B, 5-HT_1D, 5-HT_2A, 5-HT_2B, 5-HT_2C, α₁-adrenergic, and α₂-adrenergic.^[12]^[13] Though its efficacies at D₁ and D₅ are unclear, it is known to act as an agonist at these sites.^[14]

Chemistry

Properties

Apomorphine is colourless as a liquid but stains green. Therefore care must be taken to avoid splashes. Apormophine does not remain stable for more than 24 hours in a plastic container, so syringes are discarded if not used within 24 hours.

Synthesis

Apomorphine hydrochloride is synthesized by heating stoichiometric amounts of morphine and concentrated hydrochloric acid at 140ºC.

References

^ ^a ^b ^c Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes". The Journal of Pharmacology and Experimental Therapeutics 303 (2): 791–804. doi:10.1124/jpet.102.039867. PMID 12388666. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=12388666.
^ Guardia J, Casas M, Prat G, Trujols J, Segura L, Sánchez-Turet M (October 2002). "The apomorphine test: a biological marker for heroin dependence disorder?". Addict Biol 7 (4): 421–6. doi:10.1080/1355621021000006206. PMID 14578019. http://www.ncbi.nlm.nih.gov/pubmed/14578019.
^ Dent JY (1949). “Apomorphine Treatment of Addiction.” British Journal of Addiction to Alcohol & Other Drugs 46 (1); 15-28. DOI: 10.1111/j.1360-0443.1949.tb04502.x
^ Matsumoto K, Yoshida M, Andersson K, Hedlund P (2005). "Effects in vitro and in vivo by apomorphine in the rat corpus cavernosum". Br J Pharmacol 146 (2): 259–67. doi:10.1038/sj.bjp.0706317. . PMID 16025145. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1576267.
^ Schwab R, Amador L, Lettvin J (1951). "Apomorphine in Parkinson's disease". Trans Am Neurol Assoc 56: 251–3. PMID 14913646.
^ Cotzias G, Papavasiliou P, Fehling C, Kaufman B, Mena I (1970). "Similarities between neurologic effects of L-dopa and of apomorphine". N Engl J Med 282 (1): 31–3. doi:10.1056/NEJM197001012820107. PMID 4901383.
^ Corsini G, Del Zompo M, Gessa G, Mangoni A (1979). "Therapeutic efficacy of apomorphine combined with an extracerebral inhibitor of dopamine receptors in Parkinson's disease". Lancet 1 (8123): 954–6. doi:10.1016/S0140-6736(79)91725-2. PMID 87620.
^ ^a ^b ^c Chaudhuri K, Clough C (1998). "Subcutaneous apomorphine in Parkinson's disease: Effective yet underused". BMJ 316 (7132): 641. . PMID 9522772. http://bmj.bmjjournals.com/cgi/content/full/316/7132/641#B2.
^ ^a ^b ^c Pharmaceutical Business Review, "Study shows Abbott's Uprima ineffective for most UK patients"
^ MedicineNet study review
^ Lashuel HA, Hartley DM, Balakhaneh D, Aggarwal A, Teichberg S, Callaway DJE (2002). "New class of inhibitors of amyloid-beta fibril formation. Implications for the mechanism of pathogenesis in Alzheimer's disease". J Biol Chem 277 (45): 42881–42890. doi:10.1074/jbc.M206593200. PMID 12167652. http://www.jbc.org/cgi/content/abstract/277/45/42881.
^ Newman-Tancredi A, Cussac D, Audinot V, et al. (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". The Journal of Pharmacology and Experimental Therapeutics 303 (2): 805–14. doi:10.1124/jpet.102.039875. PMID 12388667. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=12388667.
^ Newman-Tancredi A, Cussac D, Quentric Y, et al. (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes". The Journal of Pharmacology and Experimental Therapeutics 303 (2): 815–22. doi:10.1124/jpet.102.039883. PMID 12388668. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=12388668.
^ Hsieh GC, Hollingsworth PR, Martino B, et al. (January 2004). "Central mechanisms regulating penile erection in conscious rats: the dopaminergic systems related to the proerectile effect of apomorphine". The Journal of Pharmacology and Experimental Therapeutics 308 (1): 330–8. doi:10.1124/jpet.103.057455. PMID 14569075. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=14569075.

External links

PDSP K_i database
"Apomorphine - Frequently Asked Questions". Britannia Pharmaceuticals. http://www.apo-go.co.uk.
Andrew Lees and Kirsten Turner (2002). "Apomorphine for Parkinson's Disease" (PDF). Practical Neurology 2 (5): 280–287. doi:10.1046/j.1474-7766.2002.00086.x. http://pn.bmjjournals.com/cgi/reprint/2/5/280.pdf. - Detailed usage guide for Apomorphine pumps for Parkinson's

Antiparkinson agents (N04)

Dopaminergics

DA precursors/prodrugs	Etilevodopa • Droxidopa • Levodopa^# • Melevodopa

DA receptor agonists	Aplindore • Apomorphine • Bromocriptine • Cabergoline • Ciladopa • Dihydroergocryptine • Lisuride • Pardoprunox • Pergolide • Piribedil • Pramipexole • Ropinirole • Rotigotine

MAO-B inhibitors	Ladostigil • Lazabemide • Mofegiline • Pargyline • Rasagiline • Selegiline

COMT inhibitors	Entacapone • Tolcapone

Aromatic L-amino acid decarboxylase inhibitors	Benserazide • Carbidopa^# • Methyldopa

Anticholinergics

Benzatropine • Biperiden^# • Bornaprine • Chlorphenoxamine • Cyrimine • Dexetimide • Dimenhydrinate • Diphenhydramine • Etanautine • Etybenzatropine • Mazaticol • Metixene • Orphenadrine • Phenglutarimide • Piroheptine • Procyclidine • Profenamine • Trihexyphenidyl • Tropatepine

Others

Amantadine • Budipine • MDMA • Memantine • Rimantadine • UWA-101

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

M: CNS

anat(n/s/m/p/4/e/b/d/c/a/f/l/g)/phys/devp

noco(m/d/e/h/v/s)/cong/tumr, sysi/epon, injr

proc, drug(N1A/2AB/C/3/4/7A/B/C/D)

Drugs for erectile dysfunction (G04BE) and premature ejaculation

For erectile dysfunction

Prostaglandins (E)	Alprostadil

PDE5 inhibitors	Avanafil • Sildenafil • Tadalafil • Udenafil • Vardenafil

Alpha blockers	Moxisylyte • Phentolamine • Yohimbine

Dopamine D₄ receptor agonists	ABT-670 • ABT-724

Others	Apomorphine • Papaverine

For premature ejaculation

SSRIs	Dapoxetine

Oxytocin receptor antagonists	Epelsiban

M: ♂ MRS

anat/phys/devp

noco/cong/tumr, sysi/epon

proc, drug (G3B/4BE/4C)

Adrenergics

Receptor ligands

α₁	Agonists: 5-FNE 6-FNE Amidephrine Anisodamine Anisodine Cirazoline Dipivefrine Dopamine Ephedrine Epinephrine (Adrenaline) Etilefrine Ethylnorepinephrine Indanidine Levonordefrin Metaraminol Methoxamine Methyldopa Midodrine Naphazoline Norepinephrine (Noradrenaline) Octopamine Oxymetazoline Phenylephrine Phenylpropanolamine Pseudoephedrine Synephrine Tetrahydrozoline Antagonists: Abanoquil Adimolol Ajmalicine Alfuzosin Amosulalol Arotinolol Atiprosin Benoxathian Buflomedil Bunazosin Carvedilol CI-926 Corynanthine Dapiprazole DL-017 Domesticine Doxazosin Eugenodilol Fenspiride GYKI-12,743 GYKI-16,084 Indoramin Ketanserin L-765,314 Labetalol Mephendioxan Metazosin Monatepil Moxisylyte (Thymoxamine) Naftopidil Nantenine Neldazosin Nicergoline Niguldipine Pelanserin Phendioxan Phenoxybenzamine Phentolamine Piperoxan Prazosin Quinazosin Ritanserin RS-97,078 SGB-1,534 Silodosin SL-89.0591 Spiperone Talipexole Tamsulosin Terazosin Tibalosin Tiodazosin Tipentosin Tolazoline Trimazosin Upidosin Urapidil Zolertine * Note that many TCAs, TeCAs, antipsychotics, ergolines, and some piperazines like buspirone, trazodone, nefazodone, etoperidone, and mepiprazole all antagonize α₁-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.

α₂	Agonists: (R)-3-Nitrobiphenyline 4-NEMD 6-FNE Amitraz Apraclonidine Brimonidine Cannabivarin Clonidine Detomidine Dexmedetomidine Dihydroergotamine Dipivefrine Dopamine Ephedrine Ergotamine Epinephrine (Adrenaline) Esproquin Etilefrine Ethylnorepinephrine Guanabenz Guanfacine Guanoxabenz Levonordefrin Lofexidine Medetomidine Methyldopa Mivazerol Naphazoline Norepinephrine (Noradrenaline) Phenylpropanolamine Piperoxan Pseudoephedrine Rilmenidine Romifidine Talipexole Tetrahydrozoline Tizanidine Tolonidine Urapidil Xylazine Xylometazoline Antagonists: 1-PP Adimolol Aptazapine Atipamezole BRL-44408 Buflomedil Cirazoline Efaroxan Esmirtazapine Fenmetozole Fluparoxan GYKI-12,743 GYKI-16,084 Idazoxan Mianserin Mirtazapine MK-912 NAN-190 Olanzapine Phentolamine Phenoxybenzamine Piperoxan Piribedil Rauwolscine Rotigotine SB-269,970 Setiptiline Spiroxatrine Sunepitron Tolazoline Yohimbine * Note that many atypical antipsychotics and azapirones like buspirone and gepirone (via metabolite 1-PP) antagonize α₂-adrenergic receptors as well.

β	Agonists: 2-FNE 5-FNE Amibegron Arbutamine Arformoterol Arotinolol BAAM Bambuterol Befunolol Bitolterol Broxaterol Buphenine Carbuterol Cimaterol Clenbuterol Denopamine Deterenol Dipivefrine Dobutamine Dopamine Dopexamine Ephedrine Epinephrine (Adrenaline) Etafedrine Etilefrine Ethylnorepinephrine Fenoterol Formoterol Hexoprenaline Higenamine Indacaterol Isoetarine Isoprenaline (Isoproterenol) Isoxsuprine Labetalol Levonordefrin Levosalbutamol Mabuterol Methoxyphenamine Methyldopa N-Isopropyloctopamine Norepinephrine (Noradrenaline) Orciprenaline Oxyfedrine Phenylpropanolamine Pirbuterol Prenalterol Ractopamine Procaterol Pseudoephedrine Reproterol Rimiterol Ritodrine Salbutamol (Albuterol) Salmeterol Solabegron Terbutaline Tretoquinol Tulobuterol Xamoterol Zilpaterol Zinterol Antagonists: Acebutolol Adaprolol Adimolol Afurolol Alprenolol Alprenoxime Amosulalol Ancarolol Arnolol Arotinolol Atenolol Befunolol Betaxolol Bevantolol Bisoprolol Bopindolol Bormetolol Bornaprolol Brefonalol Bucindolol Bucumolol Bufetolol Buftiralol Bufuralol Bunitrolol Bunolol Bupranolol Burocrolol Butaxamine Butidrine Butofilolol Capsinolol Carazolol Carpindolol Carteolol Carvedilol Celiprolol Cetamolol Cicloprolol Cinamolol Cloranolol Cyanopindolol Dalbraminol Dexpropranolol Diacetolol Dichloroisoprenaline Dihydroalprenolol Dilevalol Diprafenone Draquinolol Dropranolol Ecastolol Epanolol Ericolol Ersentilide Esatenolol Esmolol Esprolol Eugenodilol Exaprolol Falintolol Flestolol Flusoxolol Hydroxycarteolol Hydroxytertatolol ICI-118,551 Idropranolol Indenolol Indopanolol Iodocyanopindolol Iprocrolol Isoxaprolol Isamoltane Labetalol Landiolol Levobetaxolol Levobunolol Levocicloprolol Levomoprolol Medroxalol Mepindolol Metalol Metipranolol Metoprolol Moprolol Nadolol Nadoxolol Nafetolol Nebivolol Neraminol Nifenalol Nipradilol Oberadilol Oxprenolol Pacrinolol Pafenolol Pamatolol Pargolol Parodilol Penbutolol Penirolol PhQA-33 Pindolol Pirepolol Practolol Primidolol Procinolol Pronethalol Propafenone Propranolol Ridazolol Ronactolol Soquinolol Sotalol Spirendolol SR 59230A Sulfinalol TA-2005 Talinolol Tazolol Teoprolol Tertatolol Terthianolol Tienoxolol Tilisolol Timolol Tiprenolol Tolamolol Toliprolol Tribendilol Trigevolol Xibenolol Xipranolol

Reuptake inhibitors

NET	Selective norepinephrine reuptake inhibitors: Amedalin Atomoxetine (Tomoxetine) Ciclazindol Daledalin Esreboxetine Lortalamine Mazindol Nisoxetine Reboxetine Talopram Talsupram Tandamine Viloxazine; Norepinephrine-dopamine reuptake inhibitors: Amineptine Bupropion (Amfebutamone) Fencamine Fencamfamine Lefetamine Levophacetoperane LR-5182 Manifaxine Methylphenidate Nomifensine O-2172 Radafaxine; Serotonin-norepinephrine reuptake inhibitors: Bicifadine Desvenlafaxine Duloxetine Eclanamine Levomilnacipran Milnacipran Sibutramine Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors: Brasofensine Diclofensine DOV-102,677 DOV-21,947 DOV-216,303 JNJ-7925476 JZ-IV-10 Methylnaphthidate Naphyrone NS-2359 PRC200-SS SEP-225,289 SEP-227,162 Tesofensine; Tricyclic antidepressants: Amitriptyline Butriptyline Cianopramine Clomipramine Desipramine Dosulepin Doxepin Imipramine Lofepramine melitracen Nortriptyline Protriptyline Trimipramine; Tetracyclic antidepressants: Amoxapine Maprotiline Mianserin Oxaprotiline Setiptiline; Others: Cocaine CP-39,332 EXP-561 Fezolamine Ginkgo biloba Indeloxazine Nefazodone Nefopam Pridefrine Tapentadol Tedatioxetine Teniloxazine Tramadol Ziprasidone

VMAT	Ibogaine Reserpine Tetrabenazine

Releasing agents

Morpholines: Fenbutrazate
Morazone
Phendimetrazine
Phenmetrazine; Oxazolines: 4-Methylaminorex
Aminorex
Clominorex
Cyclazodone
Fenozolone
Fluminorex
Pemoline
Thozalinone; Phenethylamines (also amphetamines, cathinones, phentermines, etc): 2-OH-PEA
4-CAB
4-FA
4-FMA
4-MA
4-MMA
Alfetamine
Amfecloral
Amfepentorex
Amfepramone
Amphetamine (Dextroamphetamine
Levoamphetamine)
Amphetaminil
β-Me-PEA
BDB
Benzphetamine
BOH
Buphedrone
Butylone
Cathine
Cathinone
Clobenzorex
Clortermine
D-Deprenyl
Dimethylamphetamine
Dimethylcathinone (Dimethylpropion, metamfepramone)
DMA
DMMA
EBDB
Ephedrine
Ethcathinone
Ethylamphetamine
Ethylone
Famprofazone
Fenethylline
Fenproporex
Flephedrone
Fludorex
Furfenorex
Hordenine
IAP
IMP
Iofetamine
L-Deprenyl (Selegiline)
Lisdexamfetamine
Lophophine
MBDB
MDA (Tenamfetamine)
MDEA
MDMA
MDMPEA
MDOH
MDPEA
Mefenorex
Mephedrone
Mephentermine
Methamphetamine (Dextromethamphetamine
Levomethamphetamine)
Methcathinone
Methedrone
Methylone
NAP
Ortetamine
Paredrine
pBA
pCA
Pentorex (Phenpentermine)
Phenethylamine
Pholedrine
Phenpromethamine
Phentermine
Phenylpropanolamine
pIA
Prenylamine
Propylamphetamine
Pseudoephedrine
Tiflorex
Tyramine
Xylopropamine
Zylofuramine; Piperazines: 2C-B-BZP
BZP
MBZP
mCPP
MDBZP
MeOPP
pFPP; Others: 2-Amino-1,2-dihydronaphthalene
2-Aminoindane
2-Aminotetralin
2-Benzylpiperidine
4-Benzylpiperidine
5-IAI
Clofenciclan
Cyclopentamine
Cypenamine
Cyprodenate
Feprosidnine
Gilutensin
Heptaminol
Hexacyclonate
Indanorex
Isometheptene
Methylhexanamine
Octodrine
Phthalimidopropiophenone
Propylhexedrine (Levopropylhexedrine)
Tuaminoheptane

Enzyme inhibitors

Anabolism

PAH	3,4-Dihydroxystyrene

TH	3-Iodotyrosine Aquayamycin Bulbocapnine Metirosine Oudenone

AAAD	Benserazide Carbidopa DFMD Genistein Methyldopa

DBH	Bupicomide Disulfiram Dopastin Fusaric acid Nepicastat Phenopicolinic acid Tropolone

PNMT	CGS-19281A SKF-64139 SKF-7698

Catabolism

MAO	Nonselective: Benmoxin Caroxazone Echinopsidine Furazolidone Hydralazine Indantadol Iproclozide Iproniazid Isocarboxazid Isoniazid Linezolid Mebanazine Metfendrazine Nialamide Octamoxin Paraxazone Phenelzine Pheniprazine Phenoxypropazine Pivalylbenzhydrazine Procarbazine Safrazine Tranylcypromine; MAO-A selective: Amiflamine Bazinaprine Befloxatone Befol Brofaromine Cimoxatone Clorgiline Esuprone Harmala alkaloids (Harmine Harmaline Tetrahydroharmine Harman Norharman, etc) Methylene Blue Metralindole Minaprine Moclobemide Pirlindole Sercloremine Tetrindole Toloxatone Tyrima; MAO-B selective: D-Deprenyl Selegiline (L-Deprenyl) Ladostigil Lazabemide Milacemide Mofegiline Pargyline Rasagiline Safinamide * Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine.

COMT	Entacapone Tolcapone

Others

Precursors	L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine L-DOPS (Droxidopa)

Cofactors	Ferrous Iron (Fe²⁺) S-Adenosyl-L-Methionine Vitamin B₃ (Niacin Nicotinamide → NADPH) Vitamin B₆ (Pyridoxine Pyridoxamine Pyridoxal → Pyridoxal Phosphate) Vitamin B₉ (Folic acid → Tetrahydrofolic acid) Vitamin C (Ascorbic acid) Zinc (Zn²⁺)

Others	Activity enhancers: BPAP PPAP; Release blockers: Bethanidine Bretylium Guanadrel Guanazodine Guanclofine Guanethidine Guanoxan; Toxins: Oxidopamine (6-Hydroxydopamine)

List of adrenergic drugs

Dopaminergics

Receptor ligands

Agonists	Adamantanes: Amantadine Memantine Rimantadine; Aminotetralins: 7-OH-DPAT 8-OH-PBZI Rotigotine UH-232; Benzazepines: 6-Br-APB Fenoldopam SKF-38,393 SKF-77,434 SKF-81,297 SKF-82,958 SKF-83,959; Ergolines: Bromocriptine Cabergoline Dihydroergocryptine Epicriptine Lisuride LSD Pergolide; Dihydrexidine derivatives: 2-OH-NPA A-86,929 Ciladopa Dihydrexidine Dinapsoline Dinoxyline Doxanthrine; Others: A-68,930 A-77636 A-412,997 ABT-670 ABT-724 Aplindore Apomorphine Aripiprazole Bifeprunox BP-897 CY-208,243 Dizocilpine Etilevodopa Flibanserin Ketamine Melevodopa Modafinil Pardoprunox Phencyclidine PD-128,907 PD-168,077 PF-219,061 Piribedil Pramipexole Propylnorapomorphine Pukateine Quinagolide Quinelorane Quinpirole RDS-127 Ro10-5824 Ropinirole Rotigotine Roxindole Salvinorin A SKF-89,145 Sumanirole Terguride Umespirone WAY-100,635

Antagonists	Typical antipsychotics: Acepromazine Azaperone Benperidol Bromperidol Clopenthixol Chlorpromazine Chlorprothixene Droperidol Flupentixol Fluphenazine Fluspirilene Haloperidol Loxapine Mesoridazine Methotrimeprazine Nemonapride Penfluridol Perazine Periciazine Perphenazine Pimozide Prochlorperazine Promazine Sulforidazine Sulpiride Sultopride Thioridazine Thiothixene Trifluoperazine Triflupromazine Trifluperidol Zuclopenthixol; Atypical antipsychotics: Amisulpride Asenapine Blonanserin Cariprazine Carpipramine Clocapramine Clorotepine Clozapine Gevotroline Iloperidone Lurasidone Melperone Molindone Mosapramine Olanzapine Paliperidone Perospirone Piquindone Quetiapine Remoxipride Risperidone Sertindole Tiospirone Ziprasidone Zotepine; Antiemetics: AS-8112 Alizapride Bromopride Clebopride Domperidone Metoclopramide Thiethylperazine; Others: Amoxapine Buspirone Butaclamol Ecopipam EEDQ Eticlopride Fananserin L-745,870 Nafadotride Nuciferine PNU-99,194 Raclopride Sarizotan SB-277,011-A SCH-23,390 SKF-83,959 Sonepiprazole Spiperone Spiroxatrine Stepholidine Tetrahydropalmatine Tiapride UH-232 Yohimbine

Reuptake inhibitors

Plasmalemmal

DAT inhibitors

Piperazines: DBL-583
GBR-12,935
Nefazodone
Vanoxerine; Piperidines: BTCP
Desoxypipradrol
Dextromethylphenidate
Difemetorex
Ethylphenidate
Methylnaphthidate
Methylphenidate
Phencyclidine
Pipradrol; Pyrrolidines: Diphenylprolinol
Methylenedioxypyrovalerone (MDPV)
Naphyrone
Prolintane
Pyrovalerone; Tropanes: β-CPPIT
Altropane
Brasofensine
CFT
Cocaine
Dichloropane
Difluoropine
FE-β-CPPIT
FP-β-CPPIT
Ioflupane (¹²³I)
Iometopane
RTI-112
RTI-113
RTI-121
RTI-126
RTI-150
RTI-177
RTI-229
RTI-336
Tenocyclidine
Tesofensine
Troparil
Tropoxane
WF-11
WF-23
WF-31
WF-33; Others: Adrafinil
Armodafinil
Amfonelic acid
Amineptine
Benzatropine (Benztropine)
Bromantane
BTQ
BTS-74,398
Bupropion (Amfebutamone)
Ciclazindol
Diclofensine
Dimethocaine
Diphenylpyraline
Dizocilpine
DOV-102,677
DOV-21,947
DOV-216,303
Etybenzatropine (Ethylbenztropine)
EXP-561
Fencamine
Fencamfamine
Fezolamine
GYKI-52,895
Indatraline
Ketamine
Lefetamine
Levophacetoperane
LR-5182
Manifaxine
Mazindol
Medifoxamine
Mesocarb
Modafinil
Nefopam
Nomifensine
NS-2359
O-2172
Pridefrine
Propylamphetamine
Radafaxine
SEP-225,289
SEP-227,162
Sertraline
Sibutramine
Tametraline
Tedatioxetine
Tripelennamine

Vesicular

VMAT inhibitors	Deserpidine Ibogaine Reserpine Tetrabenazine

Releasing agents

Morpholines: Fenbutrazate
Morazone
Phendimetrazine
Phenmetrazine; Oxazolines: 4-Methylaminorex (4-MAR, 4-MAX)
Aminorex
Clominorex
Cyclazodone
Fenozolone
Fluminorex
Pemoline
Thozalinone; Phenethylamines (also amphetamines, cathinones, phentermines, etc): 2-Hydroxyphenethylamine (2-OH-PEA)
4-CAB
4-Methylamphetamine (4-MA)
4-Methylmethamphetamine (4-MMA)
Alfetamine
Amfecloral
Amfepentorex
Amfepramone
Amphetamine (Dextroamphetamine
Levoamphetamine)
Amphetaminil
β-Methylphenethylamine (β-Me-PEA)
Benzodioxolylbutanamine (BDB)
Benzodioxolylhydroxybutanamine (BOH)
Benzphetamine
Buphedrone
Butylone
Cathine
Cathinone
Clobenzorex
Clortermine
D-Deprenyl
Dimethoxyamphetamine (DMA)
Dimethoxymethamphetamine (DMMA)
Dimethylamphetamine
Dimethylcathinone (Dimethylpropion, metamfepramone)
Ethcathinone (Ethylpropion)
Ethylamphetamine
Ethylbenzodioxolylbutanamine (EBDB)
Ethylone
Famprofazone
Fenethylline
Fenproporex
Flephedrone
Fludorex
Furfenorex
Hordenine
Iofetamine
Lophophine (Homomyristicylamine)
Mefenorex
Mephedrone
Methamphetamine (Desoxyephedrine, Methedrine; Dextromethamphetamine
Levomethamphetamine)
Methcathinone (Methylpropion)
Methedrone
Methoxymethylenedioxyamphetamine (MMDA)
Methoxymethylenedioxymethamphetamine (MMDMA)
Methylbenzodioxolylbutanamine (MBDB)
Methylenedioxyamphetamine (MDA, tenamfetamine)
Methylenedioxyethylamphetamine (MDEA)
Methylenedioxyhydroxyamphetamine (MDOH)
Methylenedioxymethamphetamine (MDMA)
Methylenedioxymethylphenethylamine (MDMPEA, homarylamine)
Methylenedioxyphenethylamine (MDPEA, homopiperonylamine)
Methylone
Ortetamine
Parabromoamphetamine (PBA)
Parachloroamphetamine (PCA)
Parafluoroamphetamine (PFA)
Parafluoromethamphetamine (PFMA)
Parahydroxyamphetamine (PHA)
Paraiodoamphetamine (PIA)
Paredrine (Norpholedrine, Oxamphetamine)
Phenethylamine (PEA)
Pholedrine
Phenpromethamine
Prenylamine
Propylamphetamine
Tiflorex (Flutiorex)
Tyramine (TRA)
Xylopropamine
Zylofuramine; Piperazines: 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP)
Benzylpiperazine (BZP)
Methoxyphenylpiperazine (MeOPP, paraperazine)
Methylbenzylpiperazine (MBZP)
Methylenedioxybenzylpiperazine (MDBZP, piperonylpiperazine); Others: 2-Amino-1,2-dihydronaphthalene (2-ADN)
2-Aminoindane (2-AI)
2-Aminotetralin (2-AT)
4-Benzylpiperidine (4-BP)
5-IAI
Clofenciclan
Cyclopentamine
Cypenamine
Cyprodenate
Feprosidnine
Gilutensin
Heptaminol
Hexacyclonate
Indanylaminopropane (IAP)
Indanorex
Isometheptene
Methylhexanamine
Naphthylaminopropane (NAP)
Octodrine
Phthalimidopropiophenone
Propylhexedrine (Levopropylhexedrine)
Tuaminoheptane (Tuamine)

Allosteric modulators

Quinazolinamines: SoRI-9804 SoRI-20040 SoRI-20041

Enzyme inhibitors

Anabolism

PAH inhibitors	3,4-Dihydroxystyrene

TH inhibitors	3-Iodotyrosine Aquayamycin Bulbocapnine Metirosine Oudenone

AAAD/DDC inhibitors	Benserazide Carbidopa DFMD Genistein Methyldopa

Catabolism

MAO inhibitors	Nonselective: Benmoxin Caroxazone Echinopsidine Furazolidone Hydralazine Indantadol Iproclozide Iproniazid Isocarboxazid Isoniazid Linezolid Mebanazine Metfendrazine Nialamide Octamoxin Paraxazone Phenelzine Pheniprazine Phenoxypropazine Pivalylbenzhydrazine Procarbazine Safrazine Tranylcypromine; MAO-A selective: Amiflamine Bazinaprine Befloxatone Befol Brofaromine Cimoxatone Clorgiline Esuprone Harmala alkaloids Methylene Blue Metralindole Minaprine Moclobemide Pirlindole Sercloremine Tetrindole Toloxatone Tyrima; MAO-B selective: D-Deprenyl L-Deprenyl (Selegiline) Ladostigil Lazabemide Milacemide Pargyline Rasagiline Safinamide

COMT inhibitors	Entacapone Tolcapone

DBH inhibitors	Disulfiram Dopastin Fusaric acid Nepicastat Tropolone

Others

Precursors	L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa)

Cofactors	Ferrous iron (Fe²⁺) Tetrahydrobiopterin Vitamin B₃ (Niacin Nicotinamide → NADPH) Vitamin B₆ (Pyridoxine Pyridoxamine Pyridoxal → Pyridoxal phosphate) Vitamin B₉ (Folic acid → Tetrahydrofolic acid) Vitamin C (Ascorbic acid) Zinc (Zn²⁺)

Others	Activity enhancers: Benzofuranylpropylaminopentane (BPAP) Phenylpropylaminopentane (PPAP); Toxins: Oxidopamine (6-Hydroxydopamine)

List of dopaminergic drugs

Serotonergics

5-HT₁ receptor ligands

5-HT_1A	Agonists: Azapirones: Alnespirone Binospirone Buspirone Enilospirone Eptapirone Gepirone Ipsapirone Perospirone Revospirone Tandospirone Tiospirone Umespirone Zalospirone; Antidepressants: Etoperidone Nefazodone Trazodone Vortioxetine; Antipsychotics: Aripiprazole Asenapine Clozapine Quetiapine Ziprasidone; Ergolines: Dihydroergotamine Ergotamine Lisuride Methysergide LSD; Tryptamines: 5-CT 5-MeO-DMT 5-MT Bufotenin DMT Indorenate Psilocin Psilocybin; Others: 8-OH-DPAT Adatanserin Bay R 1531 Befiradol BMY-14802 Cannabidiol Dimemebfe Ebalzotan Eltoprazine F-11,461 F-12,826 F-13,714 F-14,679 F-15,063 F-15,599 Flesinoxan Flibanserin Lesopitron LY-293,284 LY-301,317 MKC-242 NBUMP Osemozotan Oxaflozane Pardoprunox Piclozotan Rauwolscine Repinotan Roxindole RU-24,969 S 14,506 S-14,671 S-15,535 Sarizotan SSR-181,507 Sunepitron U-92,016-A Urapidil Vilazodone Xaliproden Yohimbine Antagonists: Antipsychotics: Iloperidone Risperidone Sertindole; Beta blockers: Alprenolol Cyanopindolol Iodocyanopindolol Oxprenolol Pindobind Pindolol Propranolol Tertatolol; Others: AV965 BMY-7,378 CSP-2503 Dotarizine Flopropione GR-46611 Isamoltane Lecozotan Mefway Metitepine/Methiothepin MPPF NAN-190 PRX-00023 Robalzotan S-15535 SB-649,915 SDZ 216-525 Spiperone Spiramide Spiroxatrine UH-301 WAY-100,135 WAY-100,635 Xylamidine

5-HT_1B	Agonists: Lysergamides: Dihydroergotamine Ergotamine Methysergide; Piperazines: Eltoprazine TFMPP; Triptans: Avitriptan Eletriptan Sumatriptan Zolmitriptan; Tryptamines: 5-CT 5-MT; Others: CGS-12066A CP-93,129 CP-94,253 CP-135,807 RU-24,969 Vortioxetine Antagonists: Lysergamides: Metergoline; Others: AR-A000002 Elzasonan GR-127,935 Isamoltane Metitepine/Methiothepin SB-216,641 SB-224,289 SB-236,057 Yohimbine

5-HT_1D	Agonists: Lysergamides: Dihydroergotamine Methysergide; Triptans: Almotriptan Avitriptan Eletriptan Frovatriptan Naratriptan Rizatriptan Sumatriptan Zolmitriptan; Tryptamines: 5-CT 5-Ethyl-DMT 5-MT 5-(Nonyloxy)tryptamine; Others: CP-135,807 CP-286,601 GR-46611 L-694,247 L-772,405 PNU-109,291 PNU-142,633 Antagonists: Lysergamides: Metergoline; Others: Alniditan BRL-15,572 Elzasonan GR-127,935 Ketanserin LY-310,762 LY-367,642 LY-456,219 LY-456,220 Metitepine/Methiothepin Ritanserin Yohimbine Ziprasidone

5-HT_1E	Agonists: Lysergamides: Methysergide; Triptans: Eletriptan; Tryptamines: BRL-54443 Tryptamine Antagonists: Metitepine/Methiothepin

5-HT_1F	Agonists: Triptans: Eletriptan Naratriptan Sumatriptan; Tryptamines: 5-MT; Others: BRL-54443 Lasmiditan LY-334,370 Antagonists: Metitepine/Methiothepin

5-HT₂ receptor ligands


5-HT_2A	Agonists: Lysergamides: ALD-52 Ergometrine Lisuride LA-SS-Az LSD LSD-Pip Lysergic acid 2-butyl amide Lysergic acid 3-pentyl amide Methysergide; Phenethylamines: 25I-NBF 25I-NBMD 25I-NBOH 25I-NBOMe 2C-B 2C-B-FLY 2CB-Ind 2C-C-NBOMe 2C-E 2C-I 2C-TFM-NBOMe 2C-T-2 2C-T-7 2C-T-21 2CBCB-NBOMe 2CBFly-NBOMe Bromo-DragonFLY DOB DOC DOI DOM MDA MDMA Mescaline TCB-2 TFMFly; Piperazines: BZP Quipazine TFMPP; Tryptamines: 5-CT 5-MeO-α-ET 5-MeO-α-MT 5-MeO-DET 5-MeO-DiPT 5-MeO-DMT 5-MeO-DPT 5-MT α-ET α-Methyl-5-HT α-MT Bufotenin DET DiPT DMT DPT Psilocin Psilocybin; Others: AL-34662 AL-37350A Dimemebfe Medifoxamine O-4310 Oxaflozane PNU-22394 RH-34 Antagonists: Atypical antipsychotics: Amperozide Aripiprazole Carpipramine Clocapramine Clorotepine Clozapine Gevotroline Iloperidone Melperone Mosapramine Olanzapine Paliperidone Pimozide Quetiapine Risperidone Sertindole Ziprasidone Zotepine; Typical antipsychotics: Loxapine Pipamperone; Antidepressants: Amitriptyline Amoxapine Aptazapine Etoperidone Mianserin Mirtazapine Nefazodone Teniloxazine Trazodone; Others: 5-I-R91150 5-MeO-NBpBrT AC-90179 Adatanserin Altanserin AMDA APD-215 Blonanserin Cinanserin CSP-2503 Cyproheptadine Deramciclane Dotarizine Eplivanserin Esmirtazapine Fananserin Flibanserin Ketanserin KML-010 Lubazodone Mepiprazole Metitepine/Methiothepin Nantenine Pimavanserin Pizotifen Pruvanserin Rauwolscine Ritanserin S-14,671 Sarpogrelate Setoperone Spiperone Spiramide SR-46349B Volinanserin Xylamidine Yohimbine

5-HT_2B	Agonists: Oxazolines: 4-Methylaminorex Aminorex; Phenethylamines: Chlorphentermine Cloforex DOB DOC DOI DOM Fenfluramine MDA MDMA Norfenfluramine; Tryptamines: 5-CT 5-MT α-Methyl-5-HT; Others: BW-723C86 Cabergoline mCPP Pergolide PNU-22394 Ro60-0175 Antagonists: Agomelatine Asenapine EGIS-7625 Ketanserin Lisuride LY-272,015 Metitepine/Methiothepin PRX-08066 Rauwolscine Ritanserin RS-127,445 Sarpogrelate SB-200,646 SB-204,741 SB-206,553 SB-215,505 SB-221,284 SB-228,357 SDZ SER-082 Tegaserod Yohimbine

5-HT_2C	Agonists: Phenethylamines: 2C-B 2C-E 2C-I 2C-T-2 2C-T-7 2C-T-21 DOB DOC DOI DOM MDA MDMA Mescaline; Piperazines: Aripiprazole mCPP TFMPP; Tryptamines: 5-CT 5-MeO-α-ET 5-MeO-α-MT 5-MeO-DET 5-MeO-DiPT 5-MeO-DMT 5-MeO-DPT 5-MT α-ET α-Methyl-5-HT α-MT Bufotenin DET DiPT DMT DPT Psilocin Psilocybin; Others: A-372,159 AL-38022A CP-809,101 Dimemebfe Lorcaserin Medifoxamine MK-212 Org 12,962 ORG-37,684 Oxaflozane PNU-22394 Ro60-0175 Ro60-0213 Vabicaserin WAY-629 WAY-161,503 YM-348 Antagonists: Atypical antipsychotics: Clorotepine Clozapine Iloperidone Melperone Olanzapine Paliperidone Pimozide Quetiapine Risperidone Sertindole Ziprasidone Zotepine; Typical antipsychotics: Chlorpromazine Loxapine Pipamperone; Antidepressants: Agomelatine Amitriptyline Amoxapine Aptazapine Etoperidone Fluoxetine Mianserin Mirtazapine Nefazodone Nortriptyline Tedatioxetine Trazodone; Others: Adatanserin Cinanserin Cyproheptadine Deramciclane Dotarizine Eltoprazine Esmirtazapine FR-260,010 Ketanserin Ketotifen Latrepirdine Metitepine/Methiothepin Methysergide Pizotifen Ritanserin RS-102,221 S-14,671 SB-200,646 SB-206,553 SB-221,284 SB-228,357 SB-242,084 SB-243,213 SDZ SER-082 Xylamidine


5-HT₃	Agonists: Piperazines: BZP Quipazine; Tryptamines: 2-Methyl-5-HT 5-CT; Others: Chlorophenylbiguanide Butanol Ethanol Halothane Isoflurane RS-56812 SR-57,227 SR-57,227-A Toluene Trichloroethane Trichloroethanol Trichloroethylene YM-31636 Antagonists: Antiemetics: AS-8112 Alosetron Azasetron Batanopride Bemesetron Cilansetron Dazopride Dolasetron Granisetron Lerisetron Ondansetron Palonosetron Ramosetron Renzapride Tropisetron Zacopride Zatosetron; Atypical antipsychotics: Clozapine Olanzapine Quetiapine; Tetracyclic antidepressants: Amoxapine Mianserin Mirtazapine; Others: CSP-2503 ICS-205,930 MDL-72,222 Memantine Nitrous Oxide Ricasetron Sevoflurane Tedatioxetine Thujone Vortioxetine Xenon

5-HT₄	Agonists: Gastroprokinetic Agents: Cinitapride Cisapride Dazopride Metoclopramide Mosapride Prucalopride Renzapride Tegaserod Velusetrag Zacopride; Others: 5-MT BIMU8 CJ-033,466 PRX-03140 RS-67333 RS-67506 SL65.0155 Antagonists: GR-113,808 GR-125,487 L-Lysine Piboserod RS-39604 RS-67532 SB-203,186 SB-204,070

5-HT_5A	Agonists: Lysergamides: Ergotamine LSD; Tryptamines: 5-CT; Others: Valerenic Acid Antagonists: Asenapine Latrepirdine Metitepine/Methiothepin Ritanserin SB-699,551 * Note that the 5-HT_5B receptor is not functional in humans.

5-HT₆	Agonists: Lysergamides: Dihydroergotamine Ergotamine Lisuride LSD Mesulergine Metergoline Methysergide; Tryptamines: 2-Methyl-5-HT 5-BT 5-CT 5-MT Bufotenin E-6801 E-6837 EMD-386,088 EMDT LY-586,713 N-Methyl-5-HT Tryptamine; Others: WAY-181,187 WAY-208,466 Antagonists: Antidepressants: Amitriptyline Amoxapine Clomipramine Doxepin Mianserin Nortriptyline; Atypical antipsychotics: Aripiprazole Asenapine Clorotepine Clozapine Fluperlapine Iloperidone Olanzapine Tiospirone; Typical antipsychotics: Chlorpromazine Loxapine; Others: BGC20-760 BVT-5182 BVT-74316 Cerlapirdine EGIS-12,233 GW-742,457 Ketanserin Latrepirdine Lu AE58054 Metitepine/Methiothepin MS-245 PRX-07034 Ritanserin Ro04-6790 Ro 63-0563 SB-258,585 SB-271,046 SB-357,134 SB-399,885 SB-742,457

5-HT₇	Agonists: Lysergamides: LSD; Tryptamines: 5-CT 5-MT Bufotenin; Others: 8-OH-DPAT AS-19 Bifeprunox E-55888 LP-12 LP-44 RU-24,969 Sarizotan Antagonists: Lysergamides: 2-Bromo-LSD Bromocriptine Dihydroergotamine Ergotamine Mesulergine Metergoline Methysergide; Antidepressants: Amitriptyline Amoxapine Clomipramine Imipramine Maprotiline Mianserin; Atypical antipsychotics: Amisulpride Aripiprazole Clorotepine Clozapine Olanzapine Risperidone Sertindole Tiospirone Ziprasidone Zotepine; Typical antipsychotics: Chlorpromazine Loxapine; Others: Butaclamol EGIS-12,233 Ketanserin LY-215,840 Metitepine/Methiothepin Pimozide Ritanserin SB-258,719 SB-258,741 SB-269,970 SB-656,104 SB-656,104-A SB-691,673 SLV-313 SLV-314 Spiperone SSR-181,507 Vortioxetine

Reuptake inhibitors

SERT	Selective serotonin reuptake inhibitors (SSRIs): Alaproclate Citalopram Dapoxetine Desmethylcitalopram Desmethylsertraline Escitalopram Femoxetine Fluoxetine Fluvoxamine Indalpine Ifoxetine Litoxetine Lubazodone Panuramine Paroxetine Pirandamine RTI-353 Seproxetine Sertraline Tedatioxetine Vilazodone Vortioxetine Zimelidine; Serotonin-norepinephrine reuptake inhibitors (SNRIs): Bicifadine Desvenlafaxine Duloxetine Eclanamine Levomilnacipran Milnacipran Sibutramine Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors (SNDRIs): Brasofensine Diclofensine DOV-102,677 DOV-21,947 DOV-216,303 NS-2359 SEP-225289 SEP-227,162 Tesofensine; Tricyclic antidepressants (TCAs): Amitriptyline Butriptyline Cianopramine Clomipramine Desipramine Dosulepin Doxepin Imipramine Lofepramine Nortriptyline Pipofezine Protriptyline Trimipramine; Tetracyclic antidepressants (TeCAs): Amoxapine; Piperazines: Nefazodone Trazodone; Antihistamines: Brompheniramine Chlorphenamine Diphenhydramine Mepyramine/Pyrilamine Pheniramine Tripelennamine; Opioids: Pethidine Methadone Propoxyphene; Others: Cocaine CP-39,332 Cyclobenzaprine Dextromethorphan Dextrorphan EXP-561 Fezolamine Mesembrine Nefopam PIM-35 Pridefine Roxindole SB-649,915 Ziprasidone

VMAT	Ibogaine Reserpine Tetrabenazine

Releasing agents

Aminoindanes: 5-IAI
AMMI
ETAI
MDAI
MDMAI
MMAI
TAI; Aminotetralins: 6-CAT
8-OH-DPAT
MDAT
MDMAT; Oxazolines: 4-Methylaminorex
Aminorex
Clominorex
Fluminorex; Phenethylamines (also Amphetamines, Cathinones, Phentermines, etc): 2-Methyl-MDA
4-CAB
4-FA
4-FMA
4-HA
4-MTA
5-APDB
5-Methyl-MDA
6-APDB
6-Methyl-MDA
AEMMA
Amiflamine
BDB
BOH
Brephedrone
Butylone
Chlorphentermine
Cloforex
Amfepramone
Metamfepramone
DCA
DFMDA
DMA
DMMA
EBDB
EDMA
Ethylone
Etolorex
Fenfluramine (Dexfenfluramine)
Flephedrone
IAP
IMP
Iofetamine
Lophophine
MBDB
MDA
MDEA
MDHMA
MDMA
MDMPEA
MDOH
MDPEA
Mephedrone
Methedrone
Methylone
MMA
MMDA
MMDMA
MMMA
NAP
Norfenfluramine
4-TFMA
pBA
pCA
pIA
PMA
PMEA
PMMA
TAP; Piperazines: 2C-B-BZP
2-BZP
3-MeOPP
BZP
DCPP
MBZP
mCPP
MDBZP
MeOPP
Mepiprazole
pCPP
pFPP
pTFMPP
TFMPP; Tryptamines: 4-Methyl-αET
4-Methyl-αMT
5-CT
5-MeO-αET
5-MeO-αMT
5-MT
αET
αMT
DMT
Tryptamine (itself); Others: Indeloxazine
Tramadol
Viqualine

Enzyme inhibitors

Anabolism

TPH	AGN-2979 Fenclonine

AAAD	Benserazide Carbidopa Genistein Methyldopa

Catabolism

MAO

Nonselective: Benmoxin
Caroxazone
Echinopsidine
Furazolidone
Hydralazine
Indantadol
Iproclozide
Iproniazid
Isocarboxazid
Isoniazid
Linezolid
Mebanazine
Metfendrazine
Nialamide
Octamoxin
Paraxazone
Phenelzine
Pheniprazine
Phenoxypropazine
Pivalylbenzhydrazine
Procarbazine
Safrazine
Tranylcypromine; MAO-A Selective: Amiflamine
Bazinaprine
Befloxatone
Befol
Brofaromine
Cimoxatone
Clorgiline
Esuprone
Harmala alkaloids (Harmine
Harmaline
Tetrahydroharmine
Harman
Norharman, etc)
Methylene Blue
Metralindole
Minaprine
Moclobemide
Pirlindole
Sercloremine
Tetrindole
Toloxatone
Tyrima

Others

Precursors	L-Tryptophan → 5-HTP

Cofactors	Ferrous iron (Fe²⁺) Magnesium (Mg²⁺) Tetrahydrobiopterin Vitamin B₃ (Niacin Nicotinamide → NADPH) Vitamin B₆ (Pyridoxine Pyridoxamine Pyridoxal → Pyridoxal phosphate) Vitamin B₉ (Folic Acid → Tetrahydrofolic acid) Vitamin C (Ascorbic acid) Zinc (Zn²⁺)

Others	Activity enhancers: BPAP PPAP; Reuptake enhancers: Tianeptine

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American Heritage Dictionary The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved. Read

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