5-HT1B receptor

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5-HT1B receptor

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5-hydroxytryptamine (serotonin) receptor 1B, G protein-coupled

Available structures

PDB

Ortholog search: PDBe, RCSB

List of PDB id codes
2G1X

Identifiers

Symbols

HTR1B; 5-HT1B; 5-HT1DB; HTR1D2; HTR1DB; S12

External IDs

OMIM: 182131 MGI: 96274 HomoloGene: 669 IUPHAR: 5-HT_1B ChEMBL: 1898 GeneCards: HTR1B Gene

Gene Ontology
Molecular function	• signal transducer activity • receptor activity • G-protein coupled receptor activity • serotonin receptor activity • drug binding • serotonin binding
Cellular component	• cytoplasm • plasma membrane • integral to plasma membrane
Biological process	• G-protein coupled receptor internalization • G-protein coupled receptor signaling pathway • G-protein signaling, coupled to cyclic nucleotide second messenger • activation of protein kinase C activity by G-protein coupled receptor protein signaling pathway • serotonin receptor signaling pathway • synaptic transmission • response to toxin • regulation of dopamine secretion • negative regulation of cAMP biosynthetic process • negative regulation of synaptic transmission, GABAergic • response to cocaine • response to drug • drinking behavior • response to ethanol • bone remodeling • response to mineralocorticoid stimulus • negative regulation of synaptic transmission, glutamatergic • cellular response to temperature stimulus
Sources: Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

RefSeq (mRNA)

RefSeq (protein)

Location (UCSC)

Chr 6:
78.17 – 78.17 Mb

Chr 9:
81.52 – 81.53 Mb

PubMed search

[1]

[2]

5-hydroxytryptamine receptor 1B also known as the 5-HT_1B receptor is a protein that in humans is encoded by the HTR1B gene.^[1]^[2] The 5-HT_1B receptor is a 5-HT receptor subtype.^[3]

Contents

1 Tissue distribution and function
2 Ligands
- 2.1 Agonists
- 2.2 Antagonists and inverse agonists
3 Genetics
4 See also
5 References
6 External links
7 Further reading

Tissue distribution and function

The 5-HT_1B receptor acts on the CNS, where it induces presynaptic inhibition and behavioural effects. It also has vascular effects, such as pulmonary vasoconstriction.

Blocking the 5-HT_1B receptor decreases the number of osteoblasts, bone mass, and the bone formation rate.^[4]

5-HT_1B receptors are present in many parts of the human brain. The highest concentrations are found in the basal ganglia, striatum and the frontal cortex.^{[citation needed]} The function of the receptor differs between the areas: in the frontal cortex it is believed to act as a terminal receptor, inhibiting the release of dopamine. In the striatum and the basal ganglia, the 5-HT_1B receptor is thought to act as an autoreceptor, inhibiting the release of serotonin.^[5]

Knockout mice lacking the 5-HT_1B gene have shown an increase of aggression and a higher preference for alcohol.^[6]

Ligands

Agonists

ergotamine (vasoconstrictor in migraine)
sumatriptan (vasoconstrictor in migraine)
zolmitriptan
5-Carboxamidotryptamine
CGS-12066A
CP-93,129 (peripherally acting)
CP-94,253
CP-135,807 (mixed 5-HT_1B/1D agonist)
RU-24969 (mixed 5-HT_1A/1B agonist)

Antagonists and inverse agonists

methiothepin (antipsychotic)
yohimbine (aphrodisiac)
metergoline
isamoltane
AR-A000002^[7]
SB-216,641
SB-224,289 (inverse agonist)^[8]
SB-236,057 (inverse agonist)^[9]

Genetics

In humans the protein is coded by the gene HTR1B.

A genetic variant in the promotor region, A-161T, has been examined with respect to personality traits and showed no major effect.^[10]

References

^ Jin H, Oksenberg D, Ashkenazi A, Peroutka SJ, Duncan AM, Rozmahel R, Yang Y, Mengod G, Palacios JM, O'Dowd BF (March 1992). "Characterization of the human 5-hydroxytryptamine1B receptor". J. Biol. Chem. 267 (9): 5735–8. PMID 1348246.
^ Sanders AR, Cao Q, Taylor J, Levin TE, Badner JA, Cravchik A, Comeron JM, Naruya S, Del Rosario A, Salvi DA, Walczyk KA, Mowry BJ, Levinson DF, Crowe RR, Silverman JM, Gejman PV (February 2001). "Genetic diversity of the human serotonin receptor 1B (HTR1B) gene". Genomics 72 (1): 1–14. doi:10.1006/geno.2000.6411. PMID 11247661.
^ "Entrez Gene: HTR1B 5-hydroxytryptamine (serotonin) receptor 1B". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=3351.
^ Yadav VK, Ryu JH, Suda N, Tanaka KF, Gingrich JA, Schütz G, Glorieux FH, Chiang CY, Zajac JD, Insogna KL, Mann JJ, Hen R, Ducy P, Karsenty G (November 2008). "Lrp5 controls bone formation by inhibiting serotonin synthesis in the duodenum". Cell 135 (5): 825–37. doi:10.1016/j.cell.2008.09.059. PMC 2614332. PMID 19041748. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2614332. Lay summary – medpagetoday.com.
^ Pytliak M, Vargová V, Mechírová V, Felšöci M (2011). "Serotonin receptors - from molecular biology to clinical applications". Physiol Res 60 (1): 15–25. PMID 20945968.
^ Hoyer D, Hannon JP, Martin GR (2002). "Molecular, pharmacological and functional diversity of 5-HT receptors". Pharmacol. Biochem. Behav. 71 (4): 533–54. doi:10.1016/S0091-3057(01)00746-8. PMID 11888546.
^ Hudzik, TJ; Yanek, M; Porrey, T; Evenden, J; Paronis, C; Mastrangelo, M; Ryan, C; Ross, S et al (2003). "Behavioral pharmacology of AR-A000002, a novel, selective 5-hydroxytryptamine(1B) antagonist.". The Journal of Pharmacology and Experimental Therapeutics 304 (3): 1072–84. doi:10.1124/jpet.102.045468. PMID 12604684.
^ Selkirk, JV; Scott, C; Ho, M; Burton, MJ; Watson, J; Gaster, LM; Collin, L; Jones, BJ et al (1998). "SB-224289--a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.". British Journal of Pharmacology 125 (1): 202–8. doi:10.1038/sj.bjp.0702059. PMC 1565605. PMID 9776361. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=1565605.
^ Roberts, C; Watson, J; Price, GW; Middlemiss, DN (2001). "SB-236057-A: a selective 5-HT1B receptor inverse agonist.". CNS Drug Reviews 7 (4): 433–44. PMID 11830759.
^ Tsai SJ, Wang YC, Chen JY, Hong CJ (2003). "Allelic variants of the tryptophan hydroxylase (A218C) and serotonin 1B receptor (A-161T) and personality traits". Neuropsychobiology 48 (2): 68–71. doi:10.1159/000072879. PMID 14504413.

External links

"5-HT_1B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=2312.

Olivier B, van Oorschot R (2006). "5-HT1B receptors and aggression: a review.". Eur. J. Pharmacol. 526 (1–3): 207–17. doi:10.1016/j.ejphar.2005.09.066. PMID 16310769.
Hamblin MW, Metcalf MA, McGuffin RW, Karpells S (1992). "Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity". Biochem. Biophys. Res. Commun. 184 (2): 752–9. doi:10.1016/0006-291X(92)90654-4. PMID 1315531.
Veldman SA, Bienkowski MJ (1992). "Cloning and pharmacological characterization of a novel human 5-hydroxytryptamine1D receptor subtype". Mol. Pharmacol. 42 (3): 439–44. PMID 1328844.
Demchyshyn L, Sunahara RK, Miller K, et al. (1992). "A human serotonin 1D receptor variant (5HT1D beta) encoded by an intronless gene on chromosome 6". Proc. Natl. Acad. Sci. U.S.A. 89 (12): 5522–6. doi:10.1073/pnas.89.12.5522. PMC 49324. PMID 1351684. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=49324.
Levy FO, Gudermann T, Perez-Reyes E, et al. (1992). "Molecular cloning of a human serotonin receptor (S12) with a pharmacological profile resembling that of the 5-HT1D subtype". J. Biol. Chem. 267 (11): 7553–62. PMID 1559993.
Weinshank RL, Zgombick JM, Macchi MJ, et al. (1992). "Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta". Proc. Natl. Acad. Sci. U.S.A. 89 (8): 3630–4. doi:10.1073/pnas.89.8.3630. PMC 48922. PMID 1565658. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=48922.
Mochizuki D, Yuyama Y, Tsujita R, et al. (1992). "Cloning and expression of the human 5-HT1B-type receptor gene". Biochem. Biophys. Res. Commun. 185 (2): 517–23. doi:10.1016/0006-291X(92)91655-A. PMID 1610347.
Nöthen MM, Erdmann J, Shimron-Abarbanell D, Propping P (1995). "Identification of genetic variation in the human serotonin 1D beta receptor gene". Biochem. Biophys. Res. Commun. 205 (2): 1194–200. doi:10.1006/bbrc.1994.2792. PMID 7802650.
Ng GY, George SR, Zastawny RL, et al. (1993). "Human serotonin1B receptor expression in Sf9 cells: phosphorylation, palmitoylation, and adenylyl cyclase inhibition". Biochemistry 32 (43): 11727–33. doi:10.1021/bi00094a032. PMID 8218242.
Bouchelet I, Cohen Z, Case B, et al. (1996). "Differential expression of sumatriptan-sensitive 5-hydroxytryptamine receptors in human trigeminal ganglia and cerebral blood vessels". Mol. Pharmacol. 50 (2): 219–23. PMID 8700126.
Varnäs K, Hall H, Bonaventure P, Sedvall G (2001). "Autoradiographic mapping of 5-HT(1B) and 5-HT(1D) receptors in the post mortem human brain using [(3)H]GR 125743". Brain Res. 915 (1): 47–57. doi:10.1016/S0006-8993(01)02823-2. PMID 11578619.
Salim K, Fenton T, Bacha J, et al. (2002). "Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation". J. Biol. Chem. 277 (18): 15482–5. doi:10.1074/jbc.M201539200. PMID 11854302.
Hasegawa Y, Higuchi S, Matsushita S, Miyaoka H (2002). "Association of a polymorphism of the serotonin 1B receptor gene and alcohol dependence with inactive aldehyde dehydrogenase-2". Journal of neural transmission (Vienna, Austria : 1996) 109 (4): 513–21. doi:10.1007/s007020200042. PMID 11956970.
Hawi Z, Dring M, Kirley A, et al. (2003). "Serotonergic system and attention deficit hyperactivity disorder (ADHD): a potential susceptibility locus at the 5-HT(1B) receptor gene in 273 nuclear families from a multi-centre sample". Mol. Psychiatry 7 (7): 718–25. doi:10.1038/sj.mp.4001048. PMID 12192616.
Strausberg RL, Feingold EA, Grouse LH, et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932. //www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=139241.
Huang YY, Oquendo MA, Friedman JM, et al. (2003). "Substance abuse disorder and major depression are associated with the human 5-HT1B receptor gene (HTR1B) G861C polymorphism". Neuropsychopharmacology 28 (1): 163–9. doi:10.1038/sj.npp.1300000. PMID 12496953.
Quist JF, Barr CL, Schachar R, et al. (2003). "The serotonin 5-HT1B receptor gene and attention deficit hyperactivity disorder". Mol. Psychiatry 8 (1): 98–102. doi:10.1038/sj.mp.4001244. PMID 12556913.
Sinha R, Cloninger CR, Parsian A (2003). "Linkage disequilibrium and haplotype analysis between serotonin receptor 1B gene variations and subtypes of alcoholism". Am. J. Med. Genet. B Neuropsychiatr. Genet. 121 (1): 83–8. doi:10.1002/ajmg.b.20064. PMID 12898580.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Cell surface receptor: G protein-coupled receptors

Class A:
Rhodopsin like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3

Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)

Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)

Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine (D1 D2 D3 D4 D5) Histamine (H1 H2 H3 H4) Melatonin (1A 1B 1C) TAAR (1 2 3 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 (1 2) FPRL1 OXE Prostaglandin (DP (1 2), EP (1 2 3 4), FP) Prostacyclin Thromboxane

Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Lactate Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Niacin (1 2) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide	B/W (1 2) FF (1 2) S Y (1 2 4 5) Neuromedin (B U (1 2)) Neurotensin (1 2)

Other	Anaphylatoxin (C3a C5a) Angiotensin (1 2) Apelin Bombesin (BRS3 GRPR NMBR) Bradykinin (B1 B2) Chemokine Cholecystokinin (A B) Endothelin (A B) Formyl peptide (1 2 3) FSH Galanin (1 2 3) GHB receptor Gonadotropin-releasing hormone (1 2) Ghrelin Kisspeptin Luteinizing hormone/choriogonadotropin MAS (1 1L D E F G X1 X2 X3 X4) Melanocortin (1 2 3 4 5) MCHR (1 2) Motilin Opioid (Delta Kappa Mu Nociceptin & Zeta, but not Sigma) Orexin (1 2) Oxytocin Prokineticin (1 2) Prolactin-releasing peptide Relaxin (1 2 3 4) Somatostatin (1 2 3 4 5) Tachykinin (1 2 3) Thyrotropin Thyrotropin-releasing hormone Urotensin-II Vasopressin (1A 1B 2)

Miscellaneous

Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)

Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin like

Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)

Other	Brain-specific angiogenesis inhibitor (1 2 3) Cadherin (1 2 3) Calcitonin CALCRL CD97 Corticotropin-releasing hormone (1 2) EMR (1 2 3) Glucagon (GR GIPR GLP1R GLP2R) Growth hormone releasing hormone PACAPR1 GPR Latrophilin (1 2 3 ELTD1) Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic
glutamate / pheromone

Taste	TAS1R (1 2 3) TAS2R (1 3 4 5 8 9 10 12 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50)

Other	Calcium-sensing receptor GABA B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F:
Frizzled / Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)

Smoothened	Smoothened

B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)

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 Naluzotan 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 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 Glemanserin 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 (Dexfenfluramine, Levofenfluramine) 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 CEPC 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 Tropanserin 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 Omiloxetine Panuramine Paroxetine Pirandamine RTI-353 Seproxetine Sertraline 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 Tedatioxetine 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 Tofenacin 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, Levofenfluramine)
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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5-HT1B receptor

5-HT1B receptor

Tissue distribution and function

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Agonists

Antagonists and inverse agonists

Genetics

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