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Naluzotan

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Naluzotan
Systematic (IUPAC) name
N-(3-{4-[4-(1-cyclohexylmethanesulfonamido)butyl]piperazin-1-yl}phenyl)acetamide
Clinical data
Pregnancy cat.  ?
Legal status  ?
Routes Oral[1]
Identifiers
CAS number 740873-06-7
ATC code None
PubChem CID 11430856
ChemSpider 9605731
UNII LQ54E5B4EW YesY
Chemical data
Formula C23H38N4O3S 
Mol. mass 450.638 g/mol
SMILES eMolecules & PubChem
 YesY (what is this?)  (verify)

Naluzotan (INN, USAN; PRX-00023) is a serotonergic drug of the phenylpiperazine class that was under investigation by EPIX Pharmaceuticals Inc for the treatment of generalized anxiety disorder and major depressive disorder.[1][2] It acts as a selective and potent 5-HT1A receptor partial agonist,[2][3] readily stimulating prolactin responses,[4] though it has also been found to bind to and activate the σ receptor.[5] Naluzotan was well-tolerated in clinical trials,[4] with more patients in the control group dropping out due to adverse effects than in the active group in one study.[2] The most frequently reported side effect was headache in 15% of patients (compared to 10% for placebo).[2] In addition, naluzotan demonstrated significant antidepressant and anxiolytic effects as per the HAM-D and MADRS and the HAM-A, respectively, in some trials,[2] but in others it did not.[6][7] In the end it was not found to be significantly superior enough to placebo and development was stopped.[7]

See also

References

  1. ^ a b de Paulis T. (2007). "Drug evaluation: PRX-00023, a selective 5-HT1A receptor agonist for depression.". Curr Opin Investig Drugs. 8 (1): 78–86. PMID 17263189. 
  2. ^ a b c d e Rickels K, Mathew S, Banov MD, Zimbroff DL, Oshana S, Parsons EC Jr, Donahue SR, Kauffman M, Iyer GR, Reinhard JF Jr. (2008). "Effects of PRX-00023, a novel, selective serotonin 1A receptor agonist on measures of anxiety and depression in generalized anxiety disorder: results of a double-blind, placebo-controlled trial.". J Clin Psychopharmacol. 28 (2): 235–239. doi:10.1097/JCP.0b013e31816774de. PMID 18344738. 
  3. ^ Becker OM, Dhanoa DS, Marantz Y, Chen D, Shacham S, Cheruku S, Heifetz A, Mohanty P, Fichman M, Sharadendu A, Nudelman R, Kauffman M, Noiman S. (2006). "An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression". J Med Chem. 49 (11): 3116–3135. doi:10.1021/jm0508641. PMID 16722631. 
  4. ^ a b de Paulis T.; Reinhard Jr, JF; Oshana, S; Kauffman, M; Donahue, S (2007). "Tolerability, pharmacokinetics, and neuroendocrine effects of PRX-00023, a novel 5-HT1A agonist, in healthy subjects.". J Clin Pharmacol. 47 (7): 817–824. doi:10.1177/0091270007300953. PMID 17495280. 
  5. ^ Prof John Kelly (2010). Principles of CNS Drug Development: From Test Tube to Patient. New York: Wiley. ISBN 0-470-51979-7. http://books.google.com/?id=pfY3xcsu6EsC&lpg=PA265&dq=adatanserin&pg=PA265#v=onepage&q=PRX-00023. 
  6. ^ Mathew SJ, Garakani A, Reinhard JF Jr, Oshana S, Donahue S. (2008). "Short-term tolerability of a nonazapirone selective serotonin 1A agonist in adults with generalized anxiety disorder: a 28-day, open-label study". Clin Ther. 30 (9): 1658–1666. doi:10.1016/j.clinthera.2008.09.006. PMID 18840371. 
  7. ^ a b Kirchhoff VD, Nguyen HT, Soczynska JK, Woldeyohannes H, McIntyre RS (October 2009). "Discontinued psychiatric drugs in 2008". Expert Opinion on Investigational Drugs 18 (10): 1431–43. doi:10.1517/13543780903184591. PMID 19715445. http://informahealthcare.com/doi/abs/10.1517/13543780903184591. 
GABAA PAMs
Abecarnil • Adipiplon • Alpidem • CGS-8216 • CGS-9896 • CGS-13767 • CGS-20625 • Divaplon • ELB-139 • Fasiplon • GBLD-345 • Gedocarnil • L-838,417 • NS-2664 • NS-2710 • Ocinaplon • Pagoclone • Panadiplon • Pipequaline • RWJ-51204 • SB-205,384 • SL-651,498 • Taniplon • TP-003 • TP-13 • TPA-023 • Y-23684 • ZK-93423
Others
α2δ VDCC Blockers
5-HT1A Agonists
Azapirones: Buspirone • Gepirone • Tandospirone; Others: Flesinoxan • Naluzotan • Oxaflozane
H1 Antagonists
Diphenylmethanes: Captodiame • Hydroxyzine; Others: Brompheniramine • Chlorpheniramine • Pheniramine
CRH1 Antagonists
NK2 Antagonists
MCH1 antagonists
mGluR2/3 Agonists
mGluR5 NAMs
TSPO agonists
σ1 agonists
Others

M: PSO/PSI

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc(eval/thrp), drug(N5A/5B/5C/6A/6B/6D)
Receptor
Ligands
3-PPP • 4-IBP • 4-PPBP • Afobazole • Allylnormetazocine • Amitriptyline • Amphetamine • Berberine • Citalopram • Clorgyline • Cocaine • Cyclazocine • Dextrallorphan • Dextromethorphan • Dextrorphan • DTG • BD-1,008 • Desipramine • DHEA • Dimethyltryptamine • Dimemorfan • Ditolylguanidine • EMD-57,445 • Escitalopram • Fluoxetine • Fluvoxamine • Heroin • Igmesine • Imipramine • JO-1,784 • L-687,384 • Lamotrigine • Lu 28-179 • MDMA • Methamphetamine • Morphine • Naluzotan • Noscapine • OPC-14,523 • Opipramol • PB-28 • PD-144,415 • Pentazocine • Pentoxyverine • Phencyclidine • PRE-084 • Pregnenolone • RTI-55 • SA-4503 • Sertraline • Siramesine • Venlafaxine
BD-1,047 • BD-1,063 • BMY-14,802 • E-5,842 • Haloperidol • NE-100 • Progesterone • Rimcazole • SM-21
Unknown


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