BMY-14802

BMY-14802
Clinical data
Other names	BMS-181100; MJ-14802
ATC code	None;
Identifiers
	IUPAC name 1-(4-fluorophenyl)-4-[4-(5-fluoropyrimidin-2-yl)piperazin-1-yl]butan-1-ol;
CAS Number	105565-56-8 ;
PubChem CID	108046;
IUPHAR/BPS	8;
ChemSpider	97151 ;
UNII	A5NB5G07JO;
ChEMBL	ChEMBL60859 ;
CompTox Dashboard (EPA)	DTXSID70909596 ;
Chemical and physical data
Formula	C18H22F2N4O
Molar mass	348.398 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c1cc(F)ccc1C(O)CCCN2CCN(CC2)c3ncc(F)cn3;
	InChI InChI=1S/C18H22F2N4O/c19-15-5-3-14(4-6-15)17(25)2-1-7-23-8-10-24(11-9-23)18-21-12-16(20)13-22-18/h3-6,12-13,17,25H,1-2,7-11H2 ; Key:ZXUYYZPJUGQHLQ-UHFFFAOYSA-N ;
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BMY-14802, also known as BMS-181100, is a drug with antipsychotic effects which acts as both a sigma receptor antagonist and a 5-HT_1A receptor agonist.^[1]^[2]^[3]^[4] It also has affinity for the 5-HT₂ and D₄ receptors.^[5] The drug reached phase III clinical trials for the treatment of psychosis but was never marketed.^[6]

References

^ Taylor DP, Eison MS, Moon SL, Schlemmer RF, Shukla UA, VanderMaelen CP, et al. (1993). "A role for sigma binding in the antipsychotic profile of BMY 14802?". NIDA Research Monograph. 133: 125–157. PMID 8232511.
^ Vanecek SA, Essman WD, Taylor DP, Woods JH (January 1998). "Discriminative stimulus characteristics of BMY 14802 in the pigeon". The Journal of Pharmacology and Experimental Therapeutics. 284 (1): 1–9. PMID 9435153.
^ Kitanaka J, Kitanaka N, Tatsuta T, Hall FS, Uhl GR, Tanaka K, et al. (May 2009). "Sigma1 receptor antagonists determine the behavioral pattern of the methamphetamine-induced stereotypy in mice". Psychopharmacology. 203 (4): 781–792. doi:10.1007/s00213-008-1425-z. PMC 3157915. PMID 19052726.
^ Paquette MA, Foley K, Brudney EG, Meshul CK, Johnson SW, Berger SP (July 2009). "The sigma-1 antagonist BMY-14802 inhibits L-DOPA-induced abnormal involuntary movements by a WAY-100635-sensitive mechanism". Psychopharmacology. 204 (4): 743–754. doi:10.1007/s00213-009-1505-8. PMC 2845289. PMID 19283364.
^ Zamanillo D, Portillo-Salido E, Vela JM, Romero L (20 April 2012). "Sigma 1 Receptor Chaperone: Pharmacology and Therapeutic Perspectives". In Botana LM, Loza M (eds.). Therapeutic Targets: Modulation, Inhibition, and Activation. John Wiley & Sons. pp. 248–. ISBN 978-1-118-18552-0.
^ "BMS 181100". AdisInsight. Springer Nature Switzerland AG.

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