Serlopitant

Serlopitant
Clinical data

Routes of administration	By mouth
ATC code	None
Identifiers
IUPAC name 3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}-4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]cyclopent-2-en-1-one
CAS Number	860642-69-9
PubChem CID	23653789
ChemSpider	24686685
UNII	277V92K32B
KEGG	D09378
ChEMBL	CHEMBL447955
Chemical and physical data
Formula	C₂₉H₂₈F₇NO₂
Molar mass	555.527 g/mol
3D model (JSmol)	Interactive image
SMILES C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)O[C@H]2CC[C@@H]3CN(C[C@H]3[C@@H]2C4=CC=C(C=C4)F)C5=CC(=O)CC5
InChI InChI=1S/C29H28F7NO2/c1-16(19-10-20(28(31,32)33)12-21(11-19)29(34,35)36)39-26-9-4-18-14-37(23-7-8-24(38)13-23)15-25(18)27(26)17-2-5-22(30)6-3-17/h2-3,5-6,10-13,16,18,25-27H,4,7-9,14-15H2,1H3/t16-,18-,25-,26+,27+/m1/s1 Key:FLNYCRJBCNNHRH-OIYLJQICSA-N

Serlopitant (INN,^[1] codenamed VPD-737) is a drug which acts as an NK₁ receptor antagonist. It was assessed in clinical trials for the treatment of urinary incontinence and overactive bladder, but while it was superior to placebo it provided no advantage over existing approved drugs, and was not approved for further development.^[2]^[3]

References

↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 62" (PDF). World Health Organization. 2009. pp. 261–2. Retrieved 17 November 2016.
↑ Frenkl, TL; Zhu, H; Reiss, T; Seltzer, O; Rosenberg, E; Green, S (August 2010). "A Multicenter, Double-Blind, Randomized, Placebo Controlled Trial of a Neurokinin-1 Receptor Antagonist for Overactive Bladder". The Journal of Urology. 184 (2): 616–22. PMID 20639026. doi:10.1016/j.juro.2010.03.147.
↑ Payton, S (August 2010). "Urinary Incontinence: Neurokinin Receptor Antagonist Inferior to Tolterodine for OAB". Nature Reviews Urology. 7 (8): 418. PMID 20726068. doi:10.1038/nrurol.2010.105.

Neurokinin receptor modulators
NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant
NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant
NK₃	Agonists: Neurokinin B Senktide Antagonists: Fezolinetant (ESN-364) MLE-4901 (AZD-2624, AZD-4901) Osanetant (SR-142,801) SB-218,795 SB-222,200 Talnetant (SB-223,412)
See also: Receptor/signaling modulators • Signaling peptide/protein receptor modulators

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