Nelivaptan

Nelivaptan
Clinical data

Routes of administration	Oral
ATC code	none
Identifiers
IUPAC name (2S,4R)-1-[(3R)-5-chloro-1-(2,4-dimethoxyphenyl)sulfonyl-3-(2-methoxyphenyl)-2-oxo-indolin-3-yl]-4-hydroxy-N,N-dimethyl-pyrrolidine-2-carboxamide
CAS Number	439687-69-1^N
PubChem CID	9895468
IUPHAR/BPS	2202
ChemSpider	8071134^Y
UNII	3TY57MQ4OA
ChEMBL	CHEMBL582857^Y
ECHA InfoCard	100.210.987
Chemical and physical data
Formula	C₃₀H₃₂ClN₃O₈S
Molar mass	630.11 g/mol
InChI InChI=1S/C30H32ClN3O8S/c1-32(2)28(36)24-15-19(35)17-33(24)30(21-8-6-7-9-25(21)41-4)22-14-18(31)10-12-23(22)34(29(30)37)43(38,39)27-13-11-20(40-3)16-26(27)42-5/h6-14,16,19,24,35H,15,17H2,1-5H3/t19-,24+,30+/m1/s1^Y Key:NJXZWIIMWNEOGJ-WEWKHQNJSA-N^Y
^NY (what is this?) (verify)

Nelivaptan (INN)^[1] (developmental codename SSR-149,415) is a selective, orally active, non-peptide vasopressin receptor antagonist selective for the V_1B subtype.^[2] The drug had entered clinical trials for treatment of anxiety and depression.^[3] In July 2008, Sanofi-Aventis announced that further development of this drug had been halted.^[4]

References

↑ World Health Organization (2007). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 98" (PDF). WHO Drug Information. 21 (4): 341.
↑ Griebel G, Simiand J, Serradeil-Le Gal C, Wagnon J, Pascal M, Scatton B, Maffrand JP, Soubrie P (2002). "Anxiolytic- and antidepressant-like effects of the non-peptide vasopressin V1b receptor antagonist, SSR149415, suggest an innovative approach for the treatment of stress-related disorders". Proc. Natl. Acad. Sci. U.S.A. 99 (9): 6370–5. PMC 122955 . PMID 11959912. doi:10.1073/pnas.092012099.
↑ Serradeil-Le Gal C, Wagnon J, Tonnerre B, Roux R, Garcia G, Griebel G, Aulombard A (2005). "An overview of SSR149415, a selective nonpeptide vasopressin V(1b) receptor antagonist for the treatment of stress-related disorders". CNS Drug Reviews. 11 (1): 53–68. PMID 15867952. doi:10.1111/j.1527-3458.2005.tb00035.x.
↑ "Second-quarter 2008 results" (PDF). Press Release. Sanofi-Aventis. 2008-07-31. Retrieved 2009-06-10. It has been decided to discontinue the development of amibegron and SSR 149415 (a V1B receptor antagonist).

SSR149415 at the US National Library of Medicine Medical Subject Headings (MeSH)

V_1A	Agonists: Felypressin Lypressin Ornipressin Selepressin Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LY-307174 PF-184563 Relcovaptan RG7314 SRX246 SRX251 TC OT 39 WAY-267464 YM-218 YM-471 YM-35471
V_1B	Agonists: Desmopressin Felypressin Lypressin Ornipressin Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: ABT-436 ABT-558 Nelivaptan ORG-52186 (SCH-740935) TASP-0233278 TASP-0390325 TS-121 Ligands: TASP-699
V₂	Agonists: Desmopressin Felypressin Lypressin Ornipressin TC OT 39 Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: Conivaptan JNJ-17079166 Lixivaptan Mozavaptan RWJ-351647 Satavaptan Tolvaptan YM-471 YM-35471
Unsorted	Antagonists: Ribuvaptan RWJ-339489 VMAX-367 VMAX-372 VMAX-382 YM-222546 Other inhibitors: Demeclocycline Lithium (lithium carbonate)

Others

See also: Receptor/signaling modulators; Signaling peptide/protein receptor modulators

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