Nelivaptan

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Nelivaptan

Systematic (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
Clinical data
Pregnancy cat.	?
Legal status	?
Routes	Oral
Identifiers
CAS number	439687-69-1^N
ATC code	None
PubChem	CID 9895468
ChemSpider	8071134^Y
UNII	3TY57MQ4OA^Y
ChEMBL	CHEMBL582857^Y
Chemical data
Formula	C₃₀H₃₂Cl N₃O₈S
Mol. 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
N (what is this?) (verify)

Nelivaptan (INN^[1]), codenamed SSR-149,415, is a selective and orally active non-peptide vasopressin receptor antagonist selective for the V1b 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]

[edit] References

^ World Health Organization (2007). "International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 98". WHO Drug Information 21 (4): 341. http://www.who.int/medicines/publications/druginformation/innlists/P-List98.pdf.
^ 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. doi:10.1073/pnas.092012099. PMC 122955. PMID 11959912. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=122955.
^ 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. doi:10.1111/j.1527-3458.2005.tb00035.x. PMID 15867952.
^ "Second-quarter 2008 results". Press Release. Sanofi-Aventis. 2008-07-31. http://en.sanofi-aventis.com/binaries/20080731_results2008_Q2_CP_EN_tcm28-20271.pdf. Retrieved 2009-06-10. "It has been decided to discontinue the development of amibegron and SSR 149415 (a V1B receptor antagonist)."

[edit] External links

MeSH SSR149415

Hypothalamic-pituitary hormones and analogues (H01)

GNRH	Agonists: Gonadorelin Nafarelin Histrelin Antagonists: Cetrorelix Ganirelix

Somatostatin	Agonists: Lanreotide Octreotide Pasireotide

Anterior pituitary

ACTH	Agonists: Corticotropin Cosyntropin Tetracosactide

GH	Agonists: IGF-1 (Mecasermin/Mecasermin rinfabate) Sermorelin Somatrem Antagonists: Pegvisomant

TSH	Agonists: Thyrotropin

Posterior pituitary

Oxytocin	Agonists: Carbetocin Demoxytocin Antagonists: Atosiban

Vasopressin	Agonists: Argipressin Desmopressin Felypressin Lypressin Ornipressin Terlipressin Antagonists: Conivaptan Demeclocycline Lixivaptan Mozavaptan Nelivaptan Relcovaptan Satavaptan Tolvaptan

anat/phys/devp/horm

noco(d)/cong/tumr, sysi/epon

proc, drug (A10/H1/H2/H3/H5)

Neuropeptidergics

Cholecystokinin

CCK_A	Agonists: Cholecystokinin CCK-4 Antagonists: Asperlicin Proglumide Lorglumide Devazepide Dexloxiglumide

CCK_B	Agonists: Cholecystokinin CCK-4 Gastrin Antagonists: Proglumide CI-988

CRF₁	Agonists: Corticotropin releasing hormone Antagonists: Antalarmin CP-154,526 Pexacerfont

CRF₂	Agonists: Corticotropin releasing hormone

GAL₁	Agonists: Galanin Galanin-like peptide Galmic Galnon

GAL₂	Agonists: Galanin Galanin-like peptide Galmic Galnon

GAL₃	Agonists: Galanin Galmic Galnon

MCH₁	Agonists: Melanin concentrating hormone Antagonists: ATC-0175 GW-803,430 NGD-4715 SNAP-7941 SNAP-94847

MCH₂	Agonists: Melanin concentrating hormone

MC₁	Agonists: alpha-MSH Afamelanotide BMS-470,539 Bremelanotide Melanotan II Antagonists: Agouti signalling peptide

MC₂	Agonists: ACTH Cosyntropin Tetracosactide

MC₃	Agonists: alpha-MSH Bremelanotide Melanotan II

MC₄	Agonists: alpha-MSH Bremelanotide Melanotan II PF-00446687 THIQ Antagonists: Agouti-related peptide

MC₅	Agonists: alpha-MSH Melanotan II

Agonists: Neuropeptide S
Antagonists: SHA-68

Y₁	Agonists: Neuropeptide Y Peptide YY Antagonists: BIBP-3226

Y₂	Agonists: Neuropeptide Y Peptide YY Antagonists: BIIE-0246

Y₄	Agonists: Neuropeptide Y Pancreatic polypeptide Peptide YY Antagonists: UR-AK49

Y₅	Agonists: Neuropeptide Y Peptide YY Antagonists: Lu AA-33810

NTS₁	Agonists: Neurotensin Neuromedin N Antagonists: SR-48692 SR-142,948

NTS₂	Agonists: Neurotensin Antagonists: Levocabastine SR-142,948

see Template:Opioids

OX₁	Agonists: Orexin-A Antagonists: Almorexant SB-334,867 SB-408,124 SB-649,868 Suvorexant

OX₂	Agonists: Orexin-A Antagonists: Almorexant SB-649,868 Suvorexant TCS-OX2-29

NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Casopitant CI-1021 CP-96,345 CP-99,994 CP-122,721 Dapitant Ezlopitant FK-888 Fosaprepitant GR-203,040 GW-597,599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306,740 Maropitant Netupitant NKP-608 Nolpitantium Orvepitant RP-67,580 SDZ NKT 343 Vestipitant Vofopitant

NK₂	Agonists: Neurokinin A Antagonists: GR-159,897 Ibodutant Saredutant

NK₃	Agonists: Neurokinin B Antagonists: Osanetant Talnetant

V_1A	Agonists: Desmopressin Felypressin Ornipressin Terlipressin Vasopressin Antagonists: Conivaptan Demeclocycline Relcovaptan

V_1B	Agonists: Felypressin Ornipressin Terlipressin Vasopressin Antagonists: Demeclocycline Nelivaptan

V₂	Agonists: Desmopressin Ornipressin Vasopressin Antagonists: Conivaptan Demeclocycline Lixivaptan Mozavaptan Satavaptan Tolvaptan

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