Nelivaptan
(IUPAC ) ime
(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
Klinički podaci
Identifikatori
CAS broj
439687-69-1
ATC kod
?
PubChem [ 1] [ 2]
9895468
ChemSpider [ 3]
8071134
Hemijski podaci
Formula
C 30 H 32 Cl N 3 O 8 S
Mol. masa
630.11 g/mol
SMILES
eMolekuli & PubHem
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
Farmakoinformacioni podaci
Trudnoća
?
Pravni status
Način primene
Oralno
Nelivaptan (INN [ 4] ), kod SSR-149,415 , je selektivni i oralno aktivni ne-peptidni antagonist vazopresinskog receptora koji je selektivan za V1b podtip .[ 5] Lek je bio u kliničkim ispitivanjima za tretman anksioznosti i depresija .[ 6] Jula 2008 , Sanofi-Aventis je objavio da je dalji razvoj ovog leka obustavljen.[ 7]
Literatura
↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.” . Drug Discov Today 15 (23-24): 1052-7. DOI :10.1016/j.drudis.2010.10.003 . PMID 20970519 . edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4 : 217-241. DOI :10.1016/S1574-1400(08)00012-1 .
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining” . J Cheminform 2 (1): 3. DOI :10.1186/1758-2946-2-3 . PMID 20331846 . edit
↑ World Health Organization (2007). „International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 98” . 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. DOI :10.1073/pnas.092012099 . PMC 122955 . PMID 11959912 .
↑ 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. 31. 07. 2008.. Arhivirano iz originala na datum 2008-12-06. Pristupljeno 10. 06. 2009 . »It has been decided to discontinue the development of amibegron and SSR 149415 (a V1B receptor antagonist).«
Vanjske veze
Holecistokinin
CRH
Galanin
Grelin MCH
Melanokortin
Neuropeptid S Neuropeptid Y
Neurotenzin
Opioid Oreksin
Oksitocin Tahikinin
Agonisti :
Supstanca P Antagonisti :
Aprepitant •
Befetupitant •
Kasopitant •
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
Vazopresin