Revefenacin

Sunan Sinadari:

1- (2- (3- ((4-carbamoylpiperidin-1-yl)methyl) -N-methylbenzamido) ethyl) piperidin-4-yl [1,1'-biphenyl] -2-ylcarbamate

Lambar SMILES:

O=C(OC1CCN(CCN(C)C(C2=CC=C(CN3CCC(C(N)=O)CC3)C=C2=O)CC1)NC4=CC=CC=C4C5=CC=CC= C5

Lambar InChi:

InChi=1S/C35H43N5O4/c1-38(34(42)29-13-11-26(12-14-29)25-40-19-15-28(16-20-40)33(36)41) 23-24-39-21-17- 30 (18-22-39) 44-35 (43) 37-32-10-6-5-9-31 (32)27-7-3-2-4-8-27/h2-14,28, 30H,15-25H2,1H3,(H2,36,41)(H,37,43)

InChi Key:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Mabuɗin kalma:

Revefenacin, TD-4208, GSK-1160724, TD4208, TD 4208, GSK1160724, GSK 1160724, 864750-70-9

Solubility:Mai narkewa a cikin DMSO

Ajiya:0 - 4°C na gajeren lokaci (kwanaki zuwa makonni), ko -20°C na dogon lokaci (watanni).

Bayani:

A cikin Vitro: Kis na revefenacin sune 0.42, 0.32, 0.18, 0.56, da 6.7 nM a cikin masu karɓar M1, M2, M3, M4 da M5, bi da bi. A cikin gwajin aiki, ana nuna revefenacin a matsayin antagonist mai aiki tare da abubuwan hanawa mai kama da ɗaure Ki's. Revefenacin kuma yana hana agonist-induced agonist na Guinea alade keɓewar zobe na tracheal tare da kusanci na 0.1 nM, kama da ma'aunin M3 biding Ki[1]. A cikin Vivo: A cikin karnuka masu anesthetize, revefenacin, tare da tiotropium da glycopyrronium, suna samar da ci gaba da hanawa na bronchoconstriction na acetylcholine har zuwa awanni 24. A cikin berayen da ba su da ƙarfi, revefenacin da aka shayar da su yana nuna kariyar bronchoprotection na sa'o'i 24 da ke dogara ga allurai daga cututtukan da ke haifar da methacholine. Ƙimar ƙarfin sa'o'i 24 shine 45.0 μg/mL kuma ana kiyaye ƙarfin bronchoprotective bayan kwanaki 7 na maganin yau da kullum sau ɗaya [2].

manufa: mAChR