Revefenacin

Izina ryimiti:

1- (2- (3 - (

Kode ya 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

InChi Code:

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 Urufunguzo:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Ijambo ryibanze:

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

Gukemura:Gukemura muri DMSO

Ububiko:0 - 4 ° C mugihe gito (iminsi kugeza ibyumweru), cyangwa -20 ° C mugihe kirekire (amezi).

Ibisobanuro:

Muri Vitro K Kis ya revefenacin ni 0.42, 0.32, 0.18, 0.56, na 6.7 nM kubantu M1, M2, M3, M4 na M5. Mubisobanuro bikora, revefenacin yerekanwe kuba antagonist ikora hamwe no guhagarika ibintu bisa no guhuza Ki. Revefenacin irabuza kandi kugabanuka kwa agonist iterwa no guineya ingurube yitaruye impeta ya tracheal hamwe na 0.1 nM, bisa na M3 yapimwe Ki [1]. Muri Vivo ： Mu mbwa zatewe aneste, revefenacin, hamwe na tiotropium na glycopyrronium, bitanga uburyo buhoraho bwo kubuza acetyloline iterwa na bronchoconstriction mu gihe cyamasaha 24. Imbeba zatewe anesthete, revefenacin yashizwemo yerekana urugero-rwinshi rwamasaha 24 ya bronchoprotection yo kurwanya methacholine iterwa na bronchoconstriction. Ikigereranyo cy’amasaha 24 ni 45.0 µg / mL kandi imbaraga za bronchoprotective zikomeza nyuma yiminsi 7 yo kunywa inshuro imwe kumunsi [2].

Intego: mAChR