Revefenacin

Magaca Kiimikada:

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

Koodhka dhoola cadeynta:

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

Koodhka 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)

Furaha InChi:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Ereyga muhiimka ah:

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

Xalka:Ku milmay DMSO

Kaydinta:0 - 4°C muddo gaaban (maalmo ilaa toddobaadyo), ama -20°C muddo dheer (bilo).

Sharaxaad:

In Vitro: Kis of revefenacin waa 0.42, 0.32, 0.18, 0.56, iyo 6.7 nM ee aadanaha M1, M2, M3, M4 iyo M5, siday u kala horreeyaan. Marka la eego qiimaynta shaqaynaysa, revefenacin waxa lagu tusay in uu yahay ka soo horjeeda shaqaynaysa oo leh xannibaado joogto ah oo la mid ah xidhitaanka Ki's. Revefenacin waxay sidoo kale joojisaa foosha agonist-ku-takoorka ee diyaargarowga giraanta tracheal go'doonsan ee doofaarka oo xiriir la leh 0.1 nM, oo la mid ah qiyaasta M3 biding Ki[1]. Gudaha Vivo: Eeyaha la suuxiyay, revefenacin, oo ay weheliso tiotropium iyo glycopyrronium, waxay soo saartaa xannibaad joogto ah oo xanuunka bronchoconstriction-ku keeno acetylcholine ilaa 24 saacadood. Jiirka la suuxiyay, revefenacin ee la nuugo waxay muujinaysaa ka hortagga bronchoconstriction 24-ka saac ee ku-tiirsan ee ka hortagga bronchoconstriction-ku keeno methacholine. Qiyaasta awoodda 24-saac waa 45.0 µg/mL iyo awooda bronchoprotective waa la ilaaliyaa 7 maalmood ka dib qaadashada hal mar maalintii[2].

Hadafka: mAChR