Revefenacin

Non Chimik:

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

Kòd 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

Kòd 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 kle:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Mot:

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

Solibilite:Soluble nan DMSO

Depo:0 - 4 ° C pou kout tèm (jou a semèn), oswa -20 ° C pou tèm long (mwa).

Deskripsyon:

In vitro: Kis nan revefenacin se 0.42, 0.32, 0.18, 0.56, ak 6.7 nM nan reseptè moun M1, M2, M3, M4 ak M5, respektivman. Nan yon tès fonksyonèl, revefenacin montre yo dwe yon antagonist fonksyonèl ak konstan anpèchman ki sanble ak Ki obligatwa. Revefenacin tou inibit kontraksyon agonist-induit nan preparasyon bag tracheal izole kochon Gine ak yon afinite nan 0.1 nM, menm jan ak mezire M3 Biding Ki [1]. In Vivo: Nan chen anestezi, revefenacin, ansanm ak tiotropium ak glikopyrronium, pwodui anpèchman soutni bronkokonstriksyon asetilkolin-induit pou jiska 24 èdtan. Nan rat anestezi, revefenacin respire montre bronkopwoteksyon 24 èdtan ki depann de dòz la kont bwonkokonstriksyon metakolin-induit. Estimasyon puisans 24 èdtan an se 45.0 µg/mL ak puisans bronchoprotective yo kenbe apre 7 jou nan dòz yon fwa chak jou[2].

Sib: mAChR