Revefenacin

Nomen chemicum:

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

SMILES Code:

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 Key:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Keyword:

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

Solubilitas:Solutum in DMSO

Repono:0 - 4°C ad terminum brevem (dies ad septimanas), vel -20°C ad terminum longi (menses).

Descriptio:

In Vitro：The Kis revefenacin sunt 0.42, 0.32, 0.18, 0.56, et 6.7 nM apud homines M1, M2, M3, M4 et M5 receptores respective. In operando tentamen, revefenacin monstratur praecipuum functionis esse cum inhibitione constantibus similibus ligandi Ki's. Revefenacin etiam agonistam inducta contractionem Guineae sus anuli arteriae solitariae praeparationem cum affinitate 0.1 nM, similis mensurati M3 iubentis Ki[1]. In Vivo：In anesthetizato canes, revefenacin, cum tiotropio et glycopyrronio, inhibitionem acetylcholini bronchoconstrictionis usque ad 24 horas sustentatam efficiunt. In anesthetizato mures, revefenacin haustus, exhibet bronchoprotectionem dosis dependens 24-horam contra methacholinum bronchoconstrictionem inductam. Potentia aestimata 24-horarum est 45.0 µg/mL et bronchoprotectivae potentiae post 7 dies semel indies dosing conservantur.

Scopum: mACHR