Refenacin

Ingoa matū:

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

Waehere 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

Waehere 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)

Kī InChi:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Kupumatua:

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

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama).

Whakaahuatanga:

In Vitro：Ko te Kis o te revefenacin he 0.42, 0.32, 0.18, 0.56, me te 6.7 nM i nga kaiwhakawhiwhi M1, M2, M3, M4 me M5 tangata. I roto i te whakamatautau mahi, ka whakaatuhia te revefenacin he kaitukino mahi me nga taumau aukati e rite ana ki te here a Ki. Ka aukati ano a Revefenacin i te whakahekenga agonist-induced o te poaka guinea taratahi whakakai taratahi me te affinity o 0.1 nM, he rite ki te M3 biding Ki[1] kua ine. I roto i te Vivo：I roto i nga kurī whakamohoatanga, ko te revefenacin, me te tiotropium me te glycopyrronium, ka whakaputa i te aukati tonu o te acetylcholine-induced bronchoconstriction mo te 24 haora. I roto i nga kiore kua whakahiatohia, ko te revefenacin kua whakangohuhia e whakaatu ana i te bronchoprotection 24-haora i te horopeta ki te bronchoconstriction na te methacholine. Ko te kaha o te 24-haora ko te 45.0 µg/mL ka mau tonu te kaha o te bronchoprotective i muri i nga ra e 7 o te horopeta kotahi ia ra[2].

Whāinga: mAChR