I-Revefenacin

Igama Lekhemikhali:

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

Ikhodi ye-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

Ikhodi ye-InChi:

I-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)

I-InChi Key:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga).

Incazelo:

Ku-Vitro:I-Kis ye-revefenacin ingu-0.42, 0.32, 0.18, 0.56, kanye no-6.7 nM kuma-receptors womuntu we-M1, M2, M3, M4 kanye ne-M5, ngokulandelana. Ekuhlolweni kokusebenza, i-revefenacin iboniswa iwumbangi osebenzayo onokusebenza okuqinile okufana nokubopha kwe-Ki. I-Revefenacin iphinde ivimbele ukufinyela okubangelwa i-agonist kwe-guinea pig ehlukanisiwe yokulungiselela indandatho kaqhoqhoqho ene-affinity engu-0.1 nM, efana ne-M3 biding Ki[1] elinganiselwe. Ku-Vivo:Ezinja ezilaliswa izinzwa, i-revefenacin, kanye ne-tiotropium ne-glycopyrronium, ikhiqiza ukuvinjelwa okuqhubekayo kwe-acetylcholine-induced bronchoconstriction amahora angafika kwangu-24. Emagundaneni abulawa izinzwa, i-revefenacin ehogeliwe ibonisa i-bronchoprotection encike kumthamo wamahora angu-24 ngokumelene ne-methacholine-induced bronchoconstriction. Amandla alinganiselwe wamahora angu-24 ngu-45.0 µg/mL futhi amandla e-bronchoprotective ayagcinwa ngemva kwezinsuku ezingu-7 zomthamo kanye ngosuku[2].

Ithagethi: mAChR