Batefeenterol

Orukọ Kemikali:

"(R) -1- (3- ((2-chloro-4--)- ((2-hydroxy-2- (8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl) ethyl)amino) methyl -5-methoxyphenyl) amino) -3-oxopropyl) piperidin-4-yl [1,1'-biphenyl] -2-ylcarbamate Batefenterol Succinate"

KỌỌDỌ SMILES:

O=C(OC1CCN(CCC(NC2=CC(OC))=C(CNC[C@H](O)C3=CC=C(O)C4=C3C=CC(N4)=O)C=C2Cl)= O)CC1)NC5=CC=CC=C5C6=CC=CC=C6

Koodu InChi:

InChi=1S/C40H42ClN5O7/c1-52-36-22-33(31(41)21-26(36)23-42-24-35(48)2 9-11-13-34 (47)39-30 (29)12-14-37(49)45-39)43-38(50)17-20-46-18-15-27(1) 6-19-46)53-40 (51)44-32-10-6-5-9-28 (32)25-7-3-2-4-8-25/h2-14,21-22, 27, 35,42,47-48H,15-20,23-24H2,1H3,(H,43,50)(H,44,51)(H,45,49)/t35-/m0/s1

Bọtini InChi:

URWYQGVSPQJGGB-DHUJRADRSA-N

Koko-ọrọ:

Batefeenterol, TD-5959, GSK961081, 743461-65-6, GSK-961081, GSK 961081, TD5959, TD 5959, 743461-65-6

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu)

Apejuwe:

Batefenterol jẹ antagonist muscarinic ati β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4, 1.3, ati 3.7 nM, fun hM2, hM3, ati hβ2-AR, ni atele ni imọran abuda radioligand). Batefenterol ṣe afihan iṣẹ agonist hβ2-AR ti o lagbara (EC50 = 0.29 nM) pẹlu aṣayan iṣẹ-ṣiṣe 440- ati 320-fold lori hβ1- ati hβ3-ARs, lẹsẹsẹ. àsopọ ati idilọwọ idahun bronchoconstrictor ninu ẹlẹdẹ Guinea kan Ayẹwo bronchoprotection (ED50 = 6.4 µg/ml). Awọn agbekalẹ ti o ni awọn batefenterol wa ninu awọn idanwo ile-iwosan lati ṣe itọju arun ti ẹdọforo onibaje (COPD).

Àfojúsùn: β2-adrenoceptor