Batefenterol

Jina la 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"

Msimbo wa 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

Msimbo wa 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

Ufunguo wa InChi:

URWYQGVSPQJGGB-DHUJRADRSA-N

Neno muhimu:

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

Umumunyifu:Mumunyifu katika DMSO

Hifadhi:0 - 4°C kwa muda mfupi (siku hadi wiki), au -20°C kwa muda mrefu (miezi)

Maelezo:

Batefenterol ni mpinzani wa muscarinic na β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4, 1.3, na 3.7 nM, kwa hM2, hM3, na hβ2-AR, mtawalia katika jaribio la kumfunga radioligand). Batefenterol huonyesha shughuli yenye nguvu ya agonisti ya hβ2-AR (EC50 = 0.29 nM) ikiwa na uteuzi wa utendaji mara 440- na 320 juu ya hβ1- na hβ3-ARs, mtawalia.1 Batefenterol huleta utulivu wa misuli laini (EC50 = 11 nM) kwenye guinea iliyotengwa. tishu na huzuia mwitikio wa bronchoconstrictor katika a kipimo cha kinga ya bronchoprotection ya nguruwe ya Guinea (ED50 = 6.4 µg/mL). Miundo iliyo na batefenterol iko katika majaribio ya kimatibabu ya kutibu ugonjwa sugu wa kuzuia mapafu (COPD).

Lengo: β2-adrenoceptor