Batefenterol

Ingoa matū:

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

Waehere 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

Waehere InChi:

InChI=1S/C40H42ClN5O7/c1-52-36-22-33(31(41)21-26(36)23-42-24-35(48)29-11-13-34(47)39-30( 29)12-14-37(49)45-39)43-38(50)17-20-46-18-15-27(16-19-46)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

Kī InChi:

URWYQGVSPQJGGB-DHUJRADRSA-N

Kupumatua:

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

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:

Ko te Batefenterol he antagonist muscarinic me te β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4, 1.3, me te 3.7 nM, mo te hM2, te hM3, me te hβ2-AR, i roto i te whakamatautau here radioligand). Kei te whakaatu a Batefenterol i nga mahi agonist hβ2-AR kaha (EC50 = 0.29 nM) me te 440- me te 320-fold te whiriwhiringa mahi mo te hβ1- me te hβ3-ARs. kiko me te aukati i te urupare bronchoconstrictor i roto i te whakamatautau bronchoprotection poaka (ED50 = 6.4 µg/mL). Kei roto i nga whakamatautau haumanu nga rongoa kei roto ko te batefenterol hei rongoa i te mate pukahukahu aukati mau tonu (COPD).

Whainga: β2-adrenoceptor