Dabuzalgron (hydrochloride)

Dabuzalgron is a partial agonist of the alpha1A-adrenergic receptor (alpha1A-AR). It selectively binds to alpha1A-ARs over alpha1B- and alpha1D-ARs in CHO-K1 cells expressing the recombinant human receptors (Kis = 0.041, 1.6, and 6.5 µM, respectively) and selectively induces inositol phosphate accumulation in alpha1A-AR-expressing CHO-K1 cells over those expressing alpha1B- or alpha1D-ARs (EC50s = 0.204, >100, and >100 µM, respectively). Dabuzalgron induces urethral tension in rabbit bladder neck preparations (EC50 = 0.363 µM). Intravenous administration of dabuzalgron increases intraurethral pressure and diastolic arterial pressure in anesthetized micropigs (ED50s = 41 and 36 µg/kg, respectively). Dabuzalgron (300 µg/kg) increases urethral tension but does not affect diastolic arterial pressure or heart rate in conscious micropigs. Oral administration of dabuzalgron (10 µg/kg) decreases cardiac fibrosis and prevents decreases in heart rate and fractional shortening induced by doxorubicin (Cay15007) in a mouse model of cardiotoxicity.. SMILES: O=S(NC1=C(C)C(OCC2=NCCN2)=CC=C1Cl)(C)=O.Cl. InChi Code: InChI=1S/C12H16ClN3O3S.ClH/c1-8-10(19-7-11-14-5-6-15-11)4-3-9(13)12(8)16-20(2,17)18,/h3-4,16H,5-7H2,1-2H3,(H,14,15),1H. InChi Key: QFRMKDCRDUXTBR-UHFFFAOYSA-N