Urapidil-d3

Urapidil-d3 is intended for use as an internal standard for the quantification of urapidil (Cay29004) by GC- or LC-MS. Urapidil is an antagonist of alpha1-adrenergic receptors (alpha1-ARs) and a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. It selectively binds to alpha1- over alpha2-ARs (IC50s = 0.74 and 42 µM, respectively) and to 5-HT1A over 5-HT1B and 5-HT2 receptors (IC50s = 0.4, 20.4, and >10 µM, respectively) in rat cortex. Urapidil inhibits cAMP accumulation induced by forskolin in calf hippocampus as a functional model for 5-HT1A receptors (EC50 = 390 nM). It is also a beta1-AR antagonist that inhibits the positive chronotropic response induced by isoproterenol (Cay15592) in isolated rat atria (pA2 = 6.05). Urapidil (1 µmol/kg, i.v.) lowers mean arterial pressure (MAP) in anesthetized cats, an effect that is reduced by central administration of the 5-HT1A receptor antagonist spiroxatrine. SMILES CN(C(NCCCN(CC1)CCN1C2=CC=CC=C2OC([2H])([2H])[2H])=CC(N3C)=O)C3=O InChi Code InChI=1S/C20H29N5O3/c1-22-18(15-19(26)23(2)20(22)27)21-9-6-10-24-11-13-25(14-12-24)16-7-4-5-8-17(16)28-3/h4-5,7-8,15,21H,6,9-14H2,1-3H3/i3D3 InChi Key ICMGLRUYEQNHPF-HPRDVNIFSA-N