Background:

AH 11110 hydrochloride is a selective antagonist of α1B-adrenoceptor [1].

α1B-adrenoceptor (α1B-AR) belongs to α1- adrenergic receptors, which include three subtypes α1A, α1B and α1D and play an important role in regulating cell growth and proliferation.

AH 11110 hydrochloride is a selective α1B-AR antagonist. AH11110A inhibited cloned α1B-AR with Ki value of 79.4 nM and exhibited 32- and 26-fold selectivity over α1A- and α1D-ARs, respectively [1]. In rat vas deferens and rat perfused kidney, AH11110A exhibited affinities for α1A-AR, α1B-AR and α1D-AR with pA2 values of 6.41, 5.40-6.54 and 5.47-5.48, respectively. Also, AH11110A displayed affinity for α2-adrenoceptor in rabbit vas deferens with pA2 value of 5.44. In ligand binding studies, AH11110A exhibited affinities for native and cloned α1B-AR with pKi of 7.10-7.73. AH11110A increased contraction of rat vas deferens [2]. In isolated spleen strips from guinea-pig, AH11110A competitively antagonized tissue contraction induced by noradrenaline in a concentration-dependent way [2].

参考文献:
[1].  Erami C, Zhang H, Ho JG, et al. Alpha(1)-adrenoceptor stimulation directly induces growth of vascular wall in vivo. Am J Physiol Heart Circ Physiol, 2002, 283(4): H1577-1587.
[2].  Eltze M, K?nig H, Ullrich B, et al. Failure of AH11110A to functionally discriminate between alpha(1)-adrenoceptor subtypes A, B and D or between alpha(1)- and alpha(2)-adrenoceptors. Eur J Pharmacol, 2001, 415(2-3): 265-276.