Muramatsu I, Taniguchi T, Okada K
Department of Pharmacology, School of Medicine, Fukui Medical University, Matsuoka, Japan.
Jpn J Pharmacol. 1998 Nov;78(3):331-5. doi: 10.1254/jjp.78.331.
Selectivity of tamsulosin and terazosin to functional alpha1-adrenoceptors was examined. Both drugs competitively inhibited the contractile responses to noradrenaline in different tissues where the responses were mediated through the alpha1D-, alpha1B- or alpha1L-subtype. Together with the affinities obtained in the binding study with cloned (alpha1a, alpha1b, alpha1d) and native (alpha1A and alpha1B) subtypes, the selectivity of tamsulosin was alpha1A>alpha1L, alpha1D>alpha1B. Terazosin had lower affinity at various subtypes than tamsulosin, but showed relatively high selectivity to the alpha1D-subtype. In the human prostate, tamsulosin was more than 30-fold higher in affinity than terazosin in functional and binding studies.
研究了坦索罗辛和特拉唑嗪对功能性α1肾上腺素能受体的选择性。两种药物在不同组织中竞争性抑制去甲肾上腺素的收缩反应，这些反应是通过α1D、α1B或α1L亚型介导的。结合克隆（α1a、α1b、α1d）和天然（α1A和α1B）亚型的结合研究中获得的亲和力，坦索罗辛的选择性为α1A>α1L，α1D>α1B。特拉唑嗪在各种亚型上的亲和力低于坦索罗辛，但对α1D亚型表现出相对较高的选择性。在人类前列腺中，在功能和结合研究中，坦索罗辛的亲和力比特拉唑嗪高30倍以上。
