Testa R, Destefani C, Guarneri L, Poggesi E, Simonazzi I, Taddei C, Leonardi A
Research & Development Department, RECORDATI S.p.A., Milano, Italy.
Life Sci. 1995;57(13):PL159-63. doi: 10.1016/0024-3205(95)02079-x.
The pA2 value of several alpha 1-adrenoceptor antagonists on noradrenaline-induced contractions of rat aorta, and their affinity for the cloned alpha 1a-, alpha 1b- and alpha 1d-adrenoceptor subtypes were evaluated. Selective or moderately selective alpha 1d-, partially selective alpha 1b-, selective alpha 1a- and non subtype-selective alpha 1-adrenoceptors antagonists were included in the study. The potency of these compounds on rat aorta was well correlated with the affinity observed for the alpha 1d-adrenoceptor subtype. A poor correlation was found for the alpha 1b- and alpha 1a-subtypes. These results suggest that the alpha 1d-subtype plays a determining role in rat aorta contractions induced by noradrenaline.
评估了几种α1-肾上腺素能拮抗剂对去甲肾上腺素诱导的大鼠主动脉收缩的pA2值,以及它们对克隆的α1a-、α1b-和α1d-肾上腺素能受体亚型的亲和力。研究中包括了选择性或中度选择性的α1d-、部分选择性的α1b-、选择性α1a-和非亚型选择性的α1-肾上腺素能受体拮抗剂。这些化合物对大鼠主动脉的效力与对α1d-肾上腺素能受体亚型观察到的亲和力密切相关。而对于α1b-和α1a-亚型,相关性较差。这些结果表明,α1d-亚型在去甲肾上腺素诱导的大鼠主动脉收缩中起决定性作用。