Nielsen H, Hasenkam J M, Pilegaard H K, Mortensen F V, Mulvany M J
Institute of Pharmacology, University of Aarhus, Denmark.
Am J Physiol. 1991 Sep;261(3 Pt 2):H762-7. doi: 10.1152/ajpheart.1991.261.3.H762.
Human resistance arteries (144-332 microns diam) from colon, pericardial fat, and skeletal muscle were mounted in a myograph for measurements of isometric contractions under conditions of partial depolarization by potassium chloride. In all preparations, both phenylephrine (alpha 1-selective agonist) and B-HT 933 (alpha 2-selective agonist) evoked concentration-dependent contractions that were antagonized by the alpha 1-selective antagonist prazosin (10(-8) M) and the alpha 2-selective antagonist yohimbine (10(-7) M), respectively. The affinities (expressed as pKB values) of prazosin for the receptor mediating the responses to phenylephrine were 8.88-9.41, whereas the affinities of yohimbine for the receptor mediating the responses to B-HT 933 were 7.71-7.97. Norepinephrine (mixed alpha 1-agonist/alpha 2-agonist) also elicited concentration-dependent responses that were modestly, but significantly, antagonized by prazosin alone and yohimbine alone at the above-mentioned concentrations. The two antagonists in combination, however, effectively antagonized the responses to this agonist. These findings strongly suggest the presence of functional, postjunctional alpha 1- and alpha 2-adrenoceptors in isolated human resistance arteries from colon, pericardial fat, and skeletal muscle and that responses to norepinephrine in these vessels are mediated by both alpha-adrenoceptor subtypes.
取自结肠、心包脂肪和骨骼肌的人体阻力动脉(直径144 - 332微米)被安装在肌动描记器中,用于在氯化钾引起部分去极化的条件下测量等长收缩。在所有标本中,去氧肾上腺素(α1选择性激动剂)和B-HT 933(α2选择性激动剂)均引起浓度依赖性收缩,分别被α1选择性拮抗剂哌唑嗪(10⁻⁸ M)和α2选择性拮抗剂育亨宾(10⁻⁷ M)拮抗。哌唑嗪对介导去氧肾上腺素反应的受体的亲和力(以pKB值表示)为8.88 - 9.41,而育亨宾对介导B-HT 933反应的受体的亲和力为7.71 - 7.97。去甲肾上腺素(α1激动剂/α2激动剂混合)也引起浓度依赖性反应,在上述浓度下,单独使用哌唑嗪和单独使用育亨宾均可适度但显著地拮抗该反应。然而,这两种拮抗剂联合使用可有效拮抗对该激动剂的反应。这些发现有力地表明,在取自结肠、心包脂肪和骨骼肌的离体人体阻力动脉中存在功能性的、节后α1和α2肾上腺素能受体,并且这些血管对去甲肾上腺素的反应是由两种α肾上腺素能受体亚型介导的。