Michel M C, Büscher R, Philipp T, Brodde O E
Department of Medicine, University of Essen, Federal Republic of Germany.
Naunyn Schmiedebergs Arch Pharmacol. 1993 Feb;347(2):180-5. doi: 10.1007/BF00169264.
We have studied the role of alpha 1A- and alpha 1B-adrenoceptors in noradrenaline- and methoxamine-stimulated inositol phosphate accumulation in rat renal cortical slices. [3H]Prazosin binding studies with and without inactivation of alpha 1B-adrenoceptors by chloroethylclonidine treatment suggested that noradrenaline lacks relevant selectivity for alpha 1-adrenoceptor subtypes. Both agonists stimulated [3H]inositol phosphate accumulation with similar maximal effects. The alpha 1A-selective antagonists 5-methyl-urapidil and (+)-niguldipine inhibited inositol phosphate formation by both agonists with shallow biphasic curves but the high affinity component was only 15%-31% and 38%-41%, respectively. The irreversible alpha 1B-selective antagonist chloroethylclonidine inhibited inositol phosphate generation by both agonists by 54%-57%. In contrast to our previous data in rat cerebral cortical slices, we conclude that in rat renal cortex both alpha 1A- and alpha 1B-adrenoceptors are involved in noradrenaline- and methoxamine-stimulated inositol phosphate generation.
我们研究了α1A-和α1B-肾上腺素能受体在去甲肾上腺素和甲氧明刺激大鼠肾皮质切片中肌醇磷酸积累过程中的作用。通过氯乙可乐定处理使α1B-肾上腺素能受体失活与未失活的情况下进行的[3H]哌唑嗪结合研究表明,去甲肾上腺素对α1-肾上腺素能受体亚型缺乏相关选择性。两种激动剂刺激[3H]肌醇磷酸积累的最大效应相似。α1A选择性拮抗剂5-甲基-乌拉地尔和(+)-尼莫地平对两种激动剂诱导的肌醇磷酸形成均有抑制作用,呈浅双相曲线,但高亲和力成分分别仅为15%-31%和38%-41%。不可逆的α1B选择性拮抗剂氯乙可乐定对两种激动剂诱导的肌醇磷酸生成的抑制率为54%-57%。与我们之前在大鼠大脑皮质切片中的数据相反,我们得出结论,在大鼠肾皮质中,α1A-和α1B-肾上腺素能受体均参与去甲肾上腺素和甲氧明刺激的肌醇磷酸生成。