Hartley M L, Pennefather J N
Br J Pharmacol. 1985 Feb;84(2):463-8. doi: 10.1111/j.1476-5381.1985.tb12930.x.
The effects of two selective beta-adrenoceptor antagonists on the inhibitory responses to some sympathomimetic amines of electrically-stimulated preparations of costo-uterine muscle, taken from virgin rats, have been examined quantitatively. pA2 values for the antagonist, atenolol (beta 1-selective) and ICI 118,551 (beta 2-selective) were obtained using as agonists, fenoterol (beta 2-selective agonist) and noradrenaline (alpha- and beta-adrenoceptor agonist, beta 1-selective); and in addition, with ICI 118,551 only, isoprenaline (beta-agonist, non-selective) and adrenaline (alpha- and beta-adrenoceptor agonist, beta 2-selective). Catecholamine uptake mechanisms and alpha-adrenoceptors were not blocked in any of these experiments. Atenolol competitively antagonized the effects of fenoterol and noradrenaline to a similar extent, the pA2 values being 5.4 and 5.7, respectively. ICI 118,551 competitively antagonized the effects of fenoterol, isoprenaline, adrenaline and noradrenaline to a similar extent; pA2 values ranged from 8.7 with noradrenaline to 9.1 with isoprenaline. These results extend our previous observations which indicated that the adrenoceptors mediating inhibition of electrically-evoked contractions of costo-uterine muscle of the virgin rat are homogeneous and of the beta 2-subtype. The potency of the beta 1-selective agonist RO 363 in producing inhibition of electrically-evoked contractions of this tissue was also examined. RO 363 was 200 times less potent than isoprenaline but was a full agonist. This indicates that there is efficient coupling between beta 2-adrenoceptor activation and tissue response in this non-innervated preparation.
对取自未交配大鼠的肋子宫肌电刺激标本对某些拟交感胺的抑制反应,研究了两种选择性β-肾上腺素能拮抗剂的作用,并进行了定量分析。使用非诺特罗(β2选择性激动剂)和去甲肾上腺素(α和β肾上腺素能激动剂,β1选择性)作为激动剂,获得了拮抗剂阿替洛尔(β1选择性)和ICI 118,551(β2选择性)的pA2值;此外,仅使用ICI 118,551时,还使用了异丙肾上腺素(β激动剂,非选择性)和肾上腺素(α和β肾上腺素能激动剂,β2选择性)。在任何这些实验中,儿茶酚胺摄取机制和α肾上腺素能受体均未被阻断。阿替洛尔对非诺特罗和去甲肾上腺素的作用具有相似程度的竞争性拮抗作用,pA2值分别为5.4和5.7。ICI 118,551对非诺特罗、异丙肾上腺素、肾上腺素和去甲肾上腺素的作用具有相似程度的竞争性拮抗作用;pA2值范围从去甲肾上腺素的8.7到异丙肾上腺素的9.1。这些结果扩展了我们之前的观察结果,即介导未交配大鼠肋子宫肌电诱发收缩抑制的肾上腺素能受体是同质的,且属于β2亚型。还研究了β1选择性激动剂RO 363对该组织电诱发收缩的抑制作用。RO 363的效力比异丙肾上腺素低200倍,但却是一种完全激动剂。这表明在这种无神经支配的标本中,β2肾上腺素能受体激活与组织反应之间存在有效偶联。