Mustafa S M, Yousif M, Cherian A, Oriowo M A
Department of Pharmacology and Toxicology, Faculty of Medicine, Safat, Kuwait.
J Auton Pharmacol. 1999 Aug;19(4):193-9. doi: 10.1046/j.1365-2680.1999.00134.x.
Isoprenaline (non-selective) and noradrenaline (beta1-selective) concentration-dependently relaxed ovine tracheal strips precontracted with carbachol. The pD2 values were 7.07 +/- 0.08 and 6.13 +/- 0.10 for isoprenaline and noradrenaline, respectively. In the same preparation, salbutamol either produced weak relaxation or in some cases, contractile responses indicating the presence of very little or no beta2-adrenoceptors in this preparation. Isoprenaline-and noradrenaline-induced relaxations were antagonized by propranolol and atenolol with pA2 values in the range reported in the literature for an action on beta1-adrenoceptors. ICI 118551 also antagonized isoprenaline- and noradrenaline-induced relaxation but at concentrations much higher than are required to block beta2-adrenoceptors, confirming that beta2-adrenoceptors do not contribute significantly to these responses. The selective beta3-adrenoceptor agonist, BRL 37344A produced concentration-dependent relaxation of tracheal strips. BRL 37344A was a full agonist producing 100% relaxation of carbachol-induced tone. BRL 37344A-induced relaxation was weakly antagonized by propranolol confirming an action, mainly, on beta3-adrenoceptors. Cyanopindolol antagonized isoprenaline-induced relaxation (in the presence of propranolol, 10(-7) M) with a pA2 value of 8.06 +/- 0.24. It was therefore concluded that beta1- and beta3-adrenoceptors mediated agonist-induced relaxation in sheep tracheal strips.
异丙肾上腺素(非选择性)和去甲肾上腺素(β1选择性)能浓度依赖性地舒张由卡巴胆碱预收缩的羊气管条。异丙肾上腺素和去甲肾上腺素的pD2值分别为7.07±0.08和6.13±0.10。在同一标本中,沙丁胺醇要么产生微弱的舒张作用,要么在某些情况下产生收缩反应,表明该标本中几乎不存在或不存在β2肾上腺素能受体。异丙肾上腺素和去甲肾上腺素诱导的舒张作用被普萘洛尔和阿替洛尔拮抗,其pA2值在文献报道的作用于β1肾上腺素能受体的范围内。ICI 118551也拮抗异丙肾上腺素和去甲肾上腺素诱导的舒张作用,但所需浓度远高于阻断β2肾上腺素能受体所需的浓度,这证实β2肾上腺素能受体对这些反应的贡献不大。选择性β3肾上腺素能受体激动剂BRL 37344A能浓度依赖性地舒张气管条。BRL 37344A是一种完全激动剂,能使卡巴胆碱诱导的张力产生100%的舒张。普萘洛尔对BRL 37344A诱导的舒张作用有微弱的拮抗作用,这证实其主要作用于β3肾上腺素能受体。氰吲哚洛尔拮抗异丙肾上腺素诱导的舒张作用(在存在10⁻⁷M普萘洛尔的情况下),pA2值为8.06±0.24。因此得出结论,β1和β3肾上腺素能受体介导了激动剂诱导的羊气管条舒张。