ATYPICAL BETA-ADRENOCEPTOR (BETA-3-ADRENOCEPTOR) MEDIATED RELAXATION OF CANINE ISOLATED BRONCHIAL SMOOTH-MUSCLE

被引:22
作者
TAMOKI, J
YAMAUCHI, F
CHIYOTANI, A
YAMAWAKI, I
TAKEUCHI, S
KONNO, K
机构
关键词
BRL-37344; ADRENERGIC; BRONCHODILATOR; AIRWAY SMOOTH MUSCLE; ADENOSINE; 3'; 5'-CYCLIC MONOPHOSPHATE;
D O I
10.1152/jappl.1993.74.1.297
中图分类号
Q4 [生理学];
学科分类号
071003 ;
摘要
To determine whether atypical beta-adrenoceptors (beta3-adrenoceptors) exist in the airway smooth muscle, we studied isolated bronchial segments from dogs under isometric conditions in vitro. Addition of beta-adrenoceptor agonists produced a concentration-dependent relaxation of tissues precontracted with 10(-5) M acetylcholine, rank-order potency being isoproterenol (1) greater-than-or-equal-to salbutamol (0.95) greater-than-or-equal-to BRL 37344, a beta3-selective adrenoceptor agonist (0.83) > norepinephrine (0.10). Under the condition that alpha- and beta1-adrenoceptors had been blocked, the relaxant response to salbutamol was competitively antagonized by the beta2-adrenoceptor antagonist ICI 118551 and the pA2 was 7.01 +/- 0.25 (SE), whereas the response to BRL 37344 was resistant, with an apparent pA2 of 5.66. However, cyanopindolol, an antagonist for atypical beta-adrenoceptors, antagonized the BRL-induced relaxation in a competitive manner, with a pA2 of 6.74 +/- 0.11. This pA2 was lower than that when salbutamol was used as an agonist (P < 0.05). Intracellular adenosine 3',5'-cyclic monophosphate (cAMP) levels were increased by BRL 37344 in a concentration-dependent fashion. These results suggest that beta3-adrenoceptors may exist in canine bronchial smooth muscle and that the stimulation of this type of receptor causes a bronchodilation through a cAMP-dependent pathway.
引用
收藏
页码:297 / 302
页数:6
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