Purdy R E, Stupecky G L, Coulombe P R
Department of Pharmacology, University of California, Irvine.
J Pharmacol Exp Ther. 1988 Apr;245(1):67-71.
Isolated rings from the proximal and distal ends of the bovine epicardial anterior descending coronary artery and guinea pig tracheal rings were mounted in tissue baths for the measurement of isometric contraction and relaxation, and spontaneously beating rabbit atria were prepared for measurement of chronotropic response. All tissues were exposed to phenoxybenzamine to block tissue uptake of catecholamines and alpha adrenoceptors. The arterial and tracheal rings were contracted with 25 mM K+ in order to observe agonist-induced relaxation. Beta adrenergic agonist dose-response curves were obtained in all tissues in the presence and absence of the beta-2 selective antagonist, ICI 118,551. The orders of agonist potencies in the proximal and distal coronary arteries and the rabbit atria were the same: namely, isoproterenol (ISO) greater than norepinephrine (NE) much greater than procaterol. In contrast, that in the guinea pig trachea was procaterol greater than ISO greater than NE. Procaterol was a weak, partial agonist in the bovine coronary artery and rabbit atria and a potent, full agonist in the guinea pig trachea. The ICI 118,551 pA2 values in the proximal segment of the bovine coronary artery were the same against both NE and fenoterol, 7.38. In the distal segment, the values were 7.33 and 7.14, respectively. ICI 118,551 -log KB values in the rabbit atria, 6.81 and 6.83 for NE and ISO, respectively, were slightly below those in the coronary artery segments, whereas -log KB values in the guinea pig trachea were substantially higher, 8.19 and 8.81 for fenoterol and procaterol, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
将取自牛心外膜冠状动脉前降支近端和远端的血管环以及豚鼠气管环安装在组织浴槽中,用于测量等长收缩和舒张,并制备自发性搏动的兔心房用于测量变时反应。所有组织均用酚苄明处理,以阻断儿茶酚胺和α肾上腺素能受体的组织摄取。用25 mM K⁺使动脉和气管环收缩,以观察激动剂诱导的舒张。在存在和不存在β₂选择性拮抗剂ICI 118,551的情况下,在所有组织中获得β肾上腺素能激动剂剂量反应曲线。近端和远端冠状动脉以及兔心房中激动剂效力的顺序相同:即异丙肾上腺素(ISO)大于去甲肾上腺素(NE)远大于丙卡特罗。相比之下,豚鼠气管中的顺序是丙卡特罗大于ISO大于NE。丙卡特罗在牛冠状动脉和兔心房中是一种弱的部分激动剂,而在豚鼠气管中是一种强效的完全激动剂。在牛冠状动脉近端段,ICI 118,551对NE和非诺特罗的pA₂值相同,为7.38。在远端段,值分别为7.33和7.14。在兔心房中,ICI 118,551对NE和ISO的-log KB值分别为6.81和6.83,略低于冠状动脉段的值,而在豚鼠气管中,-log KB值则高得多,非诺特罗和丙卡特罗分别为8.19和8.81。(摘要截短于250字)