Ramagopal M V, Chitwood R W, Mustafa S J
Department of Pharmacology, School of Medicine, East Carolina University, Greenville, NC 27858-4354.
Eur J Pharmacol. 1988 Jul 14;151(3):483-6. doi: 10.1016/0014-2999(88)90548-1.
The present study was an attempt to characterize the type of adenosine receptor in human coronary arteries obtained from organ donors with the use of adenosine analogs. Prostaglandin F2 alpha (10(-6) M) produced tonic contractions followed by phasic contractions and diltiazem (10(-6) M) pretreatment changed the phasic contractions to tonic contractions. Adenosine and its analogs (5'-N-ethyl-carboxamide adenosine, NECA and N6-L-phenyl-isopropyl adenosine, L-PIA), produced concentration-dependent relaxations of the tonic contractions and the order of potency was found to be: NECA greater than L-PIA greater than adenosine. 8-Phenyltheophylline (5 X 10(-6) M) antagonized the relaxations produced by adenosine and its analogs. The data suggest the existence of A2 adenosine receptor in human coronary arteries.
本研究旨在利用腺苷类似物对取自器官捐献者的人冠状动脉中的腺苷受体类型进行表征。前列腺素F2α（10⁻⁶ M）引起强直性收缩，随后是阶段性收缩，地尔硫卓（10⁻⁶ M）预处理可将阶段性收缩转变为强直性收缩。腺苷及其类似物（5'-N-乙基-羧酰胺腺苷、NECA和N⁶-L-苯基-异丙基腺苷、L-PIA）可引起强直性收缩的浓度依赖性舒张，其效力顺序为：NECA＞L-PIA＞腺苷。8-苯基茶碱（5×10⁻⁶ M）可拮抗腺苷及其类似物产生的舒张作用。数据表明人冠状动脉中存在A2腺苷受体。
