Martinotti E, Breschi M C, Omini C, Pani M, Ciucci M A, Nieri P
Istituto Policattedra di Discipline Biologiche, Università degli Studi di Pisa, Italy.
Pharmacol Res. 1991 Jan;23(1):57-69. doi: 10.1016/s1043-6618(05)80107-0.
The alpha-adrenoceptor populations in aortic strips from humans, rats, guinea-pigs and rabbits were investigated in vitro, using specific agonists and antagonists. In rabbit and human preparations the activities of the two agonists tested, noradrenaline and methoxamine, were competitively antagonized by prazosin, whereas in the other animal species prazosin showed a competitive antagonism for methoxamine induced contraction, but an uncompetitive behaviour against noradrenaline. The alpha 2-selective agonists B-HT 920 and detomidine did not elicit any effect on aortic strips up to 10(-3) M. On the basis of these results, alpha 1-receptors seem to represent an homogeneous population in human and rabbit aortae, but not in rat and guinea-pig tissues. On the other hand, the contractile response of noradrenaline and methoxamine on aortic strips from the four animal species examined cannot be ascribed to the activation of postsynaptic alpha 2-receptors. Moreover we present preliminary evidence that rat and guinea-pig aortae do not contain a clear subdivision in alpha 1a- and alpha 1b-receptors.
利用特异性激动剂和拮抗剂,在体外研究了来自人类、大鼠、豚鼠和兔子的主动脉条中的α-肾上腺素能受体群体。在兔子和人类标本中,所测试的两种激动剂去甲肾上腺素和甲氧明的活性被哌唑嗪竞争性拮抗,而在其他动物物种中,哌唑嗪对甲氧明诱导的收缩表现出竞争性拮抗作用,但对去甲肾上腺素表现出非竞争性行为。α2选择性激动剂B-HT 920和地托咪定在浓度高达10(-3) M时对主动脉条均未产生任何影响。基于这些结果,α1受体在人类和兔子主动脉中似乎代表一个同质群体,但在大鼠和豚鼠组织中并非如此。另一方面,去甲肾上腺素和甲氧明对所检查的四种动物物种的主动脉条的收缩反应不能归因于突触后α2受体的激活。此外,我们提供的初步证据表明,大鼠和豚鼠主动脉中不存在α1a和α1b受体的明显细分。