Lafon-Cazal M, Bockaert J
Eur J Pharmacol. 1985 Dec 10;119(1-2):53-9. doi: 10.1016/0014-2999(85)90321-8.
Octopamine stimulates (20-30-fold) the adenylate cyclase activity in a broken cell preparation of locust flight muscle. This stimulation is mediated by one receptor with an apparent affinity of 3.3 X 10(-6) M. The hydroxyl group in the para position on phenylethanolamine was absolutely necessary to obtain an agonist whereas the meta hydroxyl group or the presence of a catechol almost suppressed the activity. Similar pharmacological profiles were obtained on other locust muscles, i.e. mandibular and extensor tibiae muscles. The affinities of a large series of agonists and antagonists for the octopamine receptor coupled with an adenylate cyclase were compared to those reported for octopamine 1, 2A and 2B receptors based on physiological studies in the locust extensor tibiae muscle. It appears that the octopamine receptor coupled with adenylate cyclase is likely to be identical with the octopamine 2A receptor mediating the increase in the amplitude of slow motoneuron twitch tension. The results of the pharmacological experiments are discussed, in particular concerning the possible relationship between the octopamine receptor and alpha 1- and alpha 2-adrenoceptors.
章鱼胺可刺激(20 - 30倍)蝗虫飞行肌破碎细胞制剂中的腺苷酸环化酶活性。这种刺激由一种受体介导,其表观亲和力为3.3×10⁻⁶ M。苯乙醇胺对位的羟基对于获得激动剂是绝对必要的,而间位羟基或儿茶酚的存在几乎会抑制活性。在其他蝗虫肌肉,如下颌肌和胫节伸肌上也获得了类似的药理学特征。将一系列激动剂和拮抗剂对与腺苷酸环化酶偶联的章鱼胺受体的亲和力,与基于蝗虫胫节伸肌生理学研究报道的章鱼胺1、2A和2B受体的亲和力进行了比较。似乎与腺苷酸环化酶偶联的章鱼胺受体可能与介导慢运动神经元抽搐张力幅度增加的章鱼胺2A受体相同。讨论了药理学实验的结果,特别是关于章鱼胺受体与α1和α2肾上腺素能受体之间可能的关系。