Dunwiddie T V, Worth T
J Pharmacol Exp Ther. 1982 Jan;220(1):70-6.
The behavioral and physiological effects of L-phenylisopropyladenosine, cyclohexyladenosine and 2-chloroadenosine were examined in mice and rats. These analogs of adenosine are agonists which bind with high affinity to putative central A1 receptors in vitro. Relatively low doses of these drugs administered i.p. produced marked sedation and hypothermia; higher doses resulted in an almost complete cessation of spontaneous motor activity as well as some ataxia. These analogs also antagonized seizures elicited by a variety of convulsants with different mechanisms of action. The differences observed in the anticonvulsant potencies of the analogs suggest that these effects are not produced by the interaction of these drugs with a single class of adenosine receptor. In particular, 2-chloroadenosine and cyclohexyladenosine appear to be more related to each other pharmacologically than to L-phenylisopropyladenosine. Because some of the anticonvulsant actions of L-phenylisopropyladenosine are not reversed by the adenosine antagonist theophylline, and are not shared by the other analogs, these may reflect actions mediated by other, perhaps nonpurinergic receptors. Although benzodiazepines also have sedative, hypothermic and anticonvulsant properties, responses to benzodiazepines can be clearly dissociated from responses to the adenosine agonists.
在小鼠和大鼠中研究了L-苯异丙基腺苷、环己基腺苷和2-氯腺苷的行为和生理效应。这些腺苷类似物是激动剂，在体外与假定的中枢A1受体具有高亲和力结合。腹腔注射相对低剂量的这些药物会产生明显的镇静和体温过低；较高剂量会导致自发运动活动几乎完全停止以及一些共济失调。这些类似物还拮抗了由多种作用机制不同的惊厥剂引发的癫痫发作。在这些类似物的抗惊厥效力中观察到的差异表明，这些作用不是由这些药物与单一类别的腺苷受体相互作用产生的。特别是，2-氯腺苷和环己基腺苷在药理学上彼此之间的关系似乎比与L-苯异丙基腺苷更密切。由于L-苯异丙基腺苷的一些抗惊厥作用不会被腺苷拮抗剂茶碱逆转，且其他类似物也不具有这些作用，这些作用可能反映了由其他（可能是非嘌呤能）受体介导的作用。尽管苯二氮䓬类药物也具有镇静、体温过低和抗惊厥特性，但对苯二氮䓬类药物的反应可以与对腺苷激动剂的反应明显区分开来。
