Central cardiovascular effects of alpha adrenergic drugs: differences between catecholamines and imidazolines.
Central cardiovascular effects of alpha adrenergic drugs: differences between catecholamines and imidazolines.
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发表时间：
1984-07
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通讯作者：
P. Bousquet;J. Feldman;J. Schwartz
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作者：
P. Bousquet;J. Feldman;J. Schwartz
为了验证α-肾上腺素能激动剂的中枢降压作用是否与α-2受体的刺激有关，这些药物被直接注射到可乐定降压作用的重要部位网状外侧核。这些实验是在用戊巴比妥钠麻醉的正常血压猫身上通过微量注射(每侧0.5微升)进行的。α-甲基去甲肾上腺素是一种选择性的α-2激动剂(0.1-10微克/公斤)，在该区域没有降压作用，而强有力的α-1激动剂，如Crazoline(0.01-1微克/公斤)和ST 587(1-10微克/公斤)，如可乐定，产生剂量依赖性的降压作用。我们的结果表明，α-2选择性儿茶酚胺在网状外侧核区域并不活跃，而咪唑类化合物则产生降压作用，无论它们与某一亚型的α肾上腺素受体有何亲和力。因此，可能存在某种形式的结构-活性关系，这将表明在延髓的这个特定区域中，存在偏爱咪唑啉结构的位置。
To check whether the central hypotensive effect of alpha adrenergic agonists is linked with the stimulation of alpha-2 receptors, such drugs were administered directly to the nucleus reticularis lateralis, which is an important site for the hypotensive action of clonidine. These experiments were carried out by microinjections (0.5 microliter on each side) in normotensive cats anesthetized with pentobarbital. alpha-Methylnorepinephrine, a selective alpha-2 agonist (0.1-10 micrograms/kg) had no hypotensive effect in this region, whereas potent alpha-1 agonists such as cirazoline (0.01-1 micrograms/kg) and ST 587 (1-10 micrograms/kg), like clonidine, produced dose-dependent hypotensive effects. Our results suggest that alpha-2 selective catecholamines are not active in the nucleus reticularis lateralis region, whereas imidazolines induce a hypotensive effect whatever their affinity for one subtype of alpha adrenoceptors. Therefore, there may be some form of structure-activity relationship which would indicate the existence, in this particular region of the medulla oblongata, of sites preferring the imidazoline structure.