Ruskoaho H, Karppanen H
Eur J Pharmacol. 1984 Apr 13;100(1):91-6. doi: 10.1016/0014-2999(84)90319-4.
The sedative effect of xylazine and its interaction with antagonists of alpha-adrenoceptors or opiate receptors was examined in chicks. The duration of the sleep-like behavioral state induced by xylazine was determined by measuring the time interval during which the chicks failed to exhibit the righting reflex. In these chicks, intramuscular administration of xylazine (0.3-4.8 mg/kg) induced a loss of the righting reflex, the duration of which was dose-dependent. Both alpha-adrenoceptor antagonists of the alpha2 type, i.e. yohimbine (0.1-1.0 mg/kg) and compound 170150 (0.1-1.0 mg/kg) (a benzodioxane derivative), and opiate receptor antagonists, i.e. naloxone (0.4-1.6 mg/kg) and nalorphine (3.0-30.0 mg/kg), effectively inhibited the sedative effect of xylazine while prazosin (0.1-10.0 mg/kg), an alpha 1-adrenoceptor antagonist, failed to antagonize xylazine-induced sedation. These findings suggest that in addition to the stimulation of central alpha 2-adrenoceptors, activation of an endogenous opiate mechanism may be involved in the sedative effect of xylazine.
研究了赛拉嗪对雏鸡的镇静作用及其与α-肾上腺素能受体或阿片受体拮抗剂的相互作用。通过测量雏鸡未能表现出翻正反射的时间间隔来确定赛拉嗪诱导的睡眠样行为状态的持续时间。在这些雏鸡中,肌肉注射赛拉嗪(0.3 - 4.8毫克/千克)会导致翻正反射丧失,其持续时间呈剂量依赖性。两种α2型α-肾上腺素能受体拮抗剂,即育亨宾(0.1 - 1.0毫克/千克)和化合物170150(0.1 - 1.0毫克/千克)(一种苯并二恶烷衍生物),以及阿片受体拮抗剂,即纳洛酮(0.4 - 1.6毫克/千克)和烯丙吗啡(3.0 - 30.0毫克/千克),均能有效抑制赛拉嗪的镇静作用,而α1-肾上腺素能受体拮抗剂哌唑嗪(0.1 - 10.0毫克/千克)未能拮抗赛拉嗪诱导的镇静作用。这些发现表明,除了刺激中枢α2-肾上腺素能受体外,内源性阿片机制的激活可能也参与了赛拉嗪的镇静作用。