Meltzer L T, Wiley J N, Williams A E, Heffner T G
Department of Pharmacology, Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, MI 48105.
Psychopharmacology (Berl). 1988;95(3):329-32. doi: 10.1007/BF00181942.
The ability of B-HT 920, a selective dopamine (DA) D-2 agonist, to stimulate postsynaptic DA receptors in brain was evaluated by assessing its ability to induce stereotypy and to increase locomotor activity in rats. When administered alone, B-HT 920 (0.03-3.0 mg/kg) did not induce stereotypy and produced only inhibition of locomotor activity, suggesting a lack of postsynaptic DA agonist actions. However, a different pattern of effects emerged when B-HT 920 was administered in combination with the selective DA D-1 agonist SKF 38393 (10 mg/kg): stereotypies (sniffing, licking, and gnawing) were induced and there was an inverted U-shaped function for locomotor activity. These data are consistent with the hypothesis that B-HT 920 has postsynaptic DA D-2 receptor agonist effects in normal rats that are revealed when D-1 receptor stimulation is also increased.
通过评估B-HT 920(一种选择性多巴胺(DA)D-2激动剂)诱导大鼠刻板行为和增加运动活性的能力,来评价其刺激脑内突触后DA受体的能力。单独给药时,B-HT 920(0.03 - 3.0毫克/千克)不诱导刻板行为,仅产生运动活性抑制,提示缺乏突触后DA激动剂作用。然而,当B-HT 920与选择性DA D-1激动剂SKF 38393(10毫克/千克)联合给药时,出现了不同的效应模式:诱导了刻板行为(嗅、舔和啃咬),并且运动活性呈现倒U形函数关系。这些数据与以下假设一致,即B-HT 920在正常大鼠中具有突触后DA D-2受体激动剂作用,当D-1受体刺激也增加时该作用会显现出来。