Onali P, Olianas M C
Department of Neurosciences, University of Cagliari, Italy.
J Neural Transm Gen Sect. 1992;88(2):95-104. doi: 10.1007/BF01244815.
In homogenates of female rat anterior pituitary, the azepine derivative B-HT 920 inhibited the forskolin-stimulated adenylate cyclase activity with an EC50 value of 0.35 microM. In male rat anterior pituitary, B-HT 920 curtailed the stimulation of adenylate cyclase activity by vasoactive intestinal peptide with an EC50 of 0.20 microM. In synaptic plasma membranes of rat striatum, B-HT 920 significantly reduced basal adenylate cyclase activity with an EC50 of 0.68 microM. Both in pituitary and striatum, the B-HT 920 inhibition was counteracted by the dopamine (DA) D2 receptor antagonist 1-sulpiride, but not by the alpha 2-adrenergic antagonist yohimbine. These results indicate that B-HT 920 is capable of activating DA D2 receptors negatively coupled to adenylate cyclase activity.
在雌性大鼠垂体前叶匀浆中，氮杂卓衍生物B-HT 920抑制福斯高林刺激的腺苷酸环化酶活性，其半数有效浓度（EC50）值为0.35微摩尔。在雄性大鼠垂体前叶中，B-HT 920抑制血管活性肠肽对腺苷酸环化酶活性的刺激作用，其EC50为0.20微摩尔。在大鼠纹状体的突触质膜中，B-HT 920显著降低基础腺苷酸环化酶活性，其EC50为0.68微摩尔。在垂体和纹状体中，多巴胺（DA）D2受体拮抗剂舒必利可抵消B-HT 920的抑制作用，但α2肾上腺素能拮抗剂育亨宾则不能。这些结果表明，B-HT 920能够激活与腺苷酸环化酶活性负偶联的DA D2受体。
