Zhang X X, Jin G Z, Wei Y F
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
Zhongguo Yao Li Xue Bao. 1995 Sep;16(5):423-7.
To study the potency of pergolide as a D2 receptor agonist on the firing activity of substantia nigra compacta (SNC) dopamine (DA) neurons compared with that of bromocriptine and to determine whether pergolide has the nature of D1 receptor agonist in vivo.
Extracellular single unit recording techniques.
Both pergolide and bromocriptine decreased the spontaneously firing rate of "sensitive" and "insensitive" DA cells. In regard of ID50 values, pergolide (11.9, 95% fiducial limits, 5.7-25.1 micrograms kg-1) was more potent than bromocriptine (7.8, 95% fiducial limits, 3.3-18.5 mg kg-1). The discharge inhibition of pergolide was attenuated following the injection of selective D2 receptor antagonist spiperone 0.25 mg kg-1 or selective D1 receptor antagonist Sch-23390 1-2 mg kg-1. However, the inhibition caused by bromocriptine was not always attenuated by spiperone.
Pergolide is 650 times more potent than bromocriptine at D2 receptors, and possesses D1 receptor agonist characteristics in vivo.
研究培高利特作为D2受体激动剂对黑质致密部（SNC）多巴胺（DA）神经元放电活动的作用强度，并与溴隐亭相比较，同时确定培高利特在体内是否具有D1受体激动剂的性质。
采用细胞外单单位记录技术。
培高利特和溴隐亭均降低了“敏感”和“不敏感”DA细胞的自发放电频率。就半数抑制剂量（ID50）值而言，培高利特（11.9，95%置信限，5.7 - 25.1微克/千克）比溴隐亭（7.8，95%置信限，3.3 - .5毫克/千克）作用更强。注射0.25毫克/千克的选择性D2受体拮抗剂螺哌隆或1 - 2毫克/千克的选择性D1受体拮抗剂Sch - 23390后，培高利特的放电抑制作用减弱。然而，溴隐亭引起的抑制作用并不总是被螺哌隆减弱。
培高利特在D2受体上的效力比溴隐亭强650倍，且在体内具有D1受体激动剂特性。
