Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 (Dopamine Receptor) agonist. Naxagolide has the potential for the research of parkinson's disease (PD)[1][2].
在体外,Naxagolide ((+)-PHNO) 抑制大鼠纹状体膜上的 [3H]apomorphine (IC50 = 23 nM) 或 [3 H]spiperone (IC50 = 55 nM)[1]。
在小鼠中,Naxagolide ((+)-PHNO) 在单侧尾部切除的动物中产生体温过低 (13 μg/kg i.p.) 和姿势不对称 (4 μg/kg i.p.)[1]。
在大鼠中,Naxagolide ((+)-PHNO) 在 6-羟基多巴胺损伤的动物中产生刻板印象(10 μg/kg i.p.)和对侧转向(5 μg/kg i.p.),持续 1 至 3 小时[1] 。
[1]. G E Martin, et al. Pharmacologic profile of a novel potent direct-acting dopamine agonist, (+)-4-propyl-9-hydroxynaphthoxazine [(+)-PHNO]. J Pharmacol Exp Ther. 1984 Sep;230(3):569-76.
[2]. E F Domino, et al. Relative potency and efficacy of some dopamine agonists with varying selectivities for D1 and D2 receptors in MPTP-induced hemiparkinsonian monkeys. J Pharmacol Exp Ther. 1993 Jun;265(3):1387-91.
















