Martellotta M C, Kuzmin A, Muglia P, Gessa G L, Fratta W
B.B. Brodie Department of Neuroscience, University of Cagliari, Italy.
Psychopharmacology (Berl). 1994 Jan;113(3-4):378-80. doi: 10.1007/BF02245212.
The effect of isradipine, a dihydropyridine calcium antagonist, on cocaine intravenous self-administration in rats was investigated. Administration of (+/-)isradipine (1.25-5 mg/kg SC) 2 h before the cocaine self-administration session induced a significant and dose-dependent increase in the number of cocaine injections with respect to basal values. This effect was stereospecific, with the (+) form of isradipine being active, while the (-) stereoisomer was ineffective. These results suggest that isradipine antagonizes the rewarding properties of cocaine, possibly by inhibiting those dopaminergic systems related to reward mechanisms. These results further indicate a possible use of isradipine, or structurally similar compounds, in the treatment of cocaine related disorders.
研究了二氢吡啶类钙拮抗剂伊拉地平对大鼠静脉注射可卡因自我给药行为的影响。在可卡因自我给药实验前2小时皮下注射(±)伊拉地平(1.25 - 5毫克/千克),与基础值相比,可卡因注射次数显著增加且呈剂量依赖性。这种作用具有立体特异性,伊拉地平的(+)型有活性,而(-)型立体异构体无效。这些结果表明,伊拉地平可能通过抑制与奖赏机制相关的多巴胺能系统来拮抗可卡因的奖赏特性。这些结果进一步表明伊拉地平或结构相似的化合物可能用于治疗与可卡因相关的疾病。