Adell A, Myers R D
Department of Pharmacology, School of Medicine, East Carolina University, Greenville, NC 27858, USA.
Pharmacol Toxicol. 1995 Nov;77(5):341-5. doi: 10.1111/j.1600-0773.1995.tb01038.x.
The 5-HT2A antagonist, amperozide, is considered to be a potentially useful drug for the treatment of substance abuse. The effects of this drug on the Sprague-Dawley rat were examined on the synthesis of dopamine and serotonin (5-HT) as well as on the intakes of food and water and the level of body weight. Amperozide was delivered subcutaneously by osmotic minipump in doses of 2.5 mg/kg or 5.0 mg/kg per day for 7 days. After injection of 100 mg/kg NSD-1015, each brain was dissected post mortem into midbrain, pons, hypothalamus, septum, nucleus accumbens, striatum, frontal cortex and the hippocampus. Neither concentration of amperozide altered the synthesis of dopamine or 5-HT, as measured in terms of the formation of 1-3,4-dihydroxyphenylalanine (L-DOPA) and 5-hydroxytryptophan (5-HTP), respectively, in any of the 8 brain regions analyzed. Both doses of amperozide reduced food intake by 20% within 24 hr after implantation of the pumps, but feeding resumed postoperatively at the control level within 48 hr. Amperozide affected neither the intake of water nor the level of body weight. The lack of effect on the synthesis of dopamine and 5-HT and the absence of side effects on the intakes of food and water suggest that amperozide may be a specific agent for suppressing alcohol drinking.
5-羟色胺2A受体拮抗剂氨哌齐特被认为是一种治疗药物滥用的潜在有效药物。研究了该药物对斯普拉格-道利大鼠多巴胺和5-羟色胺（5-HT）合成、食物和水摄入量以及体重水平的影响。通过渗透微型泵以每天2.5毫克/千克或5.0毫克/千克的剂量皮下注射氨哌齐特，持续7天。注射100毫克/千克NSD-1015后，每只大鼠处死后将大脑解剖为中脑、脑桥、下丘脑、隔区、伏隔核、纹状体、额叶皮质和海马体。在所分析的8个脑区中，两种浓度的氨哌齐特均未改变多巴胺或5-HT的合成，分别以1-3,4-二羟基苯丙氨酸（L-多巴）和5-羟色氨酸（5-HTP）的形成来衡量。两种剂量的氨哌齐特在植入微型泵后24小时内使食物摄入量减少了20%，但术后48小时内进食恢复到对照水平。氨哌齐特对水摄入量和体重水平均无影响。对多巴胺和5-HT合成缺乏影响以及对食物和水摄入量无副作用表明，氨哌齐特可能是一种抑制饮酒的特异性药物。
