Iusco G, Boido V, Sparatore F, Colombo G, Saba P L, Rossetti Z, Vaccari A
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Farmaco. 1997 Mar;52(3):141-6.
A set of substituted benzamides, characterized by the presence of a bulky quinolizidine moiety, were subjected to binding assays for 5-HT3 and D2 receptors on membranes obtained from the bovine area postrema ([3H]-GR65630) and the rat striatum ([3H]-spiperone) respectively. These benzamides resulted unsuitable for the recognition of D2 receptors, while a few of them, devoid of 5-HT4 receptor activity, had consistent affinity for central 5-HT3 receptors, inhibiting also potently the ethanol-induced dopamine efflux from the mesolimbic dopamine terminal region. However they failed in attenuating voluntary alcohol consumption in rats, as observed with several other chemically unrelated 5-HT3 antagonists. Thus the 5-HT3-mediated inhibition of alcohol-induced striatal release of dopamine by substituted benzamides is not a requisite for affecting ethanol intake.
一组以存在庞大喹诺里西啶部分为特征的取代苯甲酰胺，分别针对从牛最后区获得的膜上的5-HT3和D2受体（[3H]-GR65630）以及大鼠纹状体上的D2受体（[3H]-司哌罗宁）进行结合试验。这些苯甲酰胺不适合用于识别D2受体，而其中一些没有5-HT4受体活性的苯甲酰胺对中枢5-HT3受体具有一致的亲和力，还能有效抑制乙醇诱导的中脑边缘多巴胺终末区域的多巴胺外流。然而，正如其他几种化学结构不相关的5-HT3拮抗剂所观察到的那样，它们未能减少大鼠的自愿酒精摄入量。因此，取代苯甲酰胺通过5-HT3介导对酒精诱导的纹状体多巴胺释放的抑制作用并非影响乙醇摄入量的必要条件。
