relative index of in vivo dopaminergic activity. The maximal locomotor response was significantly greater for 5a than for 5b, 1a, or 1b. These findings suggest that metabolite 5a may play a role in the pharmacology of 1a. The intracerebroventricular administration of acids 2a, 2b, 6a, and 6b all produced a small increase in locomotor activity relative to their methyl esters which was not appreciably affected
合成了苏-dl-对羟基甲基
哌啶酸酯和赤-dl-对羟基甲基
哌啶酸酯(5a和5b)以及脱酯产物苏-dl-和赤-dl-对羟基羟脯
氨酸(6a和6b)。确定了这些化合物的脑室内给药对大鼠运动活性的影响,并将其与
哌醋甲酯(1a和1b)和
利他林酸(2a和2b)的各自外消旋物的影响进行比较,以作为体内
多巴胺能活性的相对指标。5a的最大运动响应显着大于5b,1a或1b。这些发现表明,代谢产物5a可能在1a的药理学中起作用。脑室内施用酸2a,2b,6a,