Marwaha J, Palmer M, Hoffer B, Freedman R, Rice K C, Paul S, Skolnick P
Naunyn Schmiedebergs Arch Pharmacol. 1981 Jan;315(3):203-9. doi: 10.1007/BF00499836.
Dextro- and levorotatory isomers of 1-(1-phenylcyclohexyl)-3-methylpiperidine (PCMP) were synthesized. Both isomers inhibited spontaneous cerebellar Purkinje neuron firing when applied locally by pressure ejection. This effect was dose-dependent, with the (+)-isomer about 5--7 times more potent than the (-)-isomer. Both isomers also depressed rotarod performance in mice. Again, the (+)-isomer was about 5 times more potent than the (-)-isomer. Both rotarod performance and Purkinje cells discharge were depressed maximally 10--15 min after i.p. injection of drug. Our results suggest a correlation between behavioral performance and central neuron electrophysiological activity and suggest that the central actions of PCP or its derivatives are probably mediated at one locus, by a stereospecific mechanism.
合成了1-(1-苯基环己基)-3-甲基哌啶（PCMP）的右旋和左旋异构体。通过压力喷射局部应用时，两种异构体均抑制小脑浦肯野神经元的自发放电。这种作用呈剂量依赖性，(+)-异构体的效力约为(-)-异构体的5至7倍。两种异构体还降低了小鼠的转棒性能。同样，(+)-异构体的效力约为(-)-异构体的5倍。腹腔注射药物后10至15分钟，转棒性能和浦肯野细胞放电均受到最大程度的抑制。我们的结果表明行为表现与中枢神经元电生理活动之间存在相关性，并表明PCP或其衍生物的中枢作用可能通过一种立体特异性机制在一个位点介导。
