Itoh Y, Oishi R, Nishibori M, Saeki K
J Pharmacol Exp Ther. 1985 Dec;235(3):788-92.
The effects of phencyclidine (PCP) on the dynamics of brain histamine (HA) were examined in the mouse brain. PCP (2-10 mg/kg i.p.) dose-dependently elevated the level of tele-methylhistamine (t-MH), a predominant metabolite of brain HA, without altering the HA level. PCP also enhanced the accumulation of t-MH after administration of pargyline hydrochloride (80 mg/kg i.p.). PCP at 5 mg/kg facilitated the HA depletion produced by (S)-alpha-fluoromethylhistidine markedly (50 mg/kg i.v.), a specific inhibitor of histidine decarboxylase. Metoprine (10 mg/kg i.p.), an inhibitor of HA-N-methyltransferase, decreased the t-MH level and increased the HA level. In the metoprine-treated mice, PCP at 10 mg/kg had no significant effect on the t-MH level, whereas it significantly increased the HA level. The increase in the t-MH level after administration of PCP (5 mg/kg) was observed in various brain regions except the pons-medulla oblongata. These results suggest that, in mice, PCP increases the brain HA turn-over possibly by facilitating the release of HA.
在小鼠脑中研究了苯环己哌啶（PCP）对脑组胺（HA）动力学的影响。PCP（腹腔注射2-10mg/kg）剂量依赖性地提高了脑HA的主要代谢产物3-甲基组胺（t-MH）的水平，而不改变HA水平。PCP还增强了盐酸帕吉林（腹腔注射80mg/kg）给药后t-MH的积累。5mg/kg的PCP显著促进了由组氨酸脱羧酶特异性抑制剂（S）-α-氟甲基组氨酸（静脉注射50mg/kg）产生的HA耗竭。HA-N-甲基转移酶抑制剂美托普利（腹腔注射10mg/kg）降低了t-MH水平并提高了HA水平。在美托普利处理的小鼠中，10mg/kg的PCP对t-MH水平无显著影响，而显著提高了HA水平。除脑桥-延髓外，在各个脑区均观察到PCP（5mg/kg）给药后t-MH水平的升高。这些结果表明，在小鼠中，PCP可能通过促进HA的释放来增加脑HA的周转率。
