Jansen K L, Elliot M, Leslie R A
Oxford University Clinical Pharmacology Department, Radcliffe Infirmary, U.K.
Eur J Pharmacol. 1992 Apr 22;214(2-3):281-3. doi: 10.1016/0014-2999(92)90131-m.
The effect of haloperidol upon [3H]1,3-di-o-tolylguanidine ([3H]DTG) binding sites was assessed in rat brain and testes. An acute injection (10 mg/kg), in rats culled 2 h later, changed Kd values from 18 +/- 2 to 108 +/- 26 nM (brain) and 14 +/- 1 to 116 +/- 35 nM (testes), with unchanged Bmax values. Rats were injected with 4 mg/kg per day for 7, 14 and 21 days and culled 4 days after the last injection. By day 21, there was an average fall in Bmax for brain of 30% and for testes of 38%. Kd values remained unchanged. Thus peripheral and central [3H]DTG binding sites were reduced by chronic haloperidol in a similar way.
在大鼠脑和睾丸中评估了氟哌啶醇对[3H]1,3 - 二 - o - 甲苯基胍（[3H]DTG）结合位点的影响。急性注射（10毫克/千克），2小时后处死大鼠，脑内Kd值从18±2变为108±26纳摩尔，睾丸内从14±1变为116±35纳摩尔，Bmax值不变。大鼠每天注射4毫克/千克，持续7天、14天和21天，最后一次注射4天后处死。到第21天，脑内Bmax平均下降30%，睾丸内下降38%。Kd值保持不变。因此，慢性氟哌啶醇以类似方式减少了外周和中枢的[3H]DTG结合位点。
