Honma T, Kitagawa S
Nihon Yakurigaku Zasshi. 1977 Apr;73(3):337-45. doi: 10.1254/fpj.73.337.
Minor tranquilizers (diazepam, nitrazepam, oxazepam, bromazepam, medazepam, fludiazepam, meprobamate) at low doses increased ambulation score to 145 approximately 288% of control rats. Nitrazepam, diazepam and bromazepam which are potent, clinically prescribed minor tranquilizers increased the ambulation at lower doses than was seen with the other drugs. Fludiazepam and nitrazepam showed a maximum increase in ambulation at the same dose. Fludiazepam, nitrazepam and diazepam proved to have potent inhibitory effects on defecation. Trifluperidol, haloperidol and ID-4708 (a new butyrophenone derivative) and chlorpromazine when given at low doses reduced ambulation, while at higher doses defecation was inhibited. These four drugs reduced ambulation and elicited a recover in rates of defecation in methamphetamine treated rats. Clozapine, thioridazine and floropipamide inhibited defecation at nearly the same doses which reduced ambulation in rats not given the methamphetamine tratment. These three durugs reduced ambulation, but did not produce a recovery in the defecation rates in methamphetamine-treated rats. These results indicate that neuroleptics such as clozapine which rarely induce extrapyramidal side-effects when clinically prescribed, inhibit defecation at nearly the same doses which reduce ambulation. In methamphetamine-treated rats, haloperidol was 31 times more potent than chlorpromazine in inhibiting activity noted with ambulation. This ratio in open-field test was close to the ratio of potency of these drugs as antipsychotic clinically prescribed agents.
小剂量的弱安定药(地西泮、硝西泮、奥沙西泮、溴西泮、美达西泮、氟西泮、甲丙氨酯)可使活动评分提高到145,约为对照大鼠的288%。硝西泮、地西泮和溴西泮是强效的临床常用弱安定药,在比其他药物更低的剂量下就能增加活动量。氟西泮和硝西泮在相同剂量时活动量增加最多。氟西泮、硝西泮和地西泮对排便有强效抑制作用。三氟哌多、氟哌啶醇和ID - 4708(一种新的丁酰苯衍生物)以及氯丙嗪在低剂量时会减少活动量,而在高剂量时会抑制排便。这四种药物在甲基苯丙胺处理的大鼠中减少活动量并使排便率恢复。氯氮平、硫利达嗪和氟罗哌酰胺在几乎相同的剂量下抑制排便,这些剂量会降低未接受甲基苯丙胺处理的大鼠的活动量。这三种药物减少活动量,但在甲基苯丙胺处理的大鼠中并未使排便率恢复。这些结果表明,像氯氮平这样在临床用药时很少引起锥体外系副作用的抗精神病药物,在几乎相同的剂量下抑制排便并降低活动量。在甲基苯丙胺处理的大鼠中,氟哌啶醇在抑制活动量方面比氯丙嗪强31倍。在旷场试验中的这个比例接近这些药物作为临床抗精神病药物的效价比。