Zharkovskiĭ A M, Chereshka K S, Zharkovskaia T A, Allikmets L Kh
Biull Eksp Biol Med. 1985 Dec;100(12):719-22.
Male Wistar rats were treated chronically with either carbidine (10 mg/kg/day) or haloperidol (1 mg/kg/day) for 23 consecutive days. On days 4-5 after the treatment discontinuation the animals were challenged with apomorphine HCl (0.5 mg/kg) or 5-OTP (150 mg/kg i. p) in combination with pargiline (40 mg/kg i. p) and stereotype responses were scored. In carbidine-treated rats the intensity of stereotype sniffings was increased after apomorphine treatment. In contrast, animals treated with haloperidol exhibited more intensive gnawing after apomorphine in comparison to vehicle-treated rats. 5-OTP-induced head twitches were increased only in carbidine-treated rats. Prolonged carbidine treatment in contrast to haloperidol induced a decrease in 5H-spiperone and 3H-LSD binding in the frontal cortex, with the density of D-2 receptors in the striatum practically unchanged. It is concluded that neuroleptic carbidine in contrast to classical neuroleptics has a more selective effect in serotonin (S-2) receptors and antidepressive properties of this compound may be due to the down-regulation of S-2 receptors in the brain.
将雄性Wistar大鼠连续23天慢性给予卡比啶(10毫克/千克/天)或氟哌啶醇(1毫克/千克/天)。在停药后的第4 - 5天,给动物注射盐酸阿扑吗啡(0.5毫克/千克)或5-羟色氨酸(150毫克/千克腹腔注射)并联合帕吉林(40毫克/千克腹腔注射),对刻板反应进行评分。在接受卡比啶治疗的大鼠中,阿扑吗啡治疗后刻板嗅探的强度增加。相比之下,与接受赋形剂治疗的大鼠相比,接受氟哌啶醇治疗的动物在注射阿扑吗啡后表现出更强烈的啃咬行为。5-羟色氨酸诱导的头部抽搐仅在接受卡比啶治疗的大鼠中增加。与氟哌啶醇相比,长期给予卡比啶会导致额叶皮质中5H-螺哌隆和3H-LSD结合减少,纹状体中D-2受体密度实际上未发生变化。结论是,与经典抗精神病药物相比,抗精神病药物卡比啶对5-羟色胺(S-2)受体具有更具选择性的作用,该化合物的抗抑郁特性可能归因于大脑中S-2受体的下调。