Cioli V, Corradino C, Piccinelli D, Rocchi M G, Valeri P
Pharmacol Res Commun. 1984 Jan;16(1):85-100.
Since 1-(m-chlorophenyl)piperazine (mCPP) is a metabolite of trazodone (TRZ) and etoperidone (ETO), two atypical antidepressants, a pharmacological study was undertaken to establish the possible contribution of mCPP to the effects of the parent compounds. Behavioral effects of mCPP in rats consist in head shakes and other signs of serotoninergic stimulation; subtoxic doses also produce clonic convulsions and prostration. TRZ and ETO produce sedation and signs of alpha-adrenergic blockade; subtoxic doses produce tremors, clonic convulsions and prostration. Peripheral effects of norepinephrine (NE) and serotonin (5-HT) in rats are potentiated by mCPP and inhibited by TRZ and ETO. 5-hydroxytriptophan (5-HTP)-induced head twitches in mice are inhibited by TRZ and ETO and unaffected by mCPP. At similar doses mCPP, TRZ and ETO inhibit some nociceptive responses in rats and mice.
由于1-(间氯苯基)哌嗪(mCPP)是两种非典型抗抑郁药曲唑酮(TRZ)和乙哌立酮(ETO)的代谢产物,因此开展了一项药理学研究,以确定mCPP对母体化合物作用可能产生的影响。mCPP对大鼠的行为影响包括头部抖动和其他5-羟色胺能刺激的迹象;亚中毒剂量还会引起阵挛性惊厥和虚脱。TRZ和ETO会产生镇静作用以及α-肾上腺素能阻滞的迹象;亚中毒剂量会引起震颤、阵挛性惊厥和虚脱。mCPP可增强大鼠体内去甲肾上腺素(NE)和5-羟色胺(5-HT)的外周效应,而TRZ和ETO则会抑制这种效应。TRZ和ETO可抑制小鼠体内5-羟色氨酸(5-HTP)诱导的头部抽搐,而mCPP对其无影响。在相似剂量下,mCPP、TRZ和ETO均可抑制大鼠和小鼠的一些伤害性反应。