Khatua A K, Bhattacharyya M
Department of Biochemistry, University College of Science and Technology, Calcutta, India.
Pol J Pharmacol. 2001 Nov-Dec;53(6):629-34.
Two widely used antipsychotic drugs, chlorpromazine (CPZ) and trifluoperazine (TFZ) inhibit NADPH-induced microsomal lipid peroxidation (LPO). Study of microsomal membrane fluidity revealed considerable disorganization in its architecture in the presence of NADPH, which can be restored back in the presence of CPZ and TFZ. NADPH-dependent microsomal LPO is catalyzed by NADPH: cytochrome P450 reductase. These drugs also inhibit the activity of this enzyme. TFZ always shows stronger inhibitory effect than CPZ. TFZ contains a trifluromethyl group (CF3) in its second position that gives rise to stronger electron abstraction tendency by which LPO and NADPH: cytochrome P450 reductase activity is inhibited more potently than by CPZ which contains a chlorine ligand in the same position. Due to the stronger antioxidant property of TFZ, it can be prescribed as a better therapeutic agent, which plays a protective role for the cellular system.
两种广泛使用的抗精神病药物,氯丙嗪(CPZ)和三氟拉嗪(TFZ)可抑制NADPH诱导的微粒体脂质过氧化(LPO)。微粒体膜流动性研究表明,在NADPH存在下其结构存在相当大的紊乱,而在CPZ和TFZ存在下可恢复正常。NADPH依赖性微粒体LPO由NADPH:细胞色素P450还原酶催化。这些药物也抑制该酶的活性。TFZ的抑制作用总是比CPZ更强。TFZ在其第二个位置含有一个三氟甲基(CF3),这导致更强的电子吸引倾向,通过这种倾向,LPO和NADPH:细胞色素P450还原酶活性比在相同位置含有氯配体的CPZ更有效地受到抑制。由于TFZ具有更强的抗氧化特性,它可以作为一种更好的治疗剂开处方,对细胞系统起到保护作用。