Dopaminergic antagonist
CAS：5588-33-0
分子式： C21H26N2OS2
分子量：386.57
纯度：98%
存储：Store at -20°C
库存：现货

Mesoridazine is an active metabolite of the typical antipsychotic thioridazine.[1],[2] It is formed via sulfoxidation of thioridazine by the cytochrome P450 (CYP) isoform CYP2D6 in human liver microsomes.[3] It binds to histamine H1, dopamine D2, muscarinic acetylcholine, and α1- and α2-adrenergic receptors (Kds = 1.8, 19, 69, 2, and 1,600 nM, respectively).[2] Mesoridazine (10, 30, and 45 mg/kg, i.p.) prevents mescaline-induced hyperactivity in mice.[4]

参考文献:
[1]. von Bahr, C., Movin, G., Nordin, C., et al. Plasma levels of thioridazine and metabolites are influenced by the debrisoquin hydroxylation phenotype. Clin. Pharmacol. Ther. 49(3), 234-240 (1991).
[2]. Richelson, E., and Nelson, A. Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. Eur. J. Pharmacol. 103(3-4), 197-204 (1984).
[3]. Wójcikowski, J., Maurel, P., and Daniel, W.A. Characterization of human cytochrome P450 enzymes involved in the metabolism of the piperidine-type phenothiazine neuroleptic thioridazine. Drug Metab. Dispos. 34(3), 471-476 (2006).
[4]. Shah, N.S. Influence of psychotropic drugs and β-diethylaminoethyl-diphenylpropylacetate (SKF 525-A) on mescaline-induced behavior and on tissue levels of mescaline in mice. Biochem. Pharmacol. 25(5), 591-597 (1976).