Metoprine(BW197U)是一种有效的组胺N-甲基转移酶(HMT)抑制剂。Metoprine是一种二氨基嘧啶衍生物，可以透过血脑屏障，并通过抑制HMT增加脑组胺水平。Metoprine是一种抗叶酸(antifolate)和抗肿瘤药。
Metoprine (BW 197U) is a potent histamine N-methyltransferase (HMT) inhibitor. Metoprine, a diaminopyrimidine derivative, can cross the blood-brain barrier and increase brain histamine levels by inhibiting HMT[1][2]. Metoprine is an antifolate and antitumor agent[3].
Metoprine (BW 197U; 2-10 mg/kg; IP) ameliorates the memory deficits induced by nucleus basalis magnocellularis (NBM) lesions in a dose-dependent manner[2].Intraperitoneal administration of Metoprine produces various behavioral effects, including decreases in food intake and increases in water consumption[1]. Animal Model: Male Sprague-dawley rats (200-280g)[2]
[1]. Junichi Kitanaka, et al. Brain Histamine N-Methyltransferase As a Possible Target of Treatment for Methamphetamine Overdose. Drug Target Insights. 2016 Mar 2;10:1-7. [2]. Zhong Chen, et al. Effects of brain histamine on memory deficit induced by nucleus basalis-lesion in rats. Acta Pharmacol Sin. 2002 Jan;23(1):66-70. [3]. John R Horton, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. J Mol Biol. 2005 Oct 21;353(2):334-344.
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