9-Amino-1,2,3,4-Tetrahydroacridine Is a Potent Inhibitor of Histamine N-Methyltransferase.
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概要
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The effect of 9-amino-1, 2, 3, 4-tetrahydroacridine (THA) on histamine N-methyltransferase (HMT), an enzyme catalyzing the methylation of histamine to form <I>tele</I>-methylhistamine in the brain, was studied in vitro using a partially purified enzyme preparation from bovine brain and in vivo in the mouse brain. THA inhibited the HMT activity in competitive and non-competitive mixed type manners with respect to histamine. The K<SUB>i</SUB> and K<SUB>i</SUB>' values were 75 nM and 1.2 μM, respectively. The IC<SUB>50</SUB> values for THA, 9-aminoacridine and physostigmine in the inhibition of HMT determined at fixed concentrations of histamine (20 μM) and S-adenosylmethionine (50 μM) were 0.2, 0.37 and 20 μM, respectively. Neostigmine exhibited only 15% inhibition even at a concentration of 100 μM. THA (2-10 mg/kg, s.c.) dose-dependently inhibited HMT in the mouse brain. The inhibition of HMT by THA (10 mg/kg) was marked at 30 and 60 min after treatment, but disappeared by 120 min after. THA (10 mg/kg) significantly increased the histamine level and decreased the <I>tele</I>-methylhistamine level in the mouse brain. These results indicate that THA is a potent inhibitor of HMT.
- 公益社団法人 日本薬理学会の論文
著者
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Oishi Ryozo
Department Of Hospital Pharmacy Faculty Of Medicine Kyushu University
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Saeki Kiyomi
Department Of Pharmacology Okayama University Medical School
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Nishibori Masahiro
Department Of Pharmacology Okayama University Graduate School Of Medicine And Dentistry
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Itoh Yoshinori
Department Of Cardiorenal And Cerebrovascular Medicine Kagawa University
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