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Rilmazafone : ウィキペディア英語版
Rilmazafone

Rilmazafone〔DE Patent 2725164〕 (Rhythmy, 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan.〔Yamamoto K, Hirose K, Matsushita A, Yoshimura K, Sawada T, Eigyo M, Jyoyama H, Fujita A, Matsubara K, Tsukinoki Y, et al. Pharmacological studies of a new sleep-inducer, 1H-1,2,4-triazolyl benzophenone derivatives (450191-S) (I). Behavioral analysis. ''Nippon Yakurigaku Zasshi''. 1984 Jul;84(1):109-54. (Japanese).〕 It has sedative and hypnotic effects.〔Yamamoto K, Matsushita A, Sawada T, Naito Y, Yoshimura K, Takesue H, Utsumi S, Kawasaki K, Hirono S, Koshida H, et al. Pharmacology of a new sleep inducer, 1H-1,2,4-triazolyl benzophenone derivative, 450191-S (II). Sleep-inducing activity and effect on the motor system. ''Nippon Yakurigaku Zasshi''. 1984 Jul;84(1):25-89. (Japanese).〕〔Ibii N, Horiuchi M, Yamamoto K. Pharmacology of a 1H-1, 2, 4-triazolyl benzophenone derivative (450191-S), a new sleep-inducer (III). Behavioral study on interactions of 450191-S and other drugs in mice. ''Nippon Yakurigaku Zasshi''. 1984 Aug;84(2):155-73. (Japanese).〕 Rilmazafone induces impairment of motor function and has hypnotic properties.
Rilmazafone has no effects on benzodiazepine receptors itself, but once inside the body is metabolised by aminopeptidase enzymes in the small intestine to form the active benzodiazepine 8-chloro-6-(2-chlorophenyl)-''N'',''N''-dimethyl-4''H''-1,2,4-triazolo ()()benzodiazepine-2-carboxamide.〔Koike M, Norikura R, Sugeno K. Intestinal activation of a new sleep inducer 450191-S, a 1H-1,2,4-triazolyl benzophenone derivative, in rats. ''Journal of Pharmacobiodynamics''. 1986 Mar;9(3):315-20.〕〔Muranushi N, Miyauchi S, Suzuki H, Sugiyama Y, Hanano M, Kinoshita H, Oguma T, Yamada H. Comparative hepatic transport of desglycylated and cyclic metabolites of rilmazafone in rats: analysis by multiple indicator dilution method. ''Biopharmaceutics and Drug Disposition''. 1993 May;14(4):279-90.〕

==See also==

* Avizafone
* Benzodiazepine

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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