Rilmazafone


Rilmazafone

Drugbox
IUPAC_name =5-( [(2-aminoacetyl)amino] methyl)-1- [4-chloro-2-(2-chlorobenzoyl)phenyl] -N,N-dimethyl-1,2,4-triazole-3-carboxamide


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CAS_number=99593-25-6
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PubChem=5069
DrugBank=
C=21 | H=20 | Cl=2 | N=6 | O=3
molecular_weight = 475.328
bioavailability=
metabolism =
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pregnancy_category =
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routes_of_administration= oral

Rilmazafone (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. [cite journal |author=Yasui M |coauthors=Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, Tai N, Shinohara S, Tokomura M, Horiuchi M, Abe K. |title= [Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes] |volume=25 |issue=3 |pages=143–51 |month=Jun |year=2005 |pmid=16045197 |journal=Nihon Shinkei Seishin Yakurigaku Zasshi ]

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-4H-1,2,4-triazolo [1,5-a] [1,4] 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.]

Rilmazafone active metabolite

ee also

*Avizafone

References


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