Rilmazafone

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Rilmazafone
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Clinical data
Routes of
administration
oral
Identifiers
CAS Number
PubChem CID
E number{{#property:P628}}
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Chemical and physical data
FormulaC21H20Cl2N6O3
Molar mass475.328

Rilmazafone (Rhythmy, 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan.[1] It has sedative and hypnotic effects.[2][3] Rilmazafone induces impairment of motor function and has hypnotic properties.[4]

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.[5][6]

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Rilmazafone active metabolite

See also

Avizafone

References

  1. 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).
  2. 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).
  3. 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).
  4. Yasui M (2005). "[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]". 25 (3): 143–51. PMID 16045197. Text "Nihon Shinkei Seishin Yakurigaku Zasshi. " ignored (help); Unknown parameter |coauthors= ignored (help); Unknown parameter |month= ignored (help)
  5. 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.
  6. 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.



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