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Rilmazafone



Rilmazafone
Systematic (IUPAC) name
5-([(2-aminoacetyl)amino]methyl)-1-[4-chloro-2-(2-chlorobenzoyl)phenyl] -N,N-dimethyl-1,2,4-triazole-3-carboxamide
Identifiers
CAS number 99593-25-6
ATC code  ?
PubChem 5069
Chemical data
Formula C21H20Cl2N6O3 
Mol. mass 475.328
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes oral

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]


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; Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, Tai N, Shinohara S, Tokomura M, Horiuchi M, Abe K. (Jun 2005). "[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]" 25 (3): 143-51. PMID 16045197.
  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.
v • d • e
Benzodiazepines (N05BA, N05CD)
1,4-Benzodiazepines
Triazolobenzodiazepines
Imidazobenzodiazepines
Oxazolobenzodiazepines
ThienobenzodiazepinesBrotizolam • Clotiazepam • Etizolam
1,5-BenzodiazepinesArfendazam • Clobazam • Lofendazam • Triflubazam
2,3-BenzodiazepinesGirisopam • GYKI-52895 • Nerisopam • Tofisopam
Benzodiazepine ProdrugsAvizafone • Rilmazafone
OthersBentazepam • Ketazolam • Tifluadom • Zolazepam
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Rilmazafone". A list of authors is available in Wikipedia.
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