Rilmazafone
Rilmazafone
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| Systematic (IUPAC) name |
| 1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-5-[(glycylamino)methyl]-N,N-dimethyl-1H-1,2,4-triazole-3-carboxamide |
| Clinical data |
| AHFS/Drugs.com |
International Drug Names |
| Pregnancy cat. |
? |
| Legal status |
? |
| Routes |
oral |
| Pharmacokinetic data |
| Half-life |
10.5 h |
| Excretion |
urine |
| Identifiers |
| CAS number |
99593-25-6 Y |
| ATC code |
None |
| PubChem |
CID 5069 |
| ChemSpider |
4891 Y |
| UNII |
CU3H37T766 Y |
| KEGG |
D08481 Y |
| Synonyms |
5-([(2-aminoacetyl)amino]methyl)-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide |
| Chemical data |
| Formula |
C21H20Cl2N6O3 |
| Mol. mass |
475.328 |
| SMILES |
eMolecules & PubChem |
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InChI=1S/C21H20Cl2N6O3/c1-28(2)21(32)20-26-17(11-25-18(30)10-24)29(27-20)16-8-7-12(22)9-14(16)19(31)13-5-3-4-6-15(13)23/h3-9H,10-11,24H2,1-2H3,(H,25,30) Y
Key:KYHFRCPLIGODFH-UHFFFAOYSA-N Y
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Y(what is this?) (verify)
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Rilmazafone[1] (Rhythmy, 450191-S) is a water-soluble benzodiazepine prodrug developed in Japan.[2] It has sedative and hypnotic effects.[3][4] Rilmazafone induces impairment of motor function and has hypnotic properties.[5]
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.[6][7]
See also
References
- ^ DE Patent 2725164
- ^ 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).
- ^ 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).
- ^ Yasui M; Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, Tai N, Shinohara S, Tokomura M, Horiuchi M, Abe K. (June 2005). "[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]". Nihon Shinkei Seishin Yakurigaku Zasshi 25 (3): 143–51. PMID 16045197.
- ^ 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.
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| 1,4-Benzodiazepines |
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| 1,5-Benzodiazepines |
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| 2,3-Benzodiazepines * |
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| Triazolobenzodiazepines |
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| Imidazobenzodiazepines |
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| Oxazolobenzodiazepines |
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| Thienodiazepines |
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| Pyridodiazepines |
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| Pyrazolodiazepines |
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| Pyrrolodiazepines |
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| Tetrahydroisoquinobenzodiazepines |
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| Benzodiazepine prodrugs |
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