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词条 Rilmazafone
释义

  1. See also

  2. References

  3. External links

{{Drugbox
| Watchedfields = changed
| verifiedrevid = 451729144
| IUPAC_name = 1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-5-[(glycylamino)methyl]-N,N-dimethyl-1H-1,2,4-triazole-3-carboxamide
| image = Rilmazafone structure.svg
| width = 220
| tradename = Rhythmy
| Drugs.com = {{drugs.com|international|rilmazafone}}
| legal_status = ℞-only (JP)
| routes_of_administration = Oral (tablets)
| bioavailability =
| metabolism =
| elimination_half-life = 10.5 h
| excretion = Urine
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 99593-25-6
| ATC_prefix = none
| PubChem = 5069
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 4891
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = CU3H37T766
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D08481
| C=21 | H=20 | Cl=2 | N=6 | O=3
| molecular_weight = 475.328 g/mol
| smiles = ClC1=C(C(C2=CC(Cl)=CC=C2N3C(CNC(CN)=O)=NC(C(N(C)C)=O)=N3)=O)C=CC=C1
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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)
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = KYHFRCPLIGODFH-UHFFFAOYSA-N
| synonyms = 5-([(2-aminoacetyl)amino]methyl)-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1,2,4-triazole-3-carboxamide
}}Rilmazafone[1] (リスミー, Rhythmy, previously known as 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

  • Avizafone
  • Benzodiazepine
  • GL-II-73

References

1. ^DE Patent 2725164
2. ^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).
3. ^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).
4. ^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).
5. ^{{cite journal |author=Yasui M |author2=Kato A |author3=Kanemasa T |author4=Murata S |author5=Nishitomi K |author6=Koike K |author7=Tai N |author8=Shinohara S |author9=Tokomura M |author10=Horiuchi M |author11=Abe K. |title=[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes] |volume=25 |issue=3 |pages=143–51 |date=June 2005 |pmid=16045197 |journal=Nihon Shinkei Seishin Yakurigaku Zasshi }}
6. ^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.
7. ^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.

External links

  • {{ja icon}} {{cite web|title=リスミー'リルマザホン塩酸塩水和物錠 Rhythmy (rilmazafone hydrochloride hydrate, tablets) Prescribing Information.|url=http://database.japic.or.jp/pdf/newPINS/00001601.pdf|publisher=Shionogi & Co., Ltd.}}
  • Drug Information Sheet
{{Benzodiazepines}}{{GABAAR PAMs}}

8 : Acetamides|Benzodiazepines|Benzophenones|Chloroarenes|GABAA receptor positive allosteric modulators|Japanese inventions|Prodrugs|Triazoles

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