Arfendazam ATC code
Ethyl 7-chloro-4-oxo-5-phenyl-2,3-dihydro-1,5-benzodiazepine-1-carboxylate
CAS Number PubChem CID ChemSpider UNII ChEMBL CompTox Dashboard (EPA ) ECHA InfoCard 100.048.694 Formula C 18 H 17 Cl N 2 O 3 Molar mass 344.792 g·mol−1 3D model (JSmol )
ClC1=CC2=C(C=C1)N(CCC(N2C3=CC=CC=C3)=O)C(OCC)=O
InChI=1S/C18H17ClN2O3/c1-2-24-18(23)20-11-10-17(22)21(14-6-4-3-5-7-14)16-12-13(19)8-9-15(16)20/h3-9,12H,2,10-11H2,1H3
Y Key:NXJWVCHVPUCWJS-UHFFFAOYSA-N
Y
N Y (what is this?)
Arfendazam (INN )[1] is a drug which is a benzodiazepine derivative. Arfendazam is a 1,5-benzodiazepine, with the nitrogen atoms located at positions 1 and 5 of the diazepine ring, and so is most closely related to other 1,5-benzodiazepines such as clobazam .
Arfendazam has sedative and anxiolytic effects similar to those produced by other benzodiazepine derivatives, but is a partial agonist at GABAA receptors, so the sedative effects are relatively mild and it produces muscle relaxant effects only at very high doses.[2] [3]
Arfendazam produces an active metabolite lofendazam , which is thought to be responsible for part of its effects.[4]
See also [ ]
References [ ]
^ "International Nonproprietary Names for Pharmaceutical Substances. Proposed International Nonproprietary Names (Prop. INN): List 39. Supplement to WHO Chronicle" (PDF) . World Health Organization. March 1978. p. 3. Retrieved 4 December 2015 .
^ Mueller E (January 1985). "Benzodiazepine receptor interactions of arfendazam, a novel 1, 5-benzodiazepine". Pharmacopsychiatry . 18 (1): 10–1. doi :10.1055/s-2007-1017288 .
^ Müller WE, Groh B, Bub O (July 1986). "In vitro and in vivo studies of the mechanism of action of arfendazam, a novel 1, 5-benzodiazepine". Pharmacopsychiatry . 19 (4): 314–315. doi :10.1055/s-2007-1017251 .
^ Adrien J, Albani F, Baruzzi A, Berger M, Bixler EO, Borbeley AA, Dikeos DG, Drucker-Colin R, Montero RF, Hishikawa Y, Inoue S (December 2012). The Pharmacology of Sleep . Springer Science & Business Media. ISBN 978-3-540-58961-7 .
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See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators