Arfendazam

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Arfendazam
Arfendazam.svg
Systematic (IUPAC) name
Ethyl 7-chloro-4-oxo-5-phenyl-2,3-dihydro-1,5-benzodiazepine-1-carboxylate
Identifiers
CAS Number 37669-57-1 YesY
ATC code none
PubChem CID 65803
ChemSpider 59219 YesY
UNII P37G7BTX8V YesY
ChEMBL CHEMBL2104444 N
Chemical data
Formula C18H17ClN2O3
Molar mass 344.792
 NYesY (what is this?)  (verify)

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[edit]

References[edit]

  1. ^ "International Nonproprietary Names for Pharmaceutical Substances. Proposed International Nonproprietary Names (Prop. INN): List 39. Supplement to WHO Chronicle, 1978, Vol. 32, No. 3 (March)" (PDF). World Health Organization. p. 3. Retrieved 4 December 2015. 
  2. ^ Müller E. Benzodiazepine receptor interactions of arfendazam, a novel 1, 5-benzodiazepine. Pharmacopsychiatry 1985, (18):10-11.
  3. ^ Müller WE, Groh B, Bub O. In vitro and in vivo studies of the mechanism of action of arfendazam, a novel 1, 5-benzodiazepine. Pharmacopsychiatry 1986, (10):314-315.
  4. ^ J. Adrien, F. Albani, A. Baruzzi, M. Berger, E.O. Bixler, A.A. Borbeley, D.G. Dikeos, R. Drucker-Colin, R. Fritsch Montero, Y. Hishikawa, S. Inoue, A. Kales, E. Lugaresi, H. Merchant-Nancy, J.M. Monti. The Pharmacology of Sleep. Springer. ISBN 978-3-540-58961-7