Arfendazam
Arfendazam.svg
Clinical data
ATC code
  • none
Identifiers
  • 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 InfoCard100.048.694 Edit this at Wikidata
Chemical and physical data
FormulaC18H17ClN2O3
Molar mass344.792 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 checkY
  • Key:NXJWVCHVPUCWJS-UHFFFAOYSA-N checkY
 ☒NcheckY (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

References

  1. ^ "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.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.