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 metabolitelofendazam, which is thought to be responsible for part of its effects.[4]
^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. S2CID144951247.
^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. S2CID143919337.
^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. ISBN978-3-540-58961-7.