Arfendazam
Chemical compound
- none
- Ethyl 7-chloro-4-oxo-5-phenyl-2,3-dihydro-1,5-benzodiazepine-1-carboxylate
- 37669-57-1
Y
- 65803
- 59219 Y
- P37G7BTX8V
- ChEMBL2104444
N
- DTXSID20191085
- Interactive image
- ClC1=CC2=C(C=C1)N(CCC(N2C3=CC=CC=C3)=O)C(OCC)=O
InChI
- 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,2,10-11H2,1H3Y
- Key:NXJWVCHVPUCWJS-UHFFFAOYSA-NY
N
Y (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
- ^ "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. S2CID 144951247.
- ^ 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. S2CID 143919337.
- ^ 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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