Arfendazam

Arfendazam

Clinical data
ATC code	none
Identifiers
IUPAC name Ethyl 7-chloro-4-oxo-5-phenyl-2,3-dihydro-1,5-benzodiazepine-1-carboxylate
CAS Number	37669-57-1
PubChem (CID)	65803
ChemSpider	59219
UNII	P37G7BTX8V
ChEMBL	CHEMBL2104444
Chemical and physical data
Formula	C18H17ClN2O3
Molar mass	344.792
3D model (Jmol)	Interactive image
SMILES 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,2,10-11H2,1H3 Key:NXJWVCHVPUCWJS-UHFFFAOYSA-N
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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 GABA_A 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

• Benzodiazepine

References

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