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Arfendazam

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
Clinical data
ATC code
  • none
Identifiers
  • Ethyl 7-chloro-4-oxo-5-phenyl-2,3-dihydro-1,5-benzodiazepine-1-carboxylate
CAS Number
  • 37669-57-1 Y
PubChem CID
  • 65803
ChemSpider
  • 59219 Y
UNII
  • P37G7BTX8V
ChEMBL
  • ChEMBL2104444 N
CompTox Dashboard (EPA)
  • DTXSID20191085
ECHA InfoCard100.048.694
Chemical and physical data
FormulaC18H17ClN2O3
Molar mass344.792 g·mol−1
3D model (JSmol)
  • Interactive image
  • 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 Y
  • Key:NXJWVCHVPUCWJS-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

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.


arfendazam, drug, which, benzodiazepine, derivative, benzodiazepine, with, nitrogen, atoms, located, positions, diazepine, ring, most, closely, related, other, benzodiazepines, such, clobazam, clinical, dataatc, codenoneidentifiersiupac, name, ethyl, chloro, p. 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 ArfendazamClinical dataATC codenoneIdentifiersIUPAC name Ethyl 7 chloro 4 oxo 5 phenyl 2 3 dihydro 1 5 benzodiazepine 1 carboxylateCAS Number37669 57 1 YPubChem CID65803ChemSpider59219 YUNIIP37G7BTX8VChEMBLChEMBL2104444 NCompTox Dashboard EPA DTXSID20191085ECHA InfoCard100 048 694Chemical and physical dataFormulaC 18H 17Cl N 2O 3Molar mass344 792 g mol 13D model JSmol Interactive imageSMILES ClC1 CC2 C C C1 N CCC N2C3 CC CC C3 O C OCC OInChI 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 YKey NXJWVCHVPUCWJS UHFFFAOYSA N Y N Y what is this verify 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 EditBenzodiazepineReferences Edit 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 Muller 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 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 amp Business Media ISBN 978 3 540 58961 7 This sedative related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Arfendazam amp oldid 1075851594, wikipedia, wiki, book, books, library,

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