Adinazolam

Adinazolam

Systematic (IUPAC) name
1-(8-chloro-6-phenyl-4H-[1,2,4]triazolo[4,5-a] [1,4]benzodiazepin-1-yl)-N,N-dimethylmethanamine
Clinical data
Pregnancy cat.	?
Legal status	Schedule IV(US)
Routes	Oral
Pharmacokinetic data
Bioavailability	?
Metabolism	Hepatic
Half-life	< 3 hours
Excretion	Renal
Identifiers
CAS number	37115-32-5 Y
ATC code	N05BA07
PubChem	CID 37632
DrugBank	APRD00724
ChemSpider	34519 Y
UNII	KN08449444 Y
KEGG	D02770 Y
ChEBI	CHEBI:251412 Y
ChEMBL	CHEMBL328250 Y
Chemical data
Formula	C19H18ClN5
Mol. mass	351.8
SMILES	eMolecules & PubChem
InChI InChI=1S/C19H18ClN5/c1-24(2)12-18-23-22-17-11-21-19(13-6-4-3-5-7-13)15-10-14(20)8-9-16(15)25(17)18/h3-10H,11-12H2,1-2H3 Y Key:GJSLOMWRLALDCT-UHFFFAOYSA-N Y
N(what is this?)  (verify)

Adinazolam^[1] (marketed under the brand name Deracyn) is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and antidepressant^[2] properties. Adinazolam was developed by Dr. Jackson B. Hester, who was seeking to enhance the antidepressant properties of alprazolam, which he also developed.^[3]

Indications

Adinazolam is indicated as a treatment for anxiety and status epilepticus.

Pharmacology

Adinazolam produces inhibitory effects by binding to GABA receptors. This increases the effects of GABA.

Metabolism

Adinazolam was reported to have active metabolites in the August 1984 issue of The Journal of Pharmacy and Pharmacology.^[4] The main metabolite is N-desmethyladinazolam.^[5] The other two metabolites are alpha-hydroxyalprazolam and estazolam.^[6] In the August 1986 issue of that same journal, Sethy, Francis and Day reported that proadifen inhibited the formation of N-desmethyladinazolam.^[7]

Chemistry

Hester, J. B.; Rudzik, A. D.; Von Voigtlander, P. F.; J. Med. Chem. 1980, 23, 392.

http://dx.doi.org/10.1021/jm00178a009

See also

• Benzodiazepine

References

1. ^ FR Patent 2248050
2. ^ Lahti, Robert A.; Vimala H. Sethy, Craig Barsuhn, Jackson B. Hester (November 1983). "Pharmacological profile of the antidepressant adinazolam, a triazolobenzodiazepine.". Neuropharmacology 22 (11): 1277–82. doi:10.1016/0028-3908(83)90200-9. PMID 6320036. 
3. ^ "Discovers Award 2004" (PDF). Special Publications. Pharmaceutical Research and Manufactureres of America. April 2004. pp. 39. Archived from the original on August 24, 2006. http://web.archive.org/web/20060824202348/http://international.phrma.org/publications/publications/admin/2004-10-12.1086.pdf. Retrieved August 18, 2006. 
4. ^ Sethy, Vimala H.; R. J. Collins and E. G. Daniels (August 1984). "Determination of biological activity of adinazolam and its metabolites.". Journal of Pharmacy and Pharmacology 36 (8): 546–8. doi:10.1111/j.2042-7158.1984.tb04449.x. PMID 6148400. 
5. ^ Peng, G. W. (August 1984). "Assay of adinazolam in plasma by liquid chromatography". Journal of Pharmaceutical Sciences 73 (8): 1173–5. doi:10.1002/jps.2600730840. PMID 6491930. 
6. ^ Fraser, A. D.; A. F. Isner and W. Bryan (November-December 1993). "Urinary screening for adinazolam and its major metabolites by the Emit d.a.u. and FPIA benzodiazepine assays with confirmation by HPLC". Journal of Analytical Toxicology 17 (7): 427–31. PMID 8309217. 
7. ^ Sethy, Vimala H.; Jonathan W. Francis and J. S. Day (August 1986). "The effect of proadifen on the metabolism of adinazolam". Journal of Pharmacy and Pharmacology 38 (8): 631–2. doi:10.1111/j.2042-7158.1986.tb03099.x. PMID 2876087. 

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.v · Categories: Benzodiazepines Hypnotics Organochlorides Triazolobenzodiazepines Nervous system drug stubs Wikimedia Foundation. 2010. Игры ⚽ Нужен реферат? Great Northern Railway (Ireland) Langerado Look at other dictionaries: Адиназолам — (Adinazolam, Дерацин) умеренный антидепрессант с мощным анксиолитическим, отчётливым тимоаналептическим и некоторым гипнотическим действием. Близок по действию к алпразоламу, но в отличие от него обладает холинолитическим эффектом. По общей… …   Энциклопедический словарь по психологии и педагогике Clazolam — Systematic (IUPAC) name 2 chloro 5 methyl 5,9,10,14b tetrahydroisoquino[2,1 d][1,4]benzodiazepin 6(7H) one Clinical data Pregnancy cat …   Wikipedia Benzodiazepine — Benzodiazepines …   Wikipedia Diazepam — Systematic (IUPAC) name 7 chlo …   Wikipedia Alprazolam — Alprazolam …   Wikipedia Lorazepam — Systematic (IUPAC) name (RS) 9 chloro 6 (2 chlorophenyl) 4 hydroxy …   Wikipedia Bromazepam — Systematic (IUPAC) name 9 bromo 6 pyridin 2 …   Wikipedia Oxazepam — Identifiers CAS number …   Wikipedia Clobazam — Not to be confused with clonazepam. Clobazam Systematic (IUPAC) name …   Wikipedia Nordazepam — Systematic (IUPAC) name 7 chloro 5 phenyl 1,3 dihydro 2H 1,4 benzodiaze …   Wikipedia 18+ © Academic, 2000-2024 Contact us: Technical Support, Advertising Dictionaries export, created on PHP, Joomla, Drupal, WordPress, MODx. Mark and share Search through all dictionaries Translate… Search Internet Share the article and excerpts Direct link … Do a right-click on the link above and select “Copy Link”