CGS-20625

drugbox
IUPAC_name = 5,6,7,8,9,10-hexahydro-2-(4-methoxyphenyl)-cyclohepta [b] pyrazolo [3,4-d] pyridin-3(2H)-one

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width = 180
CAS_number = 111205-55-1
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PubChem = 163844
DrugBank =
C=18|H=19|N=3|O=2
molecular_weight = 309.36236 g/mol
smiles = COC1=CC=C(C=C1)N2C(=O)C3=CN=C4CCCCCC4=C3N2
bioavailability = 41%
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routes_of_administration = oral

CGS-20625 is an anxiolytic drug used in scientific research. It has similar effects to, and binds to the same target as benzodiazepine drugs, [Khom S, Baburin I, Timin EN, Hohaus A, Sieghart W, Hering S. Pharmacological properties of GABAA receptors containing gamma1 subunits. "Molecular Pharmacology". 2006 Feb;69(2):640-9. [http://www.ncbi.nlm.nih.gov/pubmed/16272224 PMID 16272224] ] but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic. [Bennett DA. Pharmacology of the pyrazolo-type compounds: agonist, antagonist and inverse agonist actions. "Physiology & Behaviour". 1987;41(3):241-5. [http://www.ncbi.nlm.nih.gov/pubmed/2893398 PMID 2893398] ] [Brunner LA, Luders RC. Determination of a potential anxiolytic drug (CGS 20625) in human plasma by high-performance liquid chromatography. "Journal of Chromatography". 1991 Aug 23;568(2):487-93. [http://www.ncbi.nlm.nih.gov/pubmed/1686029 PMID 1686029] ]

CGS-20625 produces anxiolytic and anticonvulsant effects, but with no sedative effects even at high doses, and no significant muscle relaxant effects. [Williams M, Bennett DA, Loo PS, Braunwalder AF, Amrick CL, Wilson DE, Thompson TN, Schmutz M, Yokoyoma N, Wasley JW. CGS 20625, a novel pyrazolopyridine anxiolytic. "Journal of Pharmacology and Experimental Therapeutics". 1989 Jan;248(1):89-96. [http://www.ncbi.nlm.nih.gov/pubmed/2563294 PMID 2563294] ] It is orally active in humans, but with relatively low bioavailability. [Hirschberg Y, Oberle RL, Ortiz M, Lau H, Markowska M. Oral absorption of CGS-20625, an insoluble drug, in dogs and man. "Journal of Pharmacokinetics and Biopharmaceutics". 1995 Feb;23(1):11-23. [http://www.ncbi.nlm.nih.gov/pubmed/8576841 PMID 8576841] ]

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