CGS-20625

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CGS-20625
Systematic (IUPAC) name
5,6,7,8,9,10-hexahydro-2-(4-methoxyphenyl)-cyclohepta[b]pyrazolo[3,4-d]pyridin-3(2H)-one
Identifiers
CAS number 111205-55-1
ATC code  ?
PubChem 163844
Chemical data
Formula C18H19N3O2 
Mol. mass 309.36236 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 41%
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes 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,[1] but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.[2][3]

CGS-20625 produces anxiolytic and anticonvulsant effects, but with no sedative effects even at high doses, and no significant muscle relaxant effects.[4] It is orally active in humans, but with relatively low bioavailability.[5]



[edit] References

  1. ^ 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. PMID 16272224
  2. ^ Bennett DA. Pharmacology of the pyrazolo-type compounds: agonist, antagonist and inverse agonist actions. Physiology & Behaviour. 1987;41(3):241-5.PMID 2893398
  3. ^ 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. PMID 1686029
  4. ^ 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. PMID 2563294
  5. ^ 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. PMID 8576841