CGS-20625

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
Clinical data
Pregnancy cat.  ?
Legal status  ?
Routes oral
Pharmacokinetic data
Bioavailability 41%
Identifiers
CAS number 111205-55-1
ATC code  ?
PubChem CID 163844
Chemical data
Formula C18H19N3O2 
Mol. mass 309.36236 g/mol
SMILES eMolecules & PubChem
 Y(what is this?)  (verify)

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]

References

  1. ^ Khom S, Baburin I, Timin EN, Hohaus A, Sieghart W, Hering S (Feb 2006). "Pharmacological properties of GABAA receptors containing gamma1 subunits". Mol Pharmacol. 69 (2): 640–9. doi:10.1124/mol.105.017236. PMID 16272224. 
  2. ^ Bennett DA (1987). "Pharmacology of the pyrazolo-type compounds: agonist, antagonist and inverse agonist actions". Physiol. Behav. 41 (3): 241–5. doi:10.1016/0031-9384(87)90360-X. PMID 2893398. http://linkinghub.elsevier.com/retrieve/pii/0031-9384(87)90360-X. 
  3. ^ Brunner LA, Luders RC (Aug 1991). "Determination of a potential anxiolytic drug (CGS 20625) in human plasma by high-performance liquid chromatography". J Chromatogr. 568 (2): 487–93. doi:10.1016/0378-4347(91)80188-I. PMID 1686029. 
  4. ^ Williams M, Bennett DA, Loo PS, et al. (Jan 1989). "CGS 20625, a novel pyrazolopyridine anxiolytic". J Pharmacol Exp Ther. 248 (1): 89–96. PMID 2563294. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=2563294. 
  5. ^ Hirschberg Y, Oberle RL, Ortiz M, Lau H, Markowska M (Feb 1995). "Oral absorption of CGS-20625, an insoluble drug, in dogs and man". J Pharmacokinet Biopharm 23 (1): 11–23. doi:10.1007/BF02353783. PMID 8576841.