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CGS-20625

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
CGS-20625
Clinical data
Routes of
administration
By mouth
ATC code
  • none
Pharmacokinetic data
Bioavailability41%
Identifiers
  • 5,6,7,8,9,10-hexahydro-2-(4-methoxyphenyl)-cyclohepta[b]pyrazolo[3,4-d]pyridin-3(2H)-one
CAS Number
PubChemCID
ChemSpider
UNII
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC18H19N3O2
Molar mass309.369 g·mol−1
3D model (JSmol)
  • COC1=CC=C(C=C1)N2C(=O)C3=CN=C4CCCCCC4=C3N2
  • InChI=1S/C18H19N3O2/c1-23-13-9-7-12(8-10-13)21-18(22)15-11-19-16-6-4-2-3-5-14(16)17(15)20-21/h7-11,20H,2-6H2,1H3 ☒N
  • Key:UBLXQFIFWUEVGJ-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

CGS-20625 is ananxiolytic drug used in scientific research. It has similar effects tobenzodiazepine drugs,[1] but is structurally distinct and so is classed as anonbenzodiazepine anxiolytic.[2][3] It produces anxiolytic andanticonvulsant effects, but with nosedative effects even at high doses, and no significant muscle relaxant effects.[4] It is orally active in humans, but with relatively low bioavailability.[5]

CGS-20625 is apositive allosteric modulator at severalGABAA receptors types. Due to itsalicyclic moiety potency atγ1subunit, containing receptor types is more pronounced for CGS-20625 compared to benzodiazepines.[1] γ1 subunits are expressed at higher levels in thecentral amygdala.[6]

References

[edit]
  1. ^abKhom 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.S2CID 15082432.
  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.S2CID 45892825.
  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.
  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.S2CID 22126140.
  6. ^Esmaeili A, Lynch JW, Sah P (January 2009). "GABAA receptors containing gamma1 subunits contribute to inhibitory transmission in the central amygdala".J. Neurophysiol.101 (1):341–9.doi:10.1152/jn.90991.2008.PMID 19004994.S2CID 1590604.
5-HT1ARTooltip 5-HT1A receptoragonists
GABAARTooltip GABAA receptorPAMsTooltip positive allosteric modulators
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