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
Clinical data
Legal status	?
Routes	oral
Pharmacokinetic data
Bioavailability	41%
Identifiers
CAS number	111205-55-1^Y
ATC code	None
PubChem	CID 163844
ChemSpider	143700^N
Chemical data
Formula	C₁₈H₁₉N₃O₂
Mol. mass	309.36236 g/mol
SMILES COC1=CC=C(C=C1)N2C(=O)C3=CN=C4CCCCCC4=C3N2
InChI 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
N (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

↑ 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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.

Anxiolytics (N05B)

GABA_A
PAMs

non-N05B	Alcohols (2M2B, Ethanol (beverage), Ethchlorvynol, Methylpentynol) Chlormezanone Etifoxine Inhalants Kavalactones (Kava) Skullcap Valerenic acid (Valerian)

Benzodiazepine	Adinazolam Alprazolam Bretazenil Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl Loflazepate Etizolam Fludiazepam Halazepam Imidazenil Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam

Carbamates	Difebarbamate Emylcamate Febarbamate Mebutamate Meprobamate (Carisoprodol, Tybamate) Phenprobamate Procymate

Nonbenzodiazepines	Abecarnil Adipiplon Alpidem CGS-8216 CGS-9896 CGS-13767 CGS-20625 Divaplon ELB-139 Fasiplon GBLD-345 Gedocarnil L-838,417 NS-2664 NS-2710 Ocinaplon Pagoclone Panadiplon Pipequaline RWJ-51204 SB-205,384 SL-651,498 Taniplon TP-003 TP-13 TPA-023 Y-23684 ZK-93423

Pyrazolopyridines	Cartazolate Etazolate ICI-190,622 Tracazolate

α₂δ VDCC Blockers

CRH₁ Antagonists

mGluR₂_/₃ Agonists

mGluR5 NAMs

TSPO agonists

σ₁ agonists

Antidepressants

Others

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

M: PSO/PSI

mepr

dsrd (o, p, m, p, a, d, s), sysi/epon, spvo

proc (eval/thrp), drug (N5A/5B/5C/6A/6B/6D)

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