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SML0376

CGS 9895

≥98% (HPLC)

Synonym(s):

2,5-Dihydro-2-(4-methoxyphenyl)-3H-pyrazolo[4,3-c]quinolin-3-one, NSC 373970

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About This Item

Empirical Formula (Hill Notation):
C17H13N3O2
CAS Number:
77779-50-1
Molecular Weight:
291.30
NACRES:
NA.77
PubChem Substance ID:
329825377
UNSPSC Code:
12352200
MDL number:
MFCD23704790
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
desiccated
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Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

light yellow to light brown

solubility

DMSO: >2 mg/mL (warmed)

storage temp.

2-8°C

SMILES string

COc1ccc(cc1)N2N=C3C(=CNc4ccccc34)C2=O

InChI

1S/C17H13N3O2/c1-22-12-8-6-11(7-9-12)20-17(21)14-10-18-15-5-3-2-4-13(15)16(14)19-20/h2-10,18H,1H3

InChI key

KSKRJZMRHSNRBX-UHFFFAOYSA-N

Biochem/physiol Actions

CGS 9895 is a GABA antagonist that acts via the benzodiazepine binding site of ag containing GABA receptors. CGS 9895 is the only known compound that can specifically enhance GABA-induced currents in ab subunit containing receptors, and acts at the extracellular a1+b3- subunit interface.
CGS 9895 is a GABA antagonist; GABAA receptor selective enhancer.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
083M4609V
062M4605V

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D A Bennett
Physiology & behavior, 41(3), 241-245 (1987-01-01)
Five compounds that bind to the benzodiazepine (BZ) receptor, but show different pharmacological characteristics from the classical BZs, are profiled. CGS 8216 is a BZ antagonist/inverse agonist that reverses the effects of diazepam and also acts as a proconvulsant. CGS
K Wegelius et al.
European journal of pharmacology, 263(1-2), 141-147 (1994-09-22)
The effects of benzodiazepine receptor ligands with different intrinsic activity profiles were studied on voluntary ethanol consumption in the selectively bred alcohol-preferring AA (Alko, Alcohol) rat line, and compared to those of an opiate antagonist, naloxone, and a serotonin uptake
S J Cooper et al.
Psychopharmacology, 89(4), 462-466 (1986-01-01)
Non-deprived male rats were familiarized with a highly palatable diet until baseline consumption in a 30-min daily access period had stabilised. Stereospecificity of the hyperphagic effect of benzodiazepine receptor agonists was demonstrated using two enantiomers, the (S)-enantiomer being Ro11-3128 (methylclonazepam)
C Brown et al.
European journal of pharmacology, 103(1-2), 139-143 (1984-08-03)
The pyrazoloquinolinones CGS 9896, CGS 9895 and CGS 8216 potently displace the benzodiazepines from their CNS binding site in vitro but have been reported to display agonist, partial agonist and antagonist activity respectively in a number of in vivo tests
S J Cooper et al.
Physiology & behavior, 41(3), 247-255 (1987-01-01)
Several categories of compounds active at benzodiazepine receptors (BZR) in the brain have been distinguished: agonists, antagonists and the novel category of inverse agonist. In terms of their effects on ingestional responses (e.g., food, saline and water consumption), agonists increase
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Global Trade Item Number

SKUGTIN
SML0376-5MG04061832075624
SML0376-25MG04061832075617

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