SML0376
CGS 9895
≥98% (HPLC)
别名:
2,5-Dihydro-2-(4-methoxyphenyl)-3H-pyrazolo[4,3-c]quinolin-3-one, NSC 373970
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关于此项目
经验公式（希尔记法）:
C17H13N3O2
化学文摘社编号:
分子量:
291.30
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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
SMILES string
COc1ccc(cc1)N2N=C3C(=CNc4ccccc34)C2=O
InChI key
KSKRJZMRHSNRBX-UHFFFAOYSA-N
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
Quality Level
相关类别
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
Behavioral effects of benzodiazepine antagonists in chlordiazepoxide tolerant and non-tolerant rats.
K Takada et al.
Life sciences, 44(4), 289-299 (1989-01-01)
Rats were trained to respond under 3-min fixed-interval schedules of food presentation, and effects of the benzodiazepine-receptor ligands, flumazenil, 2-(4-methoxy-phenyl)-pyrazolo[4,3-c]quinolin-3(5H)-one (CGS 9895), 3-carbo-t-butoxy-beta-carboline (beta-CCtB), and beta-carboline-3-carboxylic acid ethyl ester (beta-CCE) were assessed before and after the induction of tolerance to
H E Shannon et al.
European journal of pharmacology, 92(1-2), 155-157 (1983-08-19)
The diazepam-like agonist and diazepam antagonist properties of the pyrazoloquinoline benzodiazepine receptor ligands CGS8216, CGS9895 and CGS9896 were evaluated in rats trained to discriminate between saline and 1.0 mg/kg of diazepam in a two-choice, discrete-trial procedure. None of the three
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
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
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