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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:
产品名称
CGS 9895, ≥98% (HPLC)
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
H E Shannon et al.
Pharmacology, biochemistry, and behavior, 23(2), 317-323 (1985-08-01)
The effects of diazepam and the pyrazoloquinoline benzodiazepine receptor ligands CGS8216, CGS9896, and CGS9895 on schedule-controlled responding were studied in dogs. Responding was maintained under a multiple fixed-interval (FI) 5-min fixed-ratio (FR) 30 response schedule of food presentation. Diazepam (PO)
L T Schove et al.
Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, 4(5), 307-314 (1994-01-01)
Four pyrazoloquninolinone compounds, variations of known high affinity ligands for the GABA A/Benzodiazepine receptors (BDZRs), were synthesized and their affinities for BDZRs in cerebellum and spinal cord measured and compared to the parent compounds, CGS 8216, CGS 9895, and CGS
N J Katzman et al.
The Journal of pharmacology and experimental therapeutics, 235(3), 589-595 (1985-12-01)
CGS 9895, a pyrazoloquinolone benzodiazepine receptor ligand, was administered alone and concomitantly with diazepam in order to assess its agonist and diazepam-antagonist properties on various behaviors in rodents. In mice, CGS 9895 neither potentiated nor blocked the convulsant effects of
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
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
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