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
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
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)
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
C L Brown et al.
European journal of pharmacology, 106(1), 167-173 (1984-10-30)
A series of pyrazoloquinolinones CGS 9896, CGS 9895 and CGS 8216 have been reported to exhibit agonist, partial agonist and antagonist properties, respectively, at the benzodiazepine receptor. We have examined the effects of these compounds and of diazepam on pentylenetetrazole
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