产品描述: | Pipequaline is an anticonflict & anticonvulsant quinoline derivative. It is an anxiolytic drug that was never marketed. It possesses a novel chemical structure that is not closely related to other drugs of this type. The drug has a similar pharmacological profile to the benzodiazepine family of drugs, but with mainly anxiolytic properties and very little sedative, amnestic or anticonvulsant effects, and so is classified as a nonbenzodiazepine anxiolytic |
靶点: |
GABA Receptor;GABAReceptor |
体外研究: |
Pipequaline is extensively bound to plasma proteins: i.e. human serum albumin (HSA), alpha-1-acid glycoprotein (AAG), lipoproteins and blood cells, mainly erythrocytes。 |
体内研究: |
Intravenously administered pipequaline exerts a partial suppression of activations by kainate, glutamate and acetylcholine. Microiontophoretic applications of pipequaline reduces the neuronal activation by kainate[2]. Pipequaline produces dose-related decreases in motor activity. Pipequaline produces significant dose-related decreases in the number of head-dips made。 |
动物实验: |
Rats: Pipequaline is dissolved in water to give injection volumes of 2 mL/kg. Rats are injected with 5, 10, and 50 mg/kg pipequaline. Infrared cells in the walls of the box provided automated measures of locomotor activity and rearing, respectively。 |
参考文献: |
1. Essassi D, et al. Pipequaline transport from blood to brain and liver: role of plasma protein-bound drug. J Pharm Pharmacol. 1989 Sep;41(9):595-600. 2. Debonnel G, et al. Pipequaline acts as a partial agonist of benzodiazepine receptors: an electrophysiological study in the hippocampus of the rat. Neuropharmacology. 1987 Sep;26(9):1337-42. 3. File SE., et al. Sedative effects of PK 9084 and PK 8165, alone and in combination with chlordiazepoxide. Br J Pharmacol. 1983 May;79(1):219-23. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.834 ml |
14.168 ml |
28.336 ml |
5 mM |
0.567 ml |
2.834 ml |
5.667 ml |
10 mM |
0.283 ml |
1.417 ml |
2.834 ml |
50 mM |
0.057 ml |
0.283 ml |
0.567 ml |
|
注意: |
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