| Name | Pipequaline hydrochloride |
| Description | Pipequaline hydrochloride (PK-8165 hydrochloride) is an anticonflict and anticonvulsant quinoline derivative and an anxiolytic drug that was never marketed. It possesses a novel chemical structure, not closely related to other drugs of this type, with a pharmacological profile similar to benzodiazepines but predominantly anxiolytic, exhibiting minimal sedative, amnestic, or anticonvulsant effects, thus classified as a nonbenzodiazepine anxiolytic. |
| Animal Research | 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[3]. |
| In vitro | Pipequaline is extensively bound to plasma proteins: i.e. human serum albumin (HSA), alpha-1-acid glycoprotein (AAG), lipoproteins and blood cells, mainly erythrocytes[1]. |
| In vivo | 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[3]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : >30 mg/mL (94.8 mM), Sonication is recommended.
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| Keywords | γ-Aminobutyric acid Receptor | PK-8165 Hydrochloride | PK8165 Hydrochloride | PK-8165 | PK8165 | PK 8165 Hydrochloride | PK 8165 | Pipequaline hydrochloride | Pipequaline | Inhibitor | inhibit | Gamma-aminobutyric acid Receptor | GABAReceptor | GABAA | GABA Receptor |
| Inhibitors Related | Valproic acid sodium salt | p-Hydroxybenzaldehyde | Urethane | Baicalin | Penicillin G sodium salt | Valproic Acid | Methyl eugenol | (-)-α-Pinene | Nipecotic acid | Methionine | Dihydromyricetin | Isoflurane |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Antidepressant Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Neuroprotective Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
