Pipequaline (PK-8165) (Synonyms: 45319 RP, PK 8165 ) |
Catalog No.GC30827
One-Click Copy Product Info
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Pipequaline (PK-8165) (PK 8165) est un agoniste partiel des récepteurs des benzodiazépines avec une activité anxiolytique.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 77472-98-1
Sample solution is provided at 25 µL, 10mM.
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Pipequaline (PK 8165) is a non-selective GABAA receptor partial agonist with anxiolytic activity.
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].
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].
[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.
Animal experiment: | 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]. |
References: [1]. Bradwejn J, et al. Effects of PK 8165, a partial benzodiazepine receptor agonist, on cholecystokinin-inducedactivation of hippocampal pyramidal neurons: a microiontophoretic study in the rat. Eur J Pharmacol. 1985 Jun 19;112(3):415-8. | |
| Cas No. | 77472-98-1 | SDF | |
| Synonymes | 45319 RP, PK 8165 | ||
| Canonical SMILES | C1(C2=CC=CC=C2)=NC3=CC=CC=C3C(CCC4CCNCC4)=C1 | ||
| Formula | C22H24N2 | M.Wt | 316.44 |
| Solubility | DMSO : ≥ 32 mg/mL (101.13 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1602 mL | 15.8008 mL | 31.6016 mL |
| 5 mM | 632 μL | 3.1602 mL | 6.3203 mL |
| 10 mM | 316 μL | 1.5801 mL | 3.1602 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)