CGP 36216 hydrochloride |
| Catalog No.GC13676 |
Selective GABAB antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 123691-29-2
Sample solution is provided at 25 µL, 10mM.
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CGP 36216 hydrochloride is a potent and selective antagonist of GABAB receptors with IC50 value of 43 µM.
GABAB receptors (GABABR) are metabotropic transmembrane receptors for gamma-aminobutyric acid (GABA) and are linked through G-proteins to potassium channels. Expression of GABAB receptors are found in the central as well as in the autonomic division of the peripheral nervous system. GABAB receptors play a key role in regulating membrane excitability and synaptic transmission in the brain.
In rat neocortical preparations maintained in Mg2+-free Krebs medium, CGP 36216 acts as antagonism of baclofen-induced suppression of spontaneous discharges in a concentration-dependent manner. However, CGP 36216, up to 1 mM, was ineffective in antagonising baclofen-induced hyperpolarisations, mediated through gamma-aminobutyric acid (B) GABAB postsynaptic receptors 1.
In electrically stimulated brain slices preloaded with [3H] GABA, CGP 36216 increased the release of [3H] GABA, that was reversed by baclofen. While CGP 36216 is ineffective at GABAB postsynaptic receptors, it is appreciably more active at presynaptic receptors1.
Reference:
1. Ong J, Bexis S, Marino V, et al. CGP 36216 is a selective antagonist at GABA(B) presynaptic receptors in rat brain. European journal of pharmacology. 2001;415(2-3):191-195.
| Cas No. | 123691-29-2 | SDF | |
| Chemical Name | (3-aminopropyl)(ethyl)phosphinic acid hydrochloride | ||
| Canonical SMILES | CCP(CCCN)(O)=O.Cl | ||
| Formula | C5H14NO2P.HCl | M.Wt | 187.6 |
| Solubility | <18.76mg/ml in DMSO; <18.76mg/ml in Water | Storage | Desiccate at RT |
| 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.3305 mL | 26.6525 mL | 53.3049 mL |
| 5 mM | 1.0661 mL | 5.3305 mL | 10.661 mL |
| 10 mM | 0.533 mL | 2.6652 mL | 5.3305 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 ddH2O, 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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