TPMPA (hydrate) |
Catalog No.GC48191
One-Click Copy Product Info
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A selective GABAA-ρ1 (ρ1 GABAC) receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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TPMPA is a GABAA-Ρ1 (Ρ1 GABAC) receptor antagonist that is 8-fold selective for GABAA-Ρ1 over GABAA-Ρ2 (Ρ2 GABAC) receptors expressed in X. laevis oocytes (Kbs = 2 and 16 μM, respectively).1 In rat hippocampal slices, TPMPA blocks the inhibitory effect of the GABAB agonist 3-APMPA on excitatory postsynaptic currents (EPSCs) with an EC50 value of 490 μM.2 TPMPA (100 μM) increases light sensitivity and the maximal response of rat retinal ganglion cells without altering their dynamic range.3 In sleeping rats, TPMPA (50 μg, i.c.v.) increases waking from 45 to 62% compared to a vehicle control and decreases slow-wave and paradoxical sleep (REM) by 11 and 5.4%, respectively.4
1.Chebib, M., Mewett, K.N., and Johnston, G.A.GABAC receptor antagonists differentiate between human Ρ1 and Ρ2 receptors expressed in Xenopus oocytesEur. J. Pharmacol.357(2-3)227-234(1998) 2.Ragozzino, D., Woodward, R.M., Murata, Y., et al.Design and in vitro pharmacology of a selective γ-aminobutyric acidC receptor antagonistMol. Pharmacol.50(4)1024-1030(1996) 3.Jensen, R.J.Blocking GABAC receptors increases light responsiveness of retinal ganglion cells in a rat model of retinitis pigmentosaExp. Eye Res.10521-26(2012) 4.Arnaud, C., Gauthier, P., and Gottesmann, C.Study of a GABAC receptor antagonist on sleep-waking behavior in ratsPsychopharmacology (Berl)154(4)415-419(2001)
| Cas No. | N/A | SDF | |
| Chemical Name | P-methyl-P-(1,2,3,6-tetrahydro-4-pyridinyl)-phosphinic acid, hydrate | ||
| Canonical SMILES | CP(C1=CCNCC1)(O)=O.O | ||
| Formula | C6H12NO2P.XH2O | M.Wt | 161.1 |
| Solubility | PBS (pH 7.2): 10 mg/ml | 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. |
||
| 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 | 6.2073 mL | 31.0366 mL | 62.0732 mL |
| 5 mM | 1.2415 mL | 6.2073 mL | 12.4146 mL |
| 10 mM | 620.7 μL | 3.1037 mL | 6.2073 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: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)