2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. TPMPA

TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells.

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TPMPA Chemical Structure

TPMPA Chemical Structure

CAS No. : 182485-36-5

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Based on 1 publication(s) in Google Scholar

TPMPA Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells[1][2][3].

IC50 & Target

KB: 2.1 μM (GABAC)
Cellular Effect
Cell Line Type Value Description References
Oocyte IC50
2.22 μM
Compound: 3, TPMPA
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte IC50
22.09 μM
Compound: 3, TPMPA
Antagonist activity at human recombinant GABAc rho-2 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-2 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte EC50
500 μM
Compound: 3, TPMPA
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
[PMID: 24900248]
Oocyte EC50
500 μM
Compound: 3, TPMPA
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
[PMID: 18528996]
In Vitro

TPMPA antagonizes the GABA currents of ρ1 receptors (IC50 = 1.6 μM) and those of the chimeric ρ1/α1 receptors with approximately the same potency (IC50 = 1.3 μM)[1].
TPMPA shows weak activity against rho-1 and rho-2 receptors, with the KB values of 2.0 and 15.6 μM, respectively[2]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TPMPA Related Antibodies
Molecular Weight

161.14

Formula

C6H12NO2P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=P(C1=CCNCC1)(C)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 25 mg/mL (155.14 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.2058 mL 31.0289 mL 62.0578 mL
5 mM 1.2412 mL 6.2058 mL 12.4116 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 6.2058 mL 31.0289 mL 62.0578 mL 155.1446 mL
5 mM 1.2412 mL 6.2058 mL 12.4116 mL 31.0289 mL
10 mM 0.6206 mL 3.1029 mL 6.2058 mL 15.5145 mL
15 mM 0.4137 mL 2.0686 mL 4.1372 mL 10.3430 mL
20 mM 0.3103 mL 1.5514 mL 3.1029 mL 7.7572 mL
25 mM 0.2482 mL 1.2412 mL 2.4823 mL 6.2058 mL
30 mM 0.2069 mL 1.0343 mL 2.0686 mL 5.1715 mL
40 mM 0.1551 mL 0.7757 mL 1.5514 mL 3.8786 mL
50 mM 0.1241 mL 0.6206 mL 1.2412 mL 3.1029 mL
60 mM 0.1034 mL 0.5171 mL 1.0343 mL 2.5857 mL
80 mM 0.0776 mL 0.3879 mL 0.7757 mL 1.9393 mL
100 mM 0.0621 mL 0.3103 mL 0.6206 mL 1.5514 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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TPMPA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TPMPA182485-36-5GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorisoguvacine3-APMPAganglionρ1/α1rho-1rho-2Inhibitorinhibitorinhibit

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