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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TPMPA Related Antibodies

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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.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TPMPA Related Classifications

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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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HY-101359
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