(1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid hydrate 

TPMPA is a hybrid of isoguvacine and 3-APMPA designed to retain affinity for GABA_C receptors but not to interact with GABA_A or GABA_B receptors. Electrical assays show that TPMPA is a competitive antagonist of cloned human mu 1 GABA_C receptors expressed in Xenopus laevis oocytes (Kb approx. 2 μM). TPMPA is >100-fold weaker as an inhibitor of rat brain GABA_A receptors expressed in oocytes (Kb approx. 320 μM) and has only weak agonist activity on GABA_B receptors assayed in rat hippocampal slices (EC₅₀ approx. 500 μM). TPMP_A may be used to investigate GABA_C receptor function in the outer retina and in any other areas of the nervous system in which these types of receptor are present.

Sold in the USA under exclusive license from the University of California.

≥97% (HPLC)

solid

white to off-white

H₂O: 16 mg/mL

DMSO: insoluble

Murata, Y., et al., The first selective antagonist for a GABA_C receptor. Bioorg. Med. Chem. Lett. 6, 2073-2076, (1996)

Johnston, G., GABA_C receptors: Relatively simple transmitter-gated ion channels? Trends Pharmacol. Sci. 17, 319-323, (1996) abstract

Ragozzino, D., et al., Design and in vitro pharmacology of a selective γ-aminobutyric acid C receptor antagonist. Mol. Pharmacol. 50, 1024-1030, (1996) abstract

Chebib, M., et al., Analogues of γ-aminobutyric acid (GABA) and trans-4-aminocrotonic acid (TACA) substituted in the 2 position as GABA_C receptor antagonist. Br. J. Pharmacol. 122, 1551, (1997) abstract

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