Application
(1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid hydrate has also been used as γ-aminobutyric acid C (GABAc) blocker in retinal ganglion cells.
TPMA has been used as a GABAC receptor antagonist to study the role of inner retinal inhibition in midget ganglion cells. TPMPA has also been used to study the role of GABAC receptor antagonists in suppressing orientation selectivity in ganglion cells.
Biochem/physiol Actions
TPMPA is a hybrid of isoguvacine and 3-APMPA designed to retain affinity for GABAC receptors but not to interact with GABAA or GABAB receptors. Electrical assays show that TPMPA is a competitive antagonist of cloned human mu 1 GABAC receptors expressed in Xenopus laevis oocytes (Kb approx. 2 µM). TPMPA is >100-fold weaker as an inhibitor of rat brain GABAA receptors expressed in oocytes (Kb approx. 320 µM) and has only weak agonist activity on GABAB receptors assayed in rat hippocampal slices (EC50 approx. 500 µM). TPMPA may be used to investigate GABAC receptor function in the outer retina and in any other areas of the nervous system in which these types of receptor are present.
Features and Benefits
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Legal Information
Sold in the USA under exclusive license from the University of California.
Packaging
10, 50 mg in glass bottle
Preparation Note
(1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) hydrate is soluble in water at 16 mg/ml, but is insoluble in DMSO.
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