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HomeProduct name list(1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID

(1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID

Synonym(s):TPMPA hydrate

(1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID Structural

What is (1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID?

The Uses of (1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID

Neurochemical tool.

The Uses of (1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID

TPMPA is a selective, competitive GABAC antagonist with only minimal effects on GABAA and GABAB receptor.

The Uses of (1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID

(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.

What are the applications of Application

TPMPA is TPMPA is a competitive, selective GABAC antagonist

Biological Activity

A selective, competitive GABA C antagonist with only minimal effects on GABA A and GABA B receptors (K b values are 2.1 μ M (antagonist), 320 μ M (antagonist) and EC 50 ~ 500 μ M (weak agonist) respectively). Displays 8-fold selectivity for human recombinant ρ 1 receptors over ρ 2 receptors.

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.

storage

Store at RT

Properties of (1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID

Melting point: 252-254°
Boiling point: 417.2±45.0 °C(Predicted)
Density  1.20±0.1 g/cm3(Predicted)
storage temp.  Store at RT
solubility  H2O: 16 mg/mL
form  solid
pka 1.97±0.20(Predicted)
color  white or off-white
Water Solubility  Soluble to 100 mM in water

Safety information for (1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID

Computed Descriptors for (1,2,5,6-TETRAHYDROPYRIDIN-4-YL)METHYLPHOSPHINIC ACID

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