TPMPA

Names

[ Name ]:
TPMPA

[Synonym ]:
(1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinicacid
TPMPA hydrate
TPMPA

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

KB: 2.1 μM (GABAC)

[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]

[References]

[1]. Martínez-Torres A, et al. GABArho 1/GABAAalpha 1 receptor chimeras to study receptor desensitization. Proc Natl Acad Sci U S A. 2000;97(7):3562-3566.

[2]. Graham A. R. Johnston, et al. Neurologically-active compounds. WO1998058939A1

[3]. Johnston GA. GABAc receptors: relatively simple transmitter -gated ion channels?. Trends Pharmacol Sci. 1996;17(9):319-323.

Chemical & Physical Properties

[ Molecular Formula ]:
C₆H₁₂NO₂P

[ Molecular Weight ]:
161.13900

[ Exact Mass ]:
161.06100

[ PSA ]:
59.14000

[ LogP ]:
1.09260

Safety Information

[ WGK Germany ]:
3

Related Compounds

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