182485-36-5

182485-36-5 structure

Name: TPMPA
Chemical Name: (1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid hydrate
CAS Number: 182485-36-5
Molecular Formula: C₆H₁₂NO₂P
Molecular Weight: 161.13900
Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
Create Date: 2018-12-24 12:10:04
Modify Date: 2024-01-10 03:21:05
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].

Name	(1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinic acid hydrate
Synonyms	(1,2,5,6-Tetrahydropyridin-4-yl)methylphosphinicacid TPMPA hydrate TPMPA

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.

WGK Germany	3