Abstract
Our understanding of the role GABA C receptors play in the central nervous system is limited due to a lack of specific ligands. Here we describe the pharmacological effects of (±)- cis-3- and (±)- trans-3-(aminocyclopentyl)methylphosphinic acids ((±)- cis- and (±)- trans-3-ACPMPA) as novel ligands for the GABA C receptor showing little activity at GABA A or GABA B receptors. (±)- cis-3-ACPMPA has similar potency to (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA) at human recombinant ρ1 ( K B = 1.0 ± 0.2 μM) and rat ρ3 ( K B = 5.4 ± 0.8 μM) but is 15 times more potent than TPMPA on human recombinant ρ2 ( K B = 1.0 ± 0.3 μM) GABA C receptors expressed in Xenopus oocytes. (±)- cis- and (±)- trans-3-ACPMPA are novel lead compounds for developing into more potent and selective GABA C receptor antagonists with increased lipophilicity for in vivo studies.
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