Loreclezole as a simple functional marker for homomeric rho type GABA(C) receptors.
GABA(C) receptors are expressed in the whole brain, but predominantly in the retina. They can be identified by their unique pharmacology. The establishment of the entire pharmacology is, however, quite tedious. We show here that loreclezole dose dependently inhibits ionic currents elicited by GABA (gamma-aminobutyric acid) with an IC(50) of about 0.5 microM in homomeric rho1 GABA(C) receptors expressed in Xenopus oocytes. Thus, loreclezole may constitute a functional marker for these receptors.
Thomet
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Department of Pharmacology, University of Bern, Friedbuehlstr. 49, CH-3010, Bern, Switzerland.
Baur
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Dodd
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RH
Sigel
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D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D008564:Membrane Potentials / Q000187:drug effects / Q000502:physiology; D018079:Receptors, GABA / Q000187:drug effects* / Q000502:physiology; D018080:Receptors, GABA-B; D014230:Triazoles / Q000494:pharmacology*; D014981:Xenopus; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D000927:Anticonvulsants; D018079:Receptors, GABA; D018080:Receptors, GABA-B; D014230:Triazoles; D005680:gamma-Aminobutyric Acid; C066440:loreclezole