2-Aminoethyl Diphenylborinate Blocks GABAA-Receptor-Mediated Currents in Rat Medial Preoptic Neurons
2016 (English)In: Opera Medica Et Physiologica, ISSN 2500-2295, Vol. 2, no 1, 63-68 p.Article in journal (Refereed) Published
The effect of 2-aminoethyl diphenylborinate (2-APB), a commonly used drug to modulate inositol-1,4,5-triphosphate (IP3) receptors and transient receptor potential (TRP) channels, on GABAA receptor-mediatedcurrents was studied in neurons from the medial preoptic nucleus (MPN) of rat. 2-APB gradually and reversibly reducedthe currents evoked by GABA but had no effect on the currents evoked by glycine. The blocking effect was not mediatedby alterations in intracellular calcium concentration and showed a concentration dependence with half maximal effect at~50 μM 2-APB, for currents evoked by 100 μM, as well as by 1.0 mM GABA, suggesting that 2-APB is not competing withGABA for its binding site at the GABAA receptor. Thus, the present study describes a novel pharmacological property of2-APB as a non-competitive blocker of GABAA receptors and calls for caution in the interpretation of the results where2-APB is used to affect IP3 receptors or TRP channels.
Place, publisher, year, edition, pages
2016. Vol. 2, no 1, 63-68 p.
IdentifiersURN: urn:nbn:se:umu:diva-133366OAI: oai:DiVA.org:umu-133366DiVA: diva2:1087445