Recent experiments have demonstrated that formation of functional type B gamma-aminobutyric acid (GABA B ) receptors requires co-expression of two receptor subunits, GABA B1 and GABA B2 . Despite the identification of these subunits and a number of associated splice variants, there has been little convincing evidence of pharmacological diversity between GABA B receptors comprising different subunit combinations. However, Ng et al. (Mol. Pharmacol., 59 (2000) 144) have recently suggested a novel and important pharmacological difference between GABA B receptor heterodimers expressing the GABA B1a and GABA B1b receptor subunits. This study suggested that the antiepileptic GABA analogue gabapentin (Neurontin) is an agonist at GABA B receptors expressing the GABA B1a but not the GABA B1b receptor subunit. The importance of this finding with respect to identifying novel GABA B receptor subunit specific agonists prompted us to repeat these experiments in our own ( 35 S )− GTPγS binding and second messenger assay systems. Here we report that gabapentin was completely inactive at recombinant GABA B heterodimers expressing either GABA B1a or GABA B1b receptor subunits in combination with GABA B2 receptor subunits. In addition, in both CA1 and CA3 pyramidal neurones from rodent hippocampal slices we were unable to demonstrate any agonist-like effects of gabapentin at either pre- or post-synaptic GABA B receptors. In contrast, gabapentin activated a GABA A receptor mediated chloride conductance. Our data suggest that gabapentin is not a GABA B -receptor agonist let alone a GABA B receptor subunit selective agonist.
Neuropharmacology – Elsevier
Published: Dec 1, 2001
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