Activation of GABAρ1 receptors by glycine and β-alanine

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Abstract
Neurons of the vertebrate retina possess receptors for many neurotransmitters. Particularly interesting is a new type of GABA receptor (GABAρ) that, in contrast to GABAA and GABAB receptors, shows very little desensitization, is not blocked by bicuculline, and is not activated by baclofen. Homomeric human GABAρ1 receptors were expressed inXenopusoocytes. In addition to GABA, and related agonists, GABAρ1 receptors respond to glycine (Gly) and β-alanine (β-Ala) by generating Cl- currents that do not desensitize and are resistant to bicuculline. The half-maximal concentrations for Gly and β-Ala currents were 14.2 ± 1.3 mM and 0.66 ± 0.11 mM respectively. The current responses to Gly and β-Ala were blocked by picrotoxin and TBPS. The cross-sensitivity of GABAρ1 receptors to Gly and β-Ala may play a role in retinal physiology.

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