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J Biol Chem, Vol. 273, Issue 36, 23321-23326, September 4, 1998

Cloned Human and Rat Galanin GALR3 Receptors
PHARMACOLOGY AND ACTIVATION OF G-PROTEIN INWARDLY RECTIFYING K⁺ CHANNELS

From the Departments of Molecular Biology and Pharmacology, Synaptic Pharmaceutical Corporation, Paramus, New Jersey 07652

The neuropeptide galanin has been implicated in the regulation of processes such as nociception, cognition, feeding behavior, and hormone secretion. Multiple galanin receptors are predicted to mediate its effects, but only two functionally coupled receptors have been reported. We now report the cloning of a third galanin receptor distinct from GALR1 and GALR2. The receptor, termed GALR3, was isolated from a rat hypothalamus cDNA library by both expression and homology cloning approaches. The rat GALR3 receptor cDNA can encode a protein of 370 amino acids with 35% and 52% identity to GALR1 and GALR2, respectively. Localization of mRNA by solution hybridization/RNase protection demonstrates that the GALR3 transcript is widely distributed, but expressed at low abundance, with the highest levels in the hypothalamus and pituitary. We also isolated the gene encoding the human homologue of GALR3. The human GALR3 receptor is 90% identical to rat GALR3 and contains 368 amino acids. Binding of porcine ¹²⁵I-galanin to stably expressed rat and human GALR3 receptors is saturable (rat K_D = 0.98 nM and human K_D = 2.23 nM) and displaceable by galanin peptides and analogues in the following rank order: rat galanin, porcine galanin  M32, M35  porcine galanin-(7 to +29), galantide, human galanin > M40, galanin-(1-16) > [D-Trp²]galanin-(1-29), galanin-(3-29)_. This profile resembles that of the rat GALR1 and GALR2 receptors with the notable exception that human galanin, galanin-(1-16), and M40 show lower affinity at GALR3. In Xenopus oocytes, activation of rat and human GALR3 receptors co-expressed with potassium channel subunits GIRK1 and GIRK4 resulted in inward K⁺ currents characteristic of G_i/G_o-coupled receptors. These data confirm the functional efficacy of GALR3 receptors and further suggest that GALR3 signaling pathways resemble those of GALR1 in that both can activate potassium channels linked to the regulation of neurotransmitter release.

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