Cloning, pharmacological characterization, and anatomical distribution of a rat cDNA encoding for a galanin receptor

摘要: We have cloned and expressed a rat cDNA, designated GALR1-rat, that encodes galanin receptor based on homology, pharmacology, anatomical criteria. This cDNA was isolated from brain library. The nucleotide sequence of the revealed an open reading frame encoding 346-amino-acid protein, showing 90.8% identity with previously human receptor. Membranes prepared COS cells transiently expressing GALR1-rat specifically bind125I-galanin high affinity (K d=0.12±0.01 nM). Rat, porcine, were able to displace125I-galanin nanomolar Ki (0.08±0.03, 0.10±0.01, 0.14±0.03 nM, respectively), whereas values for porcine fragments galanin-(1–16), galanin-(2–29), galanin-(3–29) 0.95±0.21 7.14±0.51 >1 µM, respectively. rank order potency these ligands is consistent reported native distribution mRNA corresponding encoded by determined byin situ hybridization sections. High levels detected in ventral hippocampal formation, thalamic, amygdala, medulla oblongata nuclei, dorsal horn spinal cord.