Pharmacological characterization and tissue distribution of the human and rat GALR1 receptors.
The diverse biological functions of galanin are mediated via membrane bound high-affinity receptors. In order to identify and characterize potential galanin receptor subtypes, we have examined the specific 125I-galanin binding to the CHP-212 human neuroblastoma cell line. The galanin receptors expressed in CHP-212 cells, like GALR1 have high affinity for galanin (Kd = 0.07 nM) and the potency for inhibition of 125I-galanin binding by galanin peptides parallels that of hGALR1 expressed in a stable CHO cell line. We confirmed that GALR1 is expressed in these cells by RT-PCR. We further determined the tissue expression patterns of hGALR1 which is expressed in a variety of human tissues at a very low level, with the highest levels seen in heart, small intestine and prostate. A species of approximately 70 kDa is recognized by antisera specific for hGALR1 by Western blot analysis and should allow future measurements of receptor protein expression.
Sullivan
K A
KA
Department of Molecular Pharmacology and Biochemistry, Merck Research Laboratories, Rahway, New Jersey 07065-0900, USA. kathleen_sullivan@merck.com
Shiao
L L
LL
Cascieri
M A
MA
D000595:Amino Acid Sequence; D000818:Animals; D001483:Base Sequence; D016466:CHO Cells; D019556:COS Cells; D006224:Cricetinae; D017931:DNA Primers / Q000235:genetics; D005260:Female; D019004:Galanin / Q000378:metabolism*; D006801:Humans; D007457:Iodine Radioisotopes; D007700:Kinetics; D008297:Male; D008969:Molecular Sequence Data; D008970:Molecular Weight; D016133:Polymerase Chain Reaction; D051381:Rats; D044088:Receptors, Galanin; D011964:Receptors, Gastrointestinal Hormone / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D014018:Tissue Distribution; D014407:Tumor Cells, Cultured
D017931:DNA Primers; D007457:Iodine Radioisotopes; D044088:Receptors, Galanin; D011964:Receptors, Gastrointestinal Hormone; D019004:Galanin