Identification of opioid receptor-like (ORL1) peptide-stimulated [35S]GTP gamma S binding in rat brain.
Recent reports have identified an endogenous peptide ligand for the opioid receptor-like (ORL1) receptor. In the present study, ORL1 peptide-stimulated [35>]GTP gamma S binding was assessed in rat cortical membranes and brain sections to localize ORL1 receptor-activated G-proteins. In membrane assays, with 20 microM GDP, ORL1 peptide stimulated [35S]GTP gamma S binding by approximately two-fold with an ED50 value of 20 nM. ORL1 peptide-stimulated [35S]GTP gamma S binding was unaffected by opioid or other G-protein-coupled receptor antagonists. In brain sections, ORL1 peptide-stimulated [35S]GTP gamma S binding was identified in regions including cortex, amygdala, hypothalamus, thalamus and brain stem. The anatomical distribution of ORL1 peptide-stimulated [35S]GTP gamma S binding suggests its involvement in cognition, emotion and homeostasis.
Sim
L J
LJ
Department of Physiology and Pharmacology, Bowman Gray School of Medicine, Wake Forest University, Winston-Salem, NC 27157, USA.
Xiao
R
R
Childers
S R
SR
D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000033:anatomy & histology / Q000187:drug effects / Q000378:metabolism*; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D004745:Enkephalins / Q000494:pharmacology; D019204:GTP-Binding Proteins / Q000378:metabolism*; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism*; D008297:Male; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D011957:Receptors, Opioid / Q000378:metabolism*; D013462:Sulfur Radioisotopes; D000094942:Nociceptin Receptor
D000700:Analgesics; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D004745:Enkephalins; D019204:GTP-Binding Proteins; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D011957:Receptors, Opioid; D013462:Sulfur Radioisotopes; D000094942:Nociceptin Receptor; C000722285:Oprl1 protein, rat