beta-Funaltrexamine inactivates ORL1 receptors in BE(2)-C human neuroblastoma cells.
The potential interactions of natively expressed mu-opioid and opioid receptor-like (ORL1) receptors were studied by exposing intact BE(2)-C cells to agonists or antagonists for 1 h. Pretreatment with the mu-opioid receptor agonist, [D-Ala(2), N-Me-Phe(4),Gly(5)-ol]enkephalin (DAMGO), or the ORL1 receptor agonist, orphanin FQ/nociceptin desensitized both mu-opioid and ORL1 receptor responses. beta-Funaltrexamine (beta-FNA) pretreatment also blocked both mu-opioid and ORL1 receptor responses, but only mu-opioid receptor binding was reduced. Moreover, beta-FNA (1 microM) failed to inhibit specific ORL1 receptor binding.
Mandyam
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CD
Department of Pharmacological and Pharmaceutical Sciences, University of Houston, 77204-5515, Houston, TX 77204-5515, USA.
Altememi
G F
GF
Standifer
K M
KM
D001932:Brain Neoplasms / Q000378:metabolism*; D000242:Cyclic AMP / Q000378:metabolism; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)- / Q000378:metabolism; D006801:Humans; D009020:Morphine / Q000494:pharmacology; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology*; D009294:Narcotics / Q000494:pharmacology; D009447:Neuroblastoma / Q000378:metabolism*; D018847:Opioid Peptides / Q000494:pharmacology; D011957:Receptors, Opioid / Q000819:agonists; D017450:Receptors, Opioid, mu / Q000037:antagonists & inhibitors; D014407:Tumor Cells, Cultured; D000094942:Nociceptin Receptor; D000097629:Nociceptin
D000242:Cyclic AMP; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D009020:Morphine; D009271:Naltrexone; D009292:Narcotic Antagonists; D009294:Narcotics; D018847:Opioid Peptides; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; D000094942:Nociceptin Receptor; D000097629:Nociceptin; C024524:beta-funaltrexamine; C000722283:OPRL1 protein, human