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Fifteen hexapeptides having high affinity for the opioid-like receptor ORL1 were identified from a combinatorial library containing more than 52 million different hexapeptides. The five compounds with the highest affinity were characterized further by use of a variety of in vitro models. Binding studies indicated that these five peptides have affinity for(More)
BACKGROUND AND PURPOSE Compounds that activate both NOP and mu-opioid receptors might be useful as analgesics and drug abuse medications. Studies were carried out to better understand the biological activity of such compounds. EXPERIMENTAL APPROACH Binding affinities were determined on membranes from cells transfected with NOP and opioid receptors.(More)
Nociceptin/orphanin FQ (N/OFQ) was recently identified as the endogenous ligand for the opioid-receptor like (ORL1) receptor. Although the ORL1 receptor shows sequence homology with the opioid receptors, the nociceptin/ORL1 ligand-receptor system has very distinct pharmacological actions compared to the opioid receptor system. Recently, several(More)
The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. The full contents can be found at(More)
Doxorubicin (DXR) is an effective antitumor agent in a wide spectrum of neoplasms. Chronic treatment is associated with cardiomyopathy and characteristic myocardial ultrastructural changes, which include swelling of the t tubules. Accordingly, we investigated excitation-contraction coupling in cardiomyopathic rat heart resulting from chronic DXR treatment.(More)
Nociceptin (orphanin FQ) is an endogenous peptide agonist for the newly discovered receptor (opioid receptor-like 1 receptor, ORL1) that bears striking homology to opioid receptors. Initial reports claimed that this peptide had hypoalgesic effects following i.c.v. or i.t. administration. The present study demonstrates that, in the presence of opioid(More)
Pregnancy and its hormonal simulation via 17beta-estradiol (E(2)) and progesterone (P) are associated with spinal opioid antinociception, primarily driven by augmented dynorphin/kappa-opioid activity. This study addresses the ovarian sex steroid-activated mechanism(s) that underlie this activation using an ex vivo spinal cord preparation. In lumbar spinal(More)
Recent studies have identified compounds with reduced efficacy relative to nociceptin/orphanin FQ at the opioid-like receptor ORL1. Utilizing stimulation of [(35)S]GTPgammaS binding as in vitro assays, it was determined that both [Phe(1)psi(CH(2)-NH)Gly(2)]N/OFQ(1-13)NH(2) and the hexapeptide Ac-RYYRIK-NH(2) act as partial agonists in CHO cells transfected(More)
The delta-opioid receptor found in SH-SY5Y cells was characterized in terms of binding profile and ability to mediate the inhibition of forskolin-stimulated cAMP accumulation. Both DPDPE ([D-Pen2,D-Pen5]enkephalin) and deltorphin II, compounds reported to be selective for the delta 1- and delta 2-opioid receptor respectively, were potent agonists in these(More)