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Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor
Data indicate that the newly discovered heptadecapeptide is an endogenous agonist of the ORL1 receptor and that it may be endowed with pro-nociceptive properties.
Standard binding and functional assays related to medications development division testing for potential cocaine and opiate narcotic treatment medications.
Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1.
- C. Dooley, C. Spaeth, L. Toll
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 November 1997
Binding studies indicated that these five peptides have affinity for ORL1 in the nanomolar range, similar to the recently discovered endogenous ligand called nociceptin and orphanin FQ (N/OFQ), which could enable them to bind to the negatively charged second extracellular loop thought to be a likely binding site for N/OF Q.
Sub-anesthetic concentrations of (R,S)-ketamine metabolites inhibit acetylcholine-evoked currents in α7 nicotinic acetylcholine receptors.
Nociceptin/Orphanin FQ Receptor Structure, Signaling, Ligands, Functions, and Interactions with Opioid Systems
How NOP pharmacology intersects, contrasts, and interacts with the mu opioid receptor in terms of tertiary structure and mechanism of receptor activation; location of receptors in the central nervous system; mechanisms of desensitization and downregulation; cellular actions; intracellular signal transduction pathways; and behavioral actions with respect to analgesia, tolerance, dependence, and reward is discussed.
Evolutionary Sequence Modeling for Discovery of Peptide Hormones
We describe a computational framework that models spatial structure along the genomic sequence simultaneously with the temporal evolutionary path structure and show how such models can be used to…
Challenges for opioid receptor nomenclature: IUPHAR Review 9
- B. Cox, M. Christie, L. Devi, L. Toll, J. Traynor
- BiologyBritish journal of pharmacology
- 1 January 2015
Presentations at the 2013 meeting of the International Narcotics Research Conference in Cairns, Australia, considered some of the new discoveries that are now unravelling the complexities of opioid receptor signalling.
Comparison of the Antinociceptive and Antirewarding Profiles of Novel Bifunctional Nociceptin Receptor/μ-Opioid Receptor Ligands: Implications for Therapeutic Applications
- L. Toll, T. Khroyan, W. Polgar, F. Jiang, C. Olsen, N. Zaveri
- Biology, PsychologyJournal of Pharmacology and Experimental…
- 1 December 2009
It is suggested that NOPr full-agonist activity is required to modulate opioid-induced reward, whereas a bifunctional Nopr/MOPr partial agonist profile may be suitable as a nonaddicting analgesic.
AT-1001: A High Affinity and Selective α3β4 Nicotinic Acetylcholine Receptor Antagonist Blocks Nicotine Self-Administration in Rats
The results suggest that its inhibition of nicotine self-administration in rats is not directly due to a decrease in dopamine release from the NAc, and most likely involves an indirect pathway requiring α3β4 nAChR.
Nociceptin/Orphanin FQ Receptor Activation Attenuates Antinociception Induced by Mixed Nociceptin/Orphanin FQ/μ-Opioid Receptor Agonists
- T. Khroyan, W. Polgar, F. Jiang, N. Zaveri, L. Toll
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 December 2009
The hypothesis that activation of NOP receptors can lead to attenuation of MOP receptor-mediated antinociception elicited by mixed NOP/MOP receptor compounds such as buprenorphine, SR16435, and SR16507 is supported.