Designing bifunctional NOP receptor–mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.
نویسندگان
چکیده
منابع مشابه
Structural determinants of opioid and NOP receptor activity in derivatives of buprenorphine.
The unique pharmacological profile of buprenorphine has led to its considerable success as an analgesic and as a treatment agent for drug abuse. Activation of nociceptin/orphanin FQ peptide (NOP) receptors has been postulated to account for certain aspects of buprenorphine's behavioral profile. In order to investigate the role of NOP activation further, a series of buprenorphine analogues has b...
متن کاملStructure-Based Virtual Screening of the Nociceptin Receptor: Hybrid Docking and Shape-Based Approaches for Improved Hit Identification
The antagonist-bound crystal structure of the nociceptin receptor (NOP), from the opioid receptor family, was recently reported along with those of the other opioid receptors bound to opioid antagonists. We recently reported the first homology model of the 'active-state' of the NOP receptor, which when docked with 'agonist' ligands showed differences in the TM helices and residues, consistent w...
متن کاملNOP Receptor Ligands as Potential Agents for Inflammatory and Autoimmune Diseases
Nociceptin/orphanin FQ (N/OFQ) is a seventeen-amino acid peptide that is the endogenous ligand of a G-protein-coupled receptor (NOP). Various immune cells express the precursor protein and secrete N/OFQ as well as display binding sites for this peptide. The functional capacity of NOP receptor was demonstrated in vitro and in vivo studies by the ability of N/OFQ to induce chemotaxis of immune ce...
متن کاملFrom models to molecules: opioid receptor dimers, bivalent ligands, and selective opioid receptor probes.
Opiates have been the most widely investigated class of natural products.1 The two most prominent opiates, morphine and codeine, have had a long history of use and abuse. Numerous semisynthetic opiates have been synthesized in an effort to obtain analgesics that are free of tolerance, physical dependence, and addiction liability. The development of totally synthetic analgesics subsequently led ...
متن کاملNociceptin Opioid Receptor (NOP) as a Therapeutic Target: Progress in Translation from Preclinical Research to Clinical Utility.
In the two decades since the discovery of the nociceptin opioid receptor (NOP) and its ligand, nociceptin/orphaninFQ (N/OFQ), steady progress has been achieved in understanding the pharmacology of this fourth opioid receptor/peptide system, aided by genetic and pharmacologic approaches. This research spawned an explosion of small-molecule NOP receptor ligands from discovery programs in major ph...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2013
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2013.03.101