title: Synthesis and biological activity of small peptides as NOP and opioid receptors' ligands: view on current developments.
abstract: The heptadecapeptide nociceptin, also called orphanin FQ (N/OFQ), is the endogenous agonist of the N/OFQ peptide receptor (NOP receptor) and is involved in several central nervous system pathways, such as nociception, reward, tolerance, and feeding. The discovery of small molecule ligands for NOP is being actively pursued for several therapeutic applications. This review presents overview of the several recently reported NOP ligands (agonists and antagonists), with an emphasis of the structural features that may be important for modulating the intrinsic activity of these ligands. In addition, a brief account on the characterization of newly synthesized ligands of NOP receptor with aminophosphonate moiety and β-tryptophan analogues will be presented.
authors: Department of Organic Chemistry, University of Chemical Technology and Metallurgy, Sofia, Bulgaria. Electronic address: e_naydenova@abv.bg.
authors: Emilia
authors: E
authors: Naydenova
authors: Department of Organic Chemistry, University of Chemical Technology and Metallurgy, Sofia, Bulgaria.
authors: Petar
authors: P
authors: Todorov
authors: Institute of Neurobiology, Bulgarian Academy of Sciences, Sofia, Bulgaria.
authors: Rositza
authors: R
authors: Zamfirova
mesh_terms: D000701:Analgesics, Opioid / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D015195:Drug Design; D015507:Drugs, Investigational / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D009292:Narcotic Antagonists / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D009419:Nerve Tissue Proteins / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*; D009474:Neurons / Q000187:drug effects* / Q000378:metabolism; D009842:Oligopeptides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D018847:Opioid Peptides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D010455:Peptides / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000819:agonists / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000737:chemistry / Q000378:metabolism; D000094942:Nociceptin Receptor; D000097629:Nociceptin
chemical_list: D000701:Analgesics, Opioid; D015507:Drugs, Investigational; D008024:Ligands; D009292:Narcotic Antagonists; D009419:Nerve Tissue Proteins; D009842:Oligopeptides; D018847:Opioid Peptides; D010455:Peptides; D011957:Receptors, Opioid; D011994:Recombinant Proteins; D000094942:Nociceptin Receptor; D000097629:Nociceptin; C000722283:OPRL1 protein, human
keywords: Agonist; Analgesic effects; Antagonist; Hexapeptide analogues; NOP receptor; Nociceptin analogues; Nociceptin/orphanin FQ; Opioid peptides; SPPS