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Pharmacological Profile Of Nociceptin/Orphanin Fq Receptors
Author(s) -
Calo’ Girolamo,
Rizzi Anna,
Bigoni Raffaella,
Guerrini Remo,
Salvadori Severo,
Regoli Domenico
Publication year - 2002
Publication title -
clinical and experimental pharmacology and physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.752
H-Index - 103
eISSN - 1440-1681
pISSN - 0305-1870
DOI - 10.1046/j.1440-1681.2002.03633.x
Subject(s) - nociceptin receptor , receptor , nop , peptide , chemistry , pharmacology , opioid peptide , opioid receptor , peptide receptor , opioid , biology , biochemistry
SUMMARY 1. Nociceptin/orphanin FQ (NC) and its receptor (OP 4 ) represent a novel peptide/receptor system pharmacologically distinct from classical opioid systems. 2. Via OP 4 receptor activation, NC regulates several biological functions, both at peripheral and central levels; therefore, the OP 4 receptor may be viewed as a novel target for drug development. However , the pharmacology of this receptor is still in its infancy, with few molecules interacting selectively with this receptor. 3. In the present article, we review the findings of studies that have investigated the pharmacological profile of ligands selective for the OP 4 receptor, these being two antagonists, the peptide [Nphe 1 ]NC(1–13)NH 2 and the non‐peptide J‐113397, and two agonists, the peptide [Arg 14 ,Lys 15 ]NC, and the non‐ peptide Ro 64‐6198. 4. The results of these studies indicate that agents that selectively activate or block the OP 4 receptor may represent new potential drugs for the treatment of human diseases.

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