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Pharmacology of nociceptin and its receptor: a novel therapeutic target
- G. Calo’, R. Guerrini, A. Rizzi, S. Salvadori, D. Regoli
- BiologyBritish journal of pharmacology
- 1 April 2000
New advances have contributed to better understanding of the pathophysiological role of the NC/OP4 system, and ultimately will help to identify the therapeutic potential of new OP4 receptor ligands.
Structure of the Nociceptin/Orphanin FQ Receptor in Complex with a Peptide Mimetic
The crystal structure of human NOP is reported, solved in complex with the peptide mimetic antagonist compound-24 (C-24), revealing atomic details of ligand–receptor recognition and selectivity and providing a new structural template for the design of NOP ligands.
Neuropeptide S is a stimulatory anxiolytic agent: a behavioural study in mice
The effects of in vivo supraspinal NPS in mice are evaluated and it is shown that in vivo NPS produces a unique behavioural profile by increasing wakefulness and exerting anxiolytic‐like effects.
Antidepressant-like effects of the nociceptin/orphanin FQ receptor antagonist UFP-101: new evidence from rats and mice
- E. Gavioli, C. Vaughan, G. Calo’
- Biology, PsychologyNaunyn-Schmiedeberg's Archives of Pharmacology
- 25 May 2004
UFP-101 exhibits pronounced antidepressant-like effects in different species and animal models, possibly by preventing the inhibitory effects of endogenous N/OFQ on brain monoaminergic (in particular serotonergic) neurotransmission.
Blockade of nociceptin/orphanin FQ–NOP receptor signalling produces antidepressant‐like effects: pharmacological and genetic evidences from the mouse forced swimming test
Results indicate that blockade of the N/OFQ‐NOP receptor signalling in the brain produces antidepressant‐like effects in the mouse FST, and support the NOP receptor as a candidate target for the development of innovative antidepressant drugs.
A new selective antagonist of the nociceptin receptor
The present findings indicate that [Phe1Ψ(CH2‐NH)Gly2]NC(1‐13)NH2 is a selective antagonist of the nociceptin receptor.
Characterization of [Nphe1]nociceptin(1‐13)NH2, a new selective nociceptin receptor antagonist
The novel peptide [Nphe1]nociceptin(1‐13)NH2 acts as the first truly selective and competitive nociceptide receptor antagonist and is devoid of any residual agonist activity, indicating that it may be the prototype of a new class of analgesics.
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.
Pharmacological Characterization of the Nociceptin/Orphanin FQ Receptor Antagonist SB-612111…
- A. Rizzi, E. Gavioli, G. Calo’
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 June 2007
It is demonstrated that SB-612111 behaves in vivo as a potent and selective NOP antagonist and suggest that the N/OFQ-NOP receptor endogenous system plays an important role in regulating mood-related behaviors.
Address and message sequences for the nociceptin receptor: a structure-activity study of nociceptin-(1-13)-peptide amide.
It is indicated that the structural requirements of NC for occupation and activation of its receptor are different from that of opioids, particularly delta agonists.