Chiara Ruzza
YOU?
Author Swipe
Synthesis and Pharmacological Characterization of Nociceptin/Orphanin FQ Dimeric Ligands Open
The neuropeptide nociceptin/orphanin FQ (N/OFQ) plays a key role in regulating several physiological functions and pathological states, which makes its receptor (NOP) a promising target for therapeutic interventions. In this study, we synt…
Activation of peripheral NOP receptors reduces periorbital mechanical allodynia evoked by CGRP in mice Open
Background and Purpose Migraine is a neurovascular disorder largely mediated by calcitonin gene‐related peptide (CGRP). This study explores the role of the nociceptin/orphanin FQ (N/OFQ)–N/OFQ receptor (NOP) system in CGRP‐induced periorbi…
View article: Sex differences in response to NLRP3 inflammasome blockage in a mouse migraine model: A genetic and pharmacological study
Sex differences in response to NLRP3 inflammasome blockage in a mouse migraine model: A genetic and pharmacological study Open
Migraine is a common disorder that affects more than a billion of people worldwide, with an incidence in women three times higher than in men. The medical need for new therapeutic treatments is only partially satisfied by innovative approa…
View article: In vitro pharmacological evaluation of the novel NOP receptor partial agonist sunobinop
In vitro pharmacological evaluation of the novel NOP receptor partial agonist sunobinop Open
Sleep-related disorders affect a significant portion of the global population. The nociceptin/orphanin FQ (N/OFQ) peptide (NOP) receptor has become a promising candidate for the development of innovative drugs to treat sleep disorders. In …
View article: Identification of isoxazole-based TRPA1 inhibitors with analgesic effects in vivo
Identification of isoxazole-based TRPA1 inhibitors with analgesic effects in vivo Open
The transient receptor potential ankyrin 1 (TRPA1) channel has been extensively studied as a potential therapeutic target for the treatment of different pain types, with better efficacy and safety profiles compared to current therapies. Be…
Effects of Stress Exposure to Pain Perception in Pre-Clinical Studies: Focus on the Nociceptin/Orphanin FQ–NOP Receptor System Open
Exposure to physical and psychological stress modulates pain transmission in a dual manner. Stress-induced analgesia (SIA) refers to the reduction in pain sensitivity that can occur in response to acute stress. On the contrary, chronic str…
In vitro pharmacological characterization of growth hormone secretagogue receptor ligands using the dynamic mass redistribution and calcium mobilization assays Open
Ghrelin modulates several biological functions via selective activation of the growth hormone secretagogue receptor (GHSR). GHSR agonists may be useful for the treatment of anorexia and cachexia, while antagonists and inverse agonists may …
View article: Lack of Direct Effects of Neurotrophic Factors in an In Vitro Model of Neuroinflammation
Lack of Direct Effects of Neurotrophic Factors in an In Vitro Model of Neuroinflammation Open
Neuroinflammation is associated with several neurological disorders including temporal lobe epilepsy. Seizures themselves can induce neuroinflammation. In an in vivo model of epilepsy, the supplementation of brain-derived neurotropic facto…
In vitro pharmacological characterization of standard and new lysophosphatidic acid receptor antagonists using dynamic mass redistribution assay Open
Lysophosphatidic acid (LPA) is a bioactive phospholipid that acts as an agonist of six G protein-coupled receptors named LPA receptors (LPA 1-6 ). LPA elicits diverse intracellular events and modulates several biological functions, includi…
Preclinical effects of cannabidiol in an experimental model of migraine Open
Migraine is a disabling disorder characterized by recurrent headaches, accompanied by abnormal sensory sensitivity and anxiety. Despite extensive historical use of cannabis in headache disorders, there is limited research on the nonpsychoa…
View article: Neuropeptide S receptor in GtoPdb v.2023.1
Neuropeptide S receptor in GtoPdb v.2023.1 Open
The neuropeptide S receptor (NPS receptor) responds to the 20 amino-acid peptide neuropeptide S derived from a precursor (NPS, P0C0P6). NPS activates its receptor at low nanomolar concentrations elevating intracellular cAMP and calcium lev…
Synthesis, Biological Activity and Molecular Docking of Chimeric Peptides Targeting Opioid and NOP Receptors Open
Recently, mixed opioid/NOP agonists came to the spotlight for their favorable functional profiles and promising outcomes in clinical trials as novel analgesics. This study reports on two novel chimeric peptides incorporating the fragment T…
Pharmacology of Kappa Opioid Receptors: Novel Assays and Ligands Open
The present study investigated the in vitro pharmacology of the human kappa opioid receptor using multiple assays, including calcium mobilization in cells expressing chimeric G proteins, the dynamic mass redistribution (DMR) label-free ass…
View article: Neuropeptide S receptor in GtoPdb v.2021.3
Neuropeptide S receptor in GtoPdb v.2021.3 Open
The neuropeptide S receptor (NPS, provisional nomenclature [23]) responds to the 20 amino-acid peptide neuropeptide S derived from a precursor (NPS, P0C0P6).
Novel Mixed NOP/Opioid Receptor Peptide Agonists Open
The nociceptin/orphanin FQ (N/OFQ)/N/OFQ receptor (NOP) system controls different biological functions including pain and cough reflex. Mixed NOP/opioid receptor agonists elicit similar effects to strong opioids but with reduced side effec…
View article: Pharmacology, Physiology and Genetics of the Neuropeptide S System
Pharmacology, Physiology and Genetics of the Neuropeptide S System Open
The Neuropeptide S (NPS) system is a rather ‘young’ transmitter system that was discovered and functionally described less than 20 years ago. This review highlights the progress that has been made in elucidating its pharmacology, anatomica…
Functional Selectivity Does Not Predict Antinociceptive/Locomotor Impairing Potencies of NOP Receptor Agonists Open
Nociceptin/orphanin FQ controls several functions, including pain transmission, via stimulation of the N/OFQ peptide (NOP) receptor. Here we tested the hypothesis that NOP biased agonism may be instrumental for identifying innovative analg…
View article: Structure–Activity Relationship Studies on Oxazolo[3,4-<i>a</i>]pyrazine Derivatives Leading to the Discovery of a Novel Neuropeptide S Receptor Antagonist with Potent <i>In Vivo</i> Activity
Structure–Activity Relationship Studies on Oxazolo[3,4-<i>a</i>]pyrazine Derivatives Leading to the Discovery of a Novel Neuropeptide S Receptor Antagonist with Potent <i>In Vivo</i> Activity Open
Neuropeptide S modulates important neurobiological functions including locomotion, anxiety, and drug abuse through interaction with its G protein-coupled receptor known as neuropeptide S receptor (NPSR). NPSR antagonists are potentially us…
Biased Agonism at Nociceptin/Orphanin FQ Receptors: A Structure Activity Study on N/OFQ(1–13)-NH<sub>2</sub> Open
Nociceptin/orphanin FQ (N/OFQ) controls different biological functions via selective stimulation of the N/OFQ peptide (NOP) receptor. The pleiotropic actions of N/OFQ may limit the development of NOP ligands as innovative drugs in differen…
Biased versus Partial Agonism in the Search for Safer Opioid Analgesics Open
Opioids such as morphine—acting at the mu opioid receptor—are the mainstay for treatment of moderate to severe pain and have good efficacy in these indications. However, these drugs produce a plethora of unwanted adverse effects including …
Synthesis and Pharmacological Evaluation of Hybrids Targeting Opioid and Neurokinin Receptors Open
Morphine, which acts through opioid receptors, is one of the most efficient analgesics for the alleviation of severe pain. However, its usefulness is limited by serious side effects, including analgesic tolerance, constipation, and depende…
View article: Neuropeptide S receptor (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
Neuropeptide S receptor (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database Open
The neuropeptide S receptor (NPS, provisional nomenclature [18]) responds to the 20 amino-acid peptide neuropeptide S derived from a precursor (NPS, P0C0P6).
Tetrabranched Hetero-Conjugated Peptides as Bifunctional Agonists of the NOP and Mu Opioid Receptors Open
The general aim of the work was the validation of a new synthetic methodology designed for obtaining bifunctional heterotetrabranched peptide ligands. Applying an easily accessible synthetic route, we provided a small series of heteromulti…
Modulation of the NOP receptor signaling affects resilience to acute stress Open
Background: The peptide nociceptin/orphanin FQ (N/OFQ) and its receptor (NOP) are implicated in the modulation of emotional states. Previous human and rodent findings support NOP antagonists as antidepressants. However, the role played by …
Dopamine D1 and D2 receptors mediate neuropeptide S-induced antinociception in the mouse formalin test Open
Neuropeptide S (NPS) is the endogenous ligand of a G-protein coupled receptor named NPS receptor. The NPS system controls several biological functions, including anxiety, wakefulness, locomotor activity, food intake, and pain transmission.…
NOP agonist action of cebranopadol counteracts its liability to promote physical dependence Open
Cebranopadol is a mixed NOP/opioid receptor agonist currently under development as innovative analgesic. In this study the liability of cebranopadol to produce opioid-type physical dependence has been evaluated in comparison with morphine …