Search Results - "Trapella, C"
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JWH-018 impairs sensorimotor functions in mice
Published in Neuroscience (06-08-2015)“…Highlights • JWH-018 impairs sensorimotor responses in mice by stimulation of CB1 receptors. • JWH-018 reduces more powerfully than Δ9 -THC sensorimotor…”
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Novel halogenated derivates of JWH-018: Behavioral and binding studies in mice
Published in Neuropharmacology (01-08-2015)“…JWH-018 is a synthetic CB1 and CB2 agonist illegally marketed as products named “Spice” or “herbal blend” for its psychoactive effects which are much higher…”
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Pharmacological Profile of Nociceptin/Orphanin FQ Receptors Interacting with G-Proteins and β-Arrestins 2
Published in PloS one (06-08-2015)“…Nociceptin/orphanin FQ (N/OFQ) controls several biological functions by selectively activating an opioid like receptor named N/OFQ peptide receptor (NOP)…”
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Antinociceptive action of NOP and opioid receptor agonists in the mouse orofacial formalin test
Published in Peptides (New York, N.Y. : 1980) (01-08-2017)“…•Nociceptin/orphanin FQ (N/OFQ) modulates several biological functions, including pain.•NOP(-/-) mice displayed a pronociceptive phenotype in the orofacial…”
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Synthetic cannabinoid JWH-018 and its halogenated derivatives JWH-018-Cl and JWH-018-Br impair Novel Object Recognition in mice: Behavioral, electrophysiological and neurochemical evidence
Published in Neuropharmacology (01-10-2016)“…It is well known that an impairment of learning and memory function is one of the major physiological effects caused by natural or synthetic cannabinoid…”
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New TRAP1 and Hsp90 chaperone inhibitors with cationic components: Preliminary studies on mitochondrial targeting
Published in Bioorganic & medicinal chemistry letters (15-07-2018)“…[Display omitted] •Analogues of known Hsp90 inhibitors with a permanent or ionizable cationic head.•Inhibition of TRAP1 ATPase activity and detection in…”
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Development and characterisation of novel fentanyl-delta opioid receptor antagonist based bivalent ligands
Published in British journal of anaesthesia : BJA (01-04-2015)“…Opioid tolerance is a limiting factor in chronic pain. Delta opioid peptide (DOP)(δ) receptor antagonism has been shown to reduce tolerance. Here, the common…”
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C subunit of F1/FO-ATP synthase as target for preventing the detrimental effect of myocardial ischemia/reperfusion injury
Published in Vascular pharmacology (01-04-2018)“…Objective: The pathophysiological effects of coronary heart diseases are imputable to the hurtful consequences of ischemia-reperfusion injury (IRI).The opening…”
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Nocistatin inhibits 5‐hydroxytryptamine release in the mouse neocortex via presynaptic G i/o protein linked pathways
Published in British journal of pharmacology (29-01-2009)“…Background and purpose: Nocistatin (NST) is a neuropeptide generated from cleavage of the nociceptin/orphanin FQ (N/OFQ) precursor. Evidence has been presented…”
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In vitro and in vivo pharmacological characterization of the novel neuropeptide S receptor ligands QA1 and PI1
Published in Peptides (New York, N.Y. : 1980) (01-10-2013)“…•The in vitro and in vivo pharmacological profile of novel NPSR ligands was assessed.•In vitro QA1 and PI1 behaved as pure and potent NPSR antagonists.•In…”
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Nocistatin inhibits 5‐hydroxytryptamine release in the mouse neocortex via presynaptic Gi/o protein linked pathways
Published in British journal of pharmacology (01-10-2007)“…Background and purpose: Nocistatin (NST) is a neuropeptide generated from cleavage of the nociceptin/orphanin FQ (N/OFQ) precursor. Evidence has been presented…”
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Synthesis and biological evaluation of new vinyl ester pseudotripeptide proteasome inhibitors
Published in European journal of medicinal chemistry (01-08-2006)“…Here we report the synthesis and biological activities of new tripeptidic-based vinyl ester derivative proteasome inhibitors. Starting from Hmb-Val-Ser-Leu-VE…”
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Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist
Published in Bioorganic & medicinal chemistry (01-02-2006)“…The compound coded as Trap-101 is an achiral analogue of the nociceptin/orphanin FQ receptor antagonist J-113397 that combines a pharmacological profile…”
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HIV protease inhibitors: synthesis and activity of N-aryl- N′-hydroxyalkyl hydrazide pseudopeptides
Published in European journal of medicinal chemistry (01-05-2005)“…We describe the synthesis and activities of a series of pseudopeptides containing an N-aryl- N′-hydroxyalkyl hydrazide core structure to inhibit human…”
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NOP receptor pharmacological profile - A dynamic mass redistribution study
Published in PloS one (30-08-2018)“…The Nociceptin/Orphanin FQ (N/OFQ) peptide NOP receptor is coupled to pertussis toxin (PTX)-sensitive G proteins (Gi/o) whose activation leads to the…”
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Tryptophan replacement in the nociceptin/orphanin FQ receptor ligand Ac-RYYRWK-NH2
Published in The journal of peptide research (01-07-2005)“…: In the present study we describe the in vitro pharmacological characterization of the nociceptin/orphanin FQ (N/OFQ) receptor (NOP) ligand Ac‐RYYRWK‐NH2 and…”
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Nonpeptide/peptide chimeric ligands for the nociceptin/orphanin FQ receptor: design, synthesis and in vitro pharmacological activity
Published in The journal of peptide research (01-06-2004)“…: Nociceptin/orphanin FQ (N/OFQ) is the endogenous ligand for the G‐protein coupled receptor referred to as N/OFQ peptide (NOP) receptor. NOP receptor…”
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The Nociceptin/Orphanin FQ Receptor Antagonist J-113397 and L-DOPA Additively Attenuate Experimental Parkinsonism through Overinhibition of the Nigrothalamic Pathway
Published in The Journal of neuroscience (07-02-2007)“…By using a battery of behavioral tests, we showed that nociceptin/orphanin FQ receptor (NOP receptor) antagonists attenuated parkinsonian-like symptoms in…”
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A novel and facile synthesis of tetra branched derivatives of nociceptin/orphanin FQ
Published in Bioorganic & medicinal chemistry (15-07-2014)“…Branched peptides have been found to be useful in several research fields however their synthesis and purification is complicated. Here we present a novel and…”
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