Search Results - "Whiteside, Garth"
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Dynamic changes in the microRNA expression profile reveal multiple regulatory mechanisms in the spinal nerve ligation model of neuropathic pain
Published in PloS one (14-03-2011)“…Neuropathic pain resulting from nerve lesions or dysfunction represents one of the most challenging neurological diseases to treat. A better understanding of…”
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An industry perspective on the role and utility of animal models of pain in drug discovery
Published in Neuroscience letters (17-12-2013)“…•Evidence that new pain drug discovery failures are due to insufficient efficacy is poorly documented.•Discovery of new drugs requires data from many assays in…”
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Loss of Retrograde Endocannabinoid Signaling and Reduced Adult Neurogenesis in Diacylglycerol Lipase Knock-out Mice
Published in The Journal of neuroscience (10-02-2010)“…Endocannabinoids (eCBs) function as retrograde signaling molecules at synapses throughout the brain, regulate axonal growth and guidance during development,…”
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A randomized, double-blind, positive-controlled, 3-way cross-over human experimental pain study of a TRPV1 antagonist (V116517) in healthy volunteers and comparison with preclinical profile
Published in Pain (Amsterdam) (01-09-2016)“…This experimental, translational, experimental pain, single-center, randomized, double-blind, single-dose, 3-treatment, 3-period cross-over proof-of-concept…”
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5
The nociceptin/orphanin FQ receptor partial agonist sunobinop promotes non-REM sleep in rodents and patients with insomnia
Published in The Journal of clinical investigation (02-01-2024)“…Insomnia is a common disorder that poses a significant public health burden. Current treatments for insomnia primarily target aminobutyric acid or orexin…”
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The nociceptin/orphanin FQ receptor partial agonist sunobinop promotes non-REM sleep in rodents and patients with insomnia
Published in The Journal of clinical investigation (01-01-2024)“…The potent and partial agonist sunobinop activates the nociceptin/orphanin-FQ peptide receptor and promotes non-REM sleep in rodents and patients with insomnia…”
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Monoacylglycerol lipase activity is a critical modulator of the tone and integrity of the endocannabinoid system
Published in Molecular pharmacology (01-12-2010)“…Endocannabinoids are lipid molecules that serve as natural ligands for the cannabinoid receptors CB1 and CB2. They modulate a diverse set of physiological…”
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Evaluation of sunobinop for next-day residual effects in healthy participants
Published in Frontiers in pharmacology (19-08-2024)“…Sunobinop is a novel, potent, selective partial agonist at nociceptin/orphanin FQ peptide (NOP) receptors. The primary objective of this randomized,…”
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9
Particulate levodopa nose-to-brain delivery targets dopamine to the brain with no plasma exposure
Published in International journal of pharmaceutics (25-04-2022)“…[Display omitted] Levodopa (L-DOPA) is an oral Parkinson’s Disease drug that generates the active metabolite - dopamine (DA) in vivo. However, oral L-DOPA…”
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10
Pharmacological evaluation of NSAID-induced gastropathy as a “Translatable” model of referred visceral sensitivity
Published in World journal of gastroenterology : WJG (07-09-2017)“…AIM To evaluate whether non-steroidal anti-inflammatory drugs(NSAIDs)-induced gastropathy is a clinically predictive model of referred visceral…”
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Depression-like phenotype following chronic CB1 receptor antagonism
Published in Neurobiology of disease (01-08-2010)“…Abstract Rimonabant was the first clinically marketed cannabinoid (CB)1 receptor antagonist developed to treat obesity. Unfortunately, CB1 receptor antagonism…”
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12
The persistence of a long-term negative affective state following the induction of either acute or chronic pain
Published in Pain (Amsterdam) (01-12-2008)“…Clinically, pain is a complex phenomenon consisting of both sensory and affective aberrations that can persist indefinitely. Pre-clinically, several animal…”
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Safety, Tolerability, and Pharmacokinetics of Single‐ and Multiple‐Ascending Doses of Sunobinop in Healthy Participants
Published in Clinical pharmacology in drug development (01-07-2024)“…Sunobinop is an investigational, potent, selective partial agonist at the nociceptin/orphanin FQ peptide receptor in vitro. Three phase 1 studies were…”
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Current and potential pharmacological treatment options for insomnia in patients with alcohol use disorder in recovery
Published in Neuropsychopharmacology reports (01-09-2020)“…Alcohol use disorder (AUD) is characterized by dysfunction in motivational, mood‐stress regulation, and sleep systems that interact in complex ways to heighten…”
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Targeting CB2 receptors and the endocannabinoid system for the treatment of pain
Published in Brain Research Reviews (01-04-2009)“…Abstract The endocannabinoid system consists of the cannabinoid (CB) receptors, CB1 and CB2 , the endogenous ligands anandamide (AEA, arachidonoylethanolamide)…”
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Journal Article Conference Proceeding -
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Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy
Published in Neuropharmacology (01-04-2005)“…To date, two cannabinoid receptors have been identified, CB1 and CB2. Activation of these receptors with non-selective cannabinoid receptor agonists reduces…”
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Pain is a salient “stressor” that is mediated by corticotropin-releasing factor-1 receptors
Published in Neuropharmacology (01-09-2010)“…Corticotropin-releasing factor (CRF) plays a major role in controlling the body’s response to stress. Because painful conditions are inherently stressful, we…”
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Abnormal gait, due to inflammation but not nerve injury, reflects enhanced nociception in preclinical pain models
Published in Brain research (12-10-2009)“…Abstract Validation of gait analysis has the potential to bridge the gap between data from animal pain models and clinical observations. The goal of these…”
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CNS penetration of small molecules following local inflammation, widespread systemic inflammation or direct injury to the nervous system
Published in Life sciences (1973) (09-09-2009)“…We sought to investigate effects of local and systemic inflammation on CNS permeability of small molecules and compare these to effects of direct injury to the…”
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Pharmacological characterisation of a rat model of incisional pain
Published in British journal of pharmacology (01-01-2004)“…Both clinical and preclinical models of postsurgical pain are being used more frequently in the early evaluation of new chemical entities. In order to assess…”
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