N3136

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Showing 1-27 of 27 results for "N3136" within Papers

Low-dose prazosin alone and in combination with propranolol or naltrexone: effects on ethanol and sucrose seeking and self-administration in the P rat.

Terril L Verplaetse et al.

Psychopharmacology, 232(15), 2647-2657 (2015-03-07)

Evidence suggests that the noradrenergic system mediates ethanol reinforcement. However, preclinical studies suggest that noradrenergic antagonists block other oral reinforcers indicating possible unwanted secondary medication effects. This study examined combinations of low-dose prazosin with propranolol or naltrexone using a behavioral

Activation of TRPM7 channels by small molecules under physiological conditions.

T Hofmann et al.

Pflugers Archiv : European journal of physiology, 466(12), 2177-2189 (2014-03-19)

Transient receptor potential cation channel, subfamily M, member 7 (TRPM7) is a cation channel covalently linked to a protein kinase domain. TRPM7 is ubiquitously expressed and regulates key cellular processes such as Mg(2+) homeostasis, motility, and proliferation. TRPM7 is involved

Differential antagonism of the rate-decreasing effects of kappa-opioid receptor agonists by naltrexone and norbinaltorphimine.

K R Powell et al.

European journal of pharmacology, 377(1), 21-28 (1999-08-17)

Eight kappa-opioid receptor agonists were examined for their effects in squirrel monkeys responding under a fixed interval 3-min schedule of stimulus termination. Six of these kappa-opioid receptor agonists decreased dose-dependently the total number of responses and with an order of

Persistent Adaptations in Afferents to Ventral Tegmental Dopamine Neurons after Opiate Withdrawal.

Jennifer Kaufling et al.

The Journal of neuroscience : the official journal of the Society for Neuroscience, 35(28), 10290-10303 (2015-07-17)

Protracted opiate withdrawal is accompanied by altered responsiveness of midbrain dopaminergic (DA) neurons, including a loss of DA cell response to morphine, and by behavioral alterations, including affective disorders. GABAergic neurons in the tail of the ventral tegmental area (tVTA)

Phytochemical composition and antinociceptive activity of Bauhinia glauca subsp. hupehana in rats.

Jinlong Xu et al.

PloS one, 10(2), e0117801-e0117801 (2015-02-07)

In traditional medicine, Bauhinia glauca subsp. hupehana has long been used as an analgesic agent in China. The aim of this study was to evaluate the antinociceptive activity of the ethanol extract of the aerial parts of B. glauca subsp.

Caenorhabditis elegans show preference for stimulants and potential as a model organism for medications screening

Engleman EA, et al.

Frontiers in Physiology, 9, 7-16 (2018)

Chronic treatment with novel brain-penetrating selective NOP receptor agonist MT-7716 reduces alcohol drinking and seeking in the rat.

Roberto Ciccocioppo et al.

Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 39(11), 2601-2610 (2014-05-28)

Since its discovery, the nociceptin/orphanin FQ (N/OFQ)-NOP receptor system has been extensively investigated as a promising target to treat alcoholism. Encouraging results obtained with the endogenous ligand N/OFQ stimulated research towards the development of novel brain-penetrating NOP receptor agonists with

Novel in situ gelling ocular films for the opioid growth factor-receptor antagonist-naltrexone hydrochloride: fabrication, mechanical properties, mucoadhesion, tolerability and stability studies.

Hamdy Abdelkader et al.

International journal of pharmaceutics, 477(1-2), 631-642 (2014-12-03)

Naltrexone hydrochloride (NTX) is an innovative drug used in ophthalmology for treatment of ocular surface diseases such as impaired corneal wound healing and severe dry eye. Poor chemical stability has been a major limitation for development of NTX in solution

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

Jing Yuan et al.

Nature chemical biology, 5(10), 765-771 (2009-09-08)

Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened seven parasite lines for differences in responses to 1,279 bioactive chemicals. Hundreds of compounds were

Behavioural profile of exendin-4/naltrexone dose combinations in male rats during tests of palatable food consumption.

F L Wright et al.

Psychopharmacology, 231(18), 3729-3744 (2014-04-01)

The glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 potently suppresses food intake in animals and humans. However, little is known about the behavioural specificity of this effect either when administered alone or when co-administered with another anorectic agent. The present

Dry eye reversal and corneal sensation restoration with topical naltrexone in diabetes mellitus.

Ian S Zagon et al.

Archives of ophthalmology (Chicago, Ill. : 1960), 127(11), 1468-1473 (2009-11-11)

To determine if topical application of naltrexone hydrochloride (NTX), an opioid antagonist, restores tear production and corneal sensation in rats with diabetes mellitus. Type 1 diabetes was induced with streptozotocin in rats. Tear production was measured by the Schirmer test

Early short-term PXT3003 combinational therapy delays disease onset in a transgenic rat model of Charcot-Marie-Tooth disease 1A (CMT1A)

Prukop T, et al.

Testing, 14(1), e0209752-e0209752 (2019)

Development and validation of a bioanalytical method for the simultaneous determination of heroin, its main metabolites, naloxone and naltrexone by LC-MS/MS in human plasma samples: Application to a clinical trial of oral administration of a heroin/naloxone formulation.

Raquel Moreno-Vicente et al.

Journal of pharmaceutical and biomedical analysis, 114, 105-112 (2015-06-04)

A bioanalytical method using high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) was developed and validated for simultaneous quantification of heroin, its main metabolites and naloxone. In addition, naltrexone was detected qualitatively. This method was used to analyse human plasma samples from

Chemical genetics reveals a complex functional ground state of neural stem cells.

Phedias Diamandis et al.

Nature chemical biology, 3(5), 268-273 (2007-04-10)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain cancer. However, the complete repertoire of signaling pathways that governs the

Discriminative stimulus effects of the novel imidazoline I₂ receptor ligand CR4056 in rats.

Yanyan Qiu et al.

Scientific reports, 4, 6605-6605 (2014-10-14)

This study examined whether a novel imidazoline I₂ receptor ligand CR4056 could serve as a discriminative stimulus and whether it shares similar discriminative stimulus effects with other reported I₂ receptor ligands. Eight male Sprague-Dawley rats were trained to discriminate 10.0 mg/kg

Parabrachial opioidergic projections to preoptic hypothalamus mediate behavioral and physiological thermal defenses.

Aaron J Norris et al.

eLife, 10 (2021-03-06)

Maintaining stable body temperature through environmental thermal stressors requires detection of temperature changes, relay of information, and coordination of physiological and behavioral responses. Studies have implicated areas in the preoptic area of the hypothalamus (POA) and the parabrachial nucleus (PBN)

Alleviating waiting impulsivity and perseverative responding by μ-opioid receptor antagonism in two inbred mouse strains.

Sandra Sanchez-Roige et al.

Psychopharmacology, 232(8), 1483-1492 (2014-11-09)

Recent evidence has implicated the opioid system in exaggerated ethanol consumption and impulsivity deficits. The opioid receptor antagonist naltrexone (NTX) has proven efficient in reducing alcohol consumption; however, its role on impulsive behaviour is not fully characterised. The aim of

Caenorhabditis elegans as a model system to identify therapeutics for alcohol use disorders

Katner SN, et al.

Behavioural Brain Research, 365, 7-16 (2019)

Ethanol-reinforced behaviour in the rat: effects of naltrexone.

P Bienkowski et al.

European journal of pharmacology, 374(3), 321-327 (1999-07-28)

It has been repeatedly reported that endogenous opioid pathways play an important role in ethanol drinking behaviour. In line with these findings, a non-selective opioid receptor antagonist, naltrexone, seems to reduce relapse rates in detoxified alcoholics. The aim of the

Involvement of nitridergic and opioidergic pathways in the antinociception of gabapentin in the orofacial formalin test in mice.

Hugo F Miranda et al.

Pharmacological reports : PR, 67(2), 399-403 (2015-02-26)

Pain is one of the most common problems in clinical medicine. There is considerable evidence that pharmacologic approaches are the most widely used therapeutic options to ameliorate persistent or chronic pain. In this study it was evaluated the effect of

Polytherapy with a combination of three repurposed drugs (PXT3003) down-regulates Pmp22 over-expression and improves myelination, axonal and functional parameters in models of CMT1A neuropathy.

Ilya Chumakov et al.

Orphanet journal of rare diseases, 9, 201-201 (2014-12-11)

Charcot-Marie-Tooth disease type 1A (CMT1A) is the most common inherited sensory and motor peripheral neuropathy. It is caused by PMP22 overexpression which leads to defects of peripheral myelination, loss of long axons, and progressive impairment then disability. There is no

A non-rewarding, non-aversive buprenorphine/naltrexone combination attenuates drug-primed reinstatement to cocaine and morphine in rats in a conditioned place preference paradigm.

Sarah F Cordery et al.

Addiction biology, 19(4), 575-586 (2012-12-18)

Concurrent use of cocaine and heroin is a major public health issue with no effective relapse prevention treatment currently available. To this purpose, a combination of buprenorphine and naltrexone, a mixed very-low efficacy mu-opioid receptor agonist/kappa-opioid receptor antagonist/nociceptin receptor agonist

Effects of baclofen and naltrexone, alone and in combination, on the consumption of palatable food in male rats.

Nicole M Avena et al.

Experimental and clinical psychopharmacology, 22(5), 460-467 (2014-07-30)

Excess consumption of palatable food has been shown to affect reward-related brain regions, and pharmaceutical treatments for drug addiction may also be effective in treating overeating of such foods. The GABA-B agonist baclofen and opioid antagonist naltrexone have both been

Caenorhabditis elegans as a model system to identify therapeutics for alcohol use disorders.

Simon N Katner et al.

Behavioural brain research, 365, 7-16 (2019-02-26)

Alcohol use disorders (AUDs) cause serious problems in society and few effective treatments are available. Caenorhabditis elegans (C. elegans) is an excellent invertebrate model to study the neurobiological basis of human behavior with a conserved, fully tractable genome, and a

The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist.

M M Gassaway et al.

Translational psychiatry, 4, e411-e411 (2014-07-16)

Current pharmacological treatments of depression and related disorders suffer from major problems, such as a low rate of response, slow onset of therapeutic effects, loss of efficacy over time and serious side effects. Therefore, there is an urgent need to

Mechanisms of QT prolongation by buprenorphine cannot be explained by direct hERG channel block.

Phu N Tran et al.

PloS one, 15(11), e0241362-e0241362 (2020-11-07)

Buprenorphine is a μ-opioid receptor (MOR) partial agonist used to manage pain and addiction. QTC prolongation that crosses the 10 msec threshold of regulatory concern was observed at a supratherapeutic dose in two thorough QT studies for the transdermal buprenorphine

Predisposing effects of neonatal visceral pain on abuse-related effects of morphine in adult male Sprague Dawley rats.

Andrew P Norwood et al.

Psychopharmacology, 231(22), 4281-4289 (2014-04-24)

Adverse early life experiences are risk factors for drug abuse and addiction. Changes in brain opioid systems have been demonstrated in response to neonatal visceral pain (NVP), but the impact of these changes on abuse-related effects of morphine are unknown.

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