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PubMed Journals Articles About "TollLike Receptor Agonists Pipeline Insights 2017 Updated 30052017" RSS

05:09 EST 11th December 2018 | BioPortfolio

TollLike Receptor Agonists Pipeline Insights 2017 Updated 30052017 PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest TollLike Receptor Agonists Pipeline Insights 2017 Updated 30052017 articles that have been published worldwide.

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Showing "TollLike Receptor Agonists Pipeline Insights 2017 Updated 30052017" PubMed Articles 1–25 of 14,000+

Gamma aminobutyric acid (GABA) receptor agonists for acute stroke.

Gamma aminobutyric acid (GABA) receptor agonists have been shown to have a neuroprotectant effect in reducing infarct size and improving functional outcome in animal models of cerebrovascular disease. However, the sedative effects of GABA receptor agonists have limited their wider application in people with acute stroke, due to the potential risk of stupor. This is an update of a Cochrane Review first published in 2013, and previously updated in 2014 and 2016.


Adenosine receptor agonists deepen the inhibition of platelet aggregation by P2Y antagonists.

Several adenosine receptor (AR) agonists have been shown in the past to possess anti-platelet potential; however, the adjunctive role of AR agonists in anti-platelet therapy with the use of P2Y receptor inhibitors has not been elucidated so far. This in vitro aggregation-based study investigates whether the inhibition of platelet function mediated by cangrelor or prasugrel metabolite can be potentiated by AR agonists. It evaluates the effect of non-selective (2-chloroadenosine), A-selective (UK 432097, MRE ...

Computationally Guided Identification of Allosteric Agonists of the Metabotropic Glutamate 7 Receptor.

The metabotropic glutamate 7 (mGlu7) receptor belongs to the group III of mGlu receptors. Since the mGlu7 receptor can control excitatory neurotransmission in the hippocampus and cortex, modulation of the receptor may has therapeutic benefit in several CNS diseases. However, mGlu7 remains relatively unexplored amongst the eight known mGlu receptors partly because of the limited availability of tool compounds to interrogate its potential therapeutic utility. Here we report the discovery of a new class of mGl...


Assessment of Switching to Suvorexant versus the Use of Add-on Suvorexant in Combination with Benzodiazepine Receptor Agonists in Insomnia Patients: A Retrospective Study.

Suvorexant is a novel hypnotic drug that does not interact with the conventional γ-aminobutyric acid (GABA)-A receptor. We investigated the method by which suvorexant was introduced in insomnia patients who were taking benzodiazepine receptor agonists (BzRA).

Glucagon-like peptide-1 receptor agonists and cardiovascular protection in type 2 diabetes: a pathophysiology-based review of clinical implications.

Cardiovascular outcome trials (CVOT) with glucagon-like peptide-1 receptor agonists (GLP-1 RA) have had variable results to date: with two CVOTs being positive and two concluding neutrality/safety results for primary cardiovascular outcome. Mechanistic insights delving into the pathophysiologic mechanisms that may link certain GLP-1 RA to cardioprotection may help define the application of this medication class in clinical practice based on the evidence of the CVOT data. We discuss the various mechanisms th...

Anticancer activity study of A adenosine receptor agonists.

A adenosine receptor (AAR) signalling activation seems to mediate anticancer effect, and it has been targeted for drug development. The identification of potent and selective AAR agonists could be crucial for cancer drug development.

Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multi-dose Formulations.

Novel peptidic dual agonists of the glucagon-like peptide 1 (GLP-1) and glucagon receptor are reported to have enhanced efficacy over pure GLP-1 receptor agonists with regard to treatment of obesity and diabetes. We describe novel exendin-4 based dual agonists designed with an activity ratio favoring the GLP-1 versus the glucagon receptor. As result of an iterative optimization procedure that included molecular modeling, structural biological studies (X-ray, NMR), peptide design & synthesis, experimental ac...

Chronic treatment with a metabotropic mGlu2/3 receptor agonist diminishes behavioral response to a phenethylamine hallucinogen.

There is evidence that mGlu2/3 receptors regulate 5-HT signaling, interactions that have been theorized to play a role in the antipsychotic-like effects of mGlu2/3 agonists as well as the hallucinogenic effects of 5-HT agonists. One approach to unraveling this interaction is through the chronic administration of agonists at the two receptors, which should influence the functional properties of the targeted receptor due to receptor downregulation or desensitization and thereby alter crosstalk between the two...

Effect of cannabinoid receptor agonists on isolated rat atria.

Cannabinoid CB2 receptor agonists are under investigation for clinical use. At the same time, synthetic cannabinoids have been implicated in a number of deaths. One cause of death is thought to be cardiac arrest subsequent to extreme tachycardia. Central mechanisms are thought to play a role in this, with CB1 but not CB2 receptors thought to mediate central effects. However, the direct effects on cannabinoids on the heart is less well understood. We therefore tested the effects of cannabinoids on isolated r...

Identification and Structure-Activity Relationship (SAR) of potent and selective oxadiazole-based agonists of sphingosine-1-phosphate receptor (S1P).

Agonism of S1P receptor has been proven to be responsible for peripheral blood lymphopenia and elicts the identification of various S1P modulators. In this paper we described a series of oxadiazole-based S1P direct-acting agonists disubstituted on terminal benzene ring, with high potency for S1P receptor and favorable selectivity against S1P receptor. In addition, two representative agents named 16-3b and 16-3g demonstrated impressive efficacy in lymphocyte reduction along with reduced effect on heart rate ...

The effect of glucagon-like peptide 1 and glucagon-like peptide 1 receptor agonists on energy expenditure: a systematic review and meta-analysis.

We reviewed clinical trials addressing the effect of glucacon-like peptide 1 (GLP-1) or GLP-1 receptor agonists (GLP-1RA) on energy expenditure (EE) in adults.

Effects of imidazoline I2 receptor agonists on reserpine-induced hyperalgesia and depressive-like behavior in rats.

Pharmacotherapies for fibromyalgia treatment are lacking. This study examined the antinociceptive and antidepressant-like effects of imidazoline I2 receptor (I2R) agonists in a reserpine-induced model of fibromyalgia in rats. Rats were treated for 3 days with vehicle or reserpine. The von Frey filament test was used to assess the antinociceptive effects of I2 receptor agonists, and the forced swim test was used to assess the antidepressant-like effects of these drugs. 2-BFI (3.2-10 mg/kg, intraperitoneall...

Cardiovascular safety of GLP-1 receptor agonists for diabetes patients with high cardiovascular risk: a meta-analysis of cardiovascular outcomes trials.

To show long-term cardiovascular safety of the GLP-1 receptor agonists for diabetes patients with cardiovascular risk.

MK212, a 5-hydroxytryptamine 2C receptor agonist, inhibits conditioned avoidance responses independent of blocking endogenous dopamine release in rats.

Although it is widely accepted that 5-hydroxytryptamine (5-HT) 2C receptor agonists produce antipsychotic effects by reducing endogenous dopamine release from presynaptic neurons, no direct evidence supports this. The aim of the present study was to investigate whether the antipsychotic effects induced by 5-HT receptor agonists are dependent on the inhibition of endogenous dopamine release. We developed a novel conditioned avoidance response paradigm to test this hypothesis. In this assay, rats in which dop...

Relationship between MRGPRX2 and pethidine hydrochloride- or fentanyl citrate-induced LAD2 cell degranulation.

Pethidine hydrochloride (PH) and fentanyl citrate (FC) are opioid receptor agonists commonly used to treat pain clinically. PH and FC have been reported to have a high potential for pseudoallergic effects, but the underlying mechanism has not been well studied. MRGPRX2 is a novel atypical opioid receptor that is mainly expressed in human mast cells and considered to mediate drug-induced pseudoallergic reactions. This study aimed to investigate the allergy effect of these two opioid receptor agonists and the...

LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.

Oxytocin (OT) and its receptor (OT-R) are implicated in the aetiology of autism spectrum disorders (ASD) and OT-R is a potential target for therapeutic intervention. Very few nonpeptide oxytocin agonists have currently been reported. Their molecular and in vivo pharmacology remain to be clarified and none of them has been shown efficient in improving social interaction in animal models relevant to ASD. In an attempt to rationalize the design of centrally active nonpeptide full agonists, we studied in a syst...

Understanding mode of action can drive the translational pipeline towards more reliable health benefits for probiotics.

The different levels of knowledge described in a translational pipeline (the connection of molecular mechanisms with pre-clinical physiological and human health effects) are not complete for many probiotics. At present, we are not in a position to fully understand the mechanistic basis of many well established probiotic health benefits which, in turn, limits our ability to use mechanisms to predict which probiotics are likely to be effective in any given population. Here we suggest that this concept of a tr...

The Chemistry and Pharmacology of Synthetic Cannabinoid Receptor Agonists as New Psychoactive Substances: Origins.

Synthetic cannabinoid receptor agonists (SCRAs) have proliferated as new psychoactive substances (NPS) over the past decade. Relative to other classes of NPS, SCRAs are structurally heterogeneous; however, most SCRAs act as potent, high-efficacy agonists of cannabinoid type 1 and type 2 receptors (CB and CB, respectively). Characterization of the pharmacology and toxicology of these substances is hindered by the dynamic nature of the SCRA marketplace. Beyond basic pharmacological profiling at CB and CB rece...

Cardiovascular Effects of Different GLP-1 Receptor Agonists in Patients with Type 2 Diabetes.

Glucagon-like peptide-1 receptor agonists (GLP-1 RAs) have positive effects on weight loss, blood pressure, hyperlipidemia, and glycemic control. They exhibit a broad range of effects on the cardiovascular system that are independent of changes in blood glucose. Cardiovascular outcome trials have demonstrated safety of GLP-1 RAs but results for cardiovascular efficacy were varied. The aim of the present review is the assessment of the effects of GLP-1 RAs on cardiovascular risk factors, and major cardiovasc...

NOCICEPTIN/ORPHANIN FQ RECEPTOR AGONISTS INCREASE AGGRESSIVENESS IN THE MOUSE RESIDENT-INTRUDER TEST.

Aggressive behaviors can be considered symptoms of bipolar disorder, schizophrenia, post-traumatic stress, intermittent explosive, and personality disorders. Nociceptin/orphanin FQ (N/OFQ) is a peptide acting as endogenous ligand of the NOP receptor. Preclinical and clinical findings suggest the NOP receptor as an innovative target for the treatment of psychopathologies, such as anxiety, depression, and drug abuse. This study investigated the effects of NOP ligands and the behavioral phenotype of mice lacki...

NOP agonists prevent the antidepressant-like effects of nortriptyline and fluoxetine but not R-ketamine.

Nociceptin/orphanin FQ (N/OFQ) is the endogenous ligand of a Gi protein-coupled receptor named NOP. Both N/OFQ and NOP receptor are widely expressed in brain areas involved in the control of emotional processes. Clinical and preclinical studies support antidepressant effects due to the blockade of NOP receptor signaling. By contrast, NOP receptor activation did not evoke any change in behavioral despair tests.

Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.

While mu opioid receptor (MOR) agonists are especially effective as broad-spectrum pain relievers, it has been exceptionally difficult to achieve a clear separation of analgesia from many problematic side effects. Recently, many groups have sought MOR agonists that induce minimal βarrestin-mediated signaling, since MOR agonist-treated βarrestin2 knockout mice were found to display enhanced antinociceptive effects with significantly less respiratory depression and tachyphylaxis. Substantial data now exists...

Targeting the Incretin/Glucagon System with Triagonists to Treat Diabetes.

Glucagon-like peptide-1 (GLP-1) receptor agonists have been efficacious for the treatment of type 2 diabetes due to their ability to reduce weight and attenuate hyperglycemia. However, the activity of GLP-1R-directed strategies is sub-maximal, and the only potent, sustainable treatment for metabolic dysfunction is bariatric surgery, necessitating the development of novel therapeutics. GLP-1 is structurally related to glucagon and glucose-dependent insulinotropic peptide (GIP), allowing for the development o...

Diagnosis and Therapy of Immune thrombocytopenia.

Immune thrombocytopenia (ITP) is a heterogeneous disease. Diagnosis of primary ITP continues to be based on the exclusion of all known causes for secondary ITP. The new ITP classification distinguishes three categories. First line treatment consists of either dexamethasone or prednisone. The most effective options in second line treatment are splenectomy or thrombopoietin receptor agonists. The medical societies for hematology and oncology of the German-speaking countries have recently updated their guideli...

Glucagon-like peptide-1 receptor action in the vasculature.

Glucagon-like peptide-1 receptor (GLP-1R) agonists augment insulin secretion and are thus used clinically to improve glycemia in subjects with type 2 diabetes (T2D). As recent data reveals marked improvement in cardiovascular outcomes in T2D subjects treated with the GLP-1R agonists liraglutide and semaglutide in the LEADER and SUSTAIN-6 clinical trials respectively, there is growing interest in delineating the mechanism(s) of action for GLP-1R agonist-induced cardioprotection. Of importance, negligible GLP...


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