Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist for the Chronic Treatment of Heart Diseases
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DOI: 10.1002/cmdc.201700151
Abstract: Adenosine is known to be released under a variety of physiological and pathophysiological conditions to facilitate the protection and regeneration of injured ischemic tissues. The activation of myocardial adenosine A1 receptors (A1Rs) has been shown to… read more here.
Keywords: a1r; agonist; treatment heart; bialanate hydrochloride ... See more keywords
The first‐in‐man randomized trial of a beta3 adrenoceptor agonist in chronic heart failure: the BEAT‐HF trial
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DOI: 10.1002/ejhf.714
Abstract: The third isotype of beta adrenergic receptors (β3 ARs) has distinctly different effects on cardiomyocytes compared with β1 and β2 ARs. Stimulation of β3 ARs may reduce cardiomyocyte Na+ overload and reduce oxidative stress in… read more here.
Keywords: agonist; trial; first man; heart failure ... See more keywords
Safety, Pharmacokinetics, and Pharmacodynamics of the Oral TLR8 Agonist Selgantolimod in Chronic Hepatitis B
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DOI: 10.1002/hep.31795
Abstract: In patients with chronic hepatitis B (CHB) infection, activation of toll‐like receptor 8 may induce antiviral immunity and drive functional cure. Selgantolimod, a toll‐like receptor 8 agonist, was evaluated in patients with CHB who were… read more here.
Keywords: chronic hepatitis; hepatitis; agonist; pharmacokinetics pharmacodynamics ... See more keywords
Parameterization of the GPR119 Receptor Agonist AR231453
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DOI: 10.1002/jcc.25079
Abstract: The GPR119 receptor is a class A G protein‐coupled receptor expressed mainly in pancreatic beta cells. Since GPR119 receptor activation ameliorates Type 2 Diabetes through an increase in glucose‐dependent insulin release, the development of new… read more here.
Keywords: force field; agonist; parameterization gpr119; gpr119 receptor ... See more keywords
Comparison and interaction of morphine and CB1 agonist conditioned place preference in the rat model of early life stress
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DOI: 10.1002/jdn.10094
Abstract: Early life stress (ELS) disrupts brain development and subsequently affects physical and psychological health. ELS has been associated with an increased risk of relapse and inadequate treatment response in addicted patients. The current study was… read more here.
Keywords: morphine; agonist; rewarding effect; effect ... See more keywords
Behavioural and pharmacological profiles of zebrafish administrated pyrrolidinyl benzodioxanes and prolinol aryl ethers with high affinity for heteromeric nicotinic acetylcholine receptors
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DOI: 10.1007/s00213-020-05536-6
Abstract: Rationale Prolinol aryl ethers and their rigidified analogues pyrrolidinyl benzodioxanes have a high affinity for mammalian α4β2 nicotinic acetylcholine receptors (nAChRs). Electrophysiological studies have shown that the former are full agonists and the latter partial… read more here.
Keywords: aryl ethers; high affinity; prolinol aryl; agonist ... See more keywords
The adenosine A(2A) receptor agonist CGS 21680 alleviates auditory sensorimotor gating deficits and increases in accumbal CREB in rats neonatally treated with quinpirole
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DOI: 10.1007/s00213-020-05631-8
Abstract: The adenosine A(2A) receptor forms a mutually inhibitory heteromer with the dopamine D2 receptor, and A(2A) agonists decrease D2 signaling. This study analyzed whether an adenosine A(2A) agonist would alleviate deficits in sensorimotor gating and… read more here.
Keywords: agonist; sensorimotor gating; cgs 21680; adenosine receptor ... See more keywords
Effect of coadministration of the GABAB agonist baclofen and the 5-HT2C agonist Ro60-0175 on the expression of amphetamine-induced locomotor sensitization
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DOI: 10.1007/s00221-019-05540-z
Abstract: GABAB and 5-HT2C agonists are effective in attenuating the behavioral effects of psychostimulants. However, they induce adverse side effects when used in high doses. The previous evidence has suggested that the 5HT2C receptor activation effect… read more here.
Keywords: baclofen; gabab; agonist; ro60 0175 ... See more keywords
G protein-coupled estrogen receptor 1 (GPER-1) and agonist G-1 inhibit growth of ovarian cancer cells by activation of anti-tumoral transcriptome responses: impact of GPER-1 mRNA on survival
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DOI: 10.1007/s00432-020-03333-4
Abstract: The present study intended to further elucidate the role of G protein-coupled estrogen receptor 1 (GPER-1) in ovarian cancer by comparing the effects of a GPER-1 knockdown and treatment with its agonist G-1 on cell… read more here.
Keywords: cell; agonist; gper; ovarian cancer ... See more keywords
Dopamine D1 receptor agonist treatment attenuates extinction of morphine conditioned place preference while increasing dendritic complexity in the nucleus accumbens core
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DOI: 10.1016/j.bbr.2017.01.011
Abstract: HighlightsD1R agonist given after extinction training attenuates extinction of morphine CPP.D1R agonist given after extinction increases dendritic complexity in accumbens core.D1R agonist effect on accumbal dendritic morphology depends on previous conditioning. Abstract The dopamine D1… read more here.
Keywords: morphine; agonist; extinction; morphology ... See more keywords
Transient receptor potential vanilloid 4 agonist GSK1016790A improves neurological outcomes after intracerebral hemorrhage in mice.
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DOI: 10.1016/j.bbrc.2020.06.103
Abstract: Intracerebral hemorrhage (ICH) is one of the most severe subtypes of stroke with high morbidity and mortality. Although a lot of drug discovery studies have been conducted, the drugs with satisfactory therapeutic effects for motor… read more here.
Keywords: trpv4 agonist; agonist; intracerebral hemorrhage; receptor potential ... See more keywords