Results 51 to 60 of about 261,867 (135)

Agonist binding, agonist affinity and agonist efficacy at G protein‐coupled receptors [PDF]

open access: yesBritish Journal of Pharmacology, 2008
Measurements of affinity and efficacy are fundamental for work on agonists both in drug discovery and in basic studies on receptors. In this review I wish to consider methods for measuring affinity and efficacy at G protein coupled receptors (GPCRs).
openaire   +2 more sources

Two small-molecule activators share similar effector sites in the KCNQ1 channel pore but have distinct effects on voltage sensor movements

open access: yesFrontiers in Physiology, 2022
ML277 and R-L3 are two small-molecule activators of KCNQ1, the pore-forming subunit of the slowly activating potassium channel IKs. KCNQ1 loss-of-function mutations prolong cardiac action potential duration and are associated with long QT syndrome, which
Lei Chen   +6 more
doaj   +1 more source

Treatment of drug addiction and psychopathology: A field study

open access: yesEuropean Journal of Psychology Applied to Legal Context, 2010
Field study to assess the concurrence of the psychopathology of drug addiction, and to evaluate the efficacy of pharmacological treatment versus drug-free treatments for the psychopathology of drug addiction.
Antonio Souto   +2 more
doaj  

Development and characterization of a potent free fatty acid receptor 1 (FFA1) fluorescent tracer [PDF]

open access: yes, 2016
The free fatty acid receptor 1 (FFA1/GPR40) is a potential target for treatment of type 2 diabetes. Although several potent agonists have been described, there remains a strong need for suitable tracers to interrogate ligand binding to this receptor.
Christiansen, Elisabeth   +4 more
core   +3 more sources

Treatment of type 2 diabetes by free fatty acid receptor agonists [PDF]

open access: yes, 2014
Dietary free fatty acids (FFAs), such as ω-3 fatty acids, regulate metabolic and anti-inflammatory processes, with many of these effects attributed to FFAs interacting with a family of G protein-coupled receptors.
Hudson, Brian D.   +3 more
core   +2 more sources

Small-angle neutron scattering studies on the AMPA receptor GluA2 in the resting, AMPA-bound and GYKI-53655-bound states

open access: yesIUCrJ, 2018
The AMPA receptor GluA2 belongs to the family of ionotropic glutamate receptors, which are responsible for most of the fast excitatory neuronal signalling in the central nervous system. These receptors are important for memory and learning, but have also
Andreas Haahr Larsen   +7 more
doaj   +1 more source

PROSPECTS OF Toll-LIKE RECEPTOR AGONISTS AND ANTAGONISTS FOR PREVENTION AND TREATMENT OF VIRAL INFECTIONS

open access: yesМедицинская иммунология, 2019
Antiviral research has focused mainly on viral targets. However, cellular targets involved in the viral life cycle and antiviral response are becoming more attractive for research, providing a variety of opportunities for antiviral therapy.
A. A. Nikonova   +2 more
doaj   +3 more sources

An updated assessment of the translational promise of G-protein-biased kappa opioid receptor agonists to treat pain and other indications without debilitating adverse effects

open access: yesPharmacological Research, 2022
Kappa opioid receptor (κOR) agonists lack the abuse liability and respiratory depression effects of clinically used mu opioid receptor (μOR) analgesics and are hypothesized to be safer alternatives.
Alexander R. French, Richard M. van Rijn
doaj   +1 more source

Mutations of MRGPRX2, drug sensitivity, and genetic markers related to disease

open access: yesJournal of Allergy and Clinical Immunology: Global
Mast cells (MCs) express the novel class A Mas-related G protein–coupled receptor X2 (MRGPRX2). Additionally, neurons and other leukocytes including basophils express MRGPRX2.
Subashini Hemamala Ratnayake, MSc, BSc   +5 more
doaj   +1 more source

Current Advances in Immunoassays for the Detection of β2-Agonists

open access: yesFoods, 2022
β2-agonists are a group of synthetic phenylethanolamine compounds which are traditionally used for treating bronchospasm. These compounds can also increase skeletal muscle mass and decrease body fat.
Shuyu Ouyang, Shuting Yu, Yingying Le
doaj   +1 more source

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