Effects of urotensin II receptor antagonist, GSK1440115, in asthma
Frontiers in Pharmacology, 2013 Background: Urotensin II (U-II) is highly expressed in the human lung and has been implicated in regulating respiratory physiology in preclinical studies.
Alison D Portnoy +6 more
doaj +1 more source
Interaction of hypothalamic GABA\u3csub\u3eA\u3c/sub\u3e and excitatory amino acid receptors controlling heart rate in rats [PDF]
, 1991 We have previously shown that microinjection of drugs that impair gamma-aminobutyric acid (GABA)-mediated synaptic inhibition into the dorsomedial hypothalamus (DMH) of rats generates cardiovascular and behavioral changes that mimic the response to ...
DiMicco, Joseph A., Soltis, Robert P.
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Orexin-1 receptor blockade dysregulates REM sleep in the presence of orexin-2 receptor antagonism
Frontiers in Neuroscience, 2014 In accordance with the prominent role of orexins in the maintenance of wakefulness via activation of orexin-1 (OX1R) and orexin-2 (OX2R) receptors, various dual OX1/2R antagonists have been shown to promote sleep in animals and humans.
Christine eDugovic +5 more
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Biomedicines, 2022 Background: autism spectrum disorder (ASD) is a neurodevelopmental disorder affecting around 1 out of 68 children and its incidence shows an increasing tendency. There is currently no effective treatment for ASD.
Kristóf László +14 more
doaj +1 more source
A single extracellular amino acid in Free Fatty Acid Receptor 2 defines antagonist species selectivity and G protein selection bias [PDF]
, 2017 Free Fatty Acid Receptor 2 is a GPCR activated by short chain fatty acids produced in high levels in the lower gut by microbial fermentation of non-digestible carbohydrates.
Aoki, Junken +9 more
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mGluR5 antagonism inhibits cocaine reinforcement and relapse by elevation of extracellular glutamate in the nucleus accumbens via a CB1 receptor mechanism. [PDF]
, 2018 Metabotropic glutamate receptor 5 (mGluR5) antagonism inhibits cocaine self-administration and reinstatement of drug-seeking behavior. However, the cellular and molecular mechanisms underlying this action are poorly understood.
Bi, Guo-Hua +9 more
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Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function [PDF]
, 2006 Following inducible expression in HEK293 cells, the human orexin-1 receptor was targeted to the cell surface but became internalized following exposure to the peptide agonist orexin A.
Canals Buj, M. +4 more
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Dynamic regulation of quaternary organization of the M1 muscarinic receptor by subtype-selective antagonist drugs [PDF]
, 2016 Although rhodopsin-like G protein-coupled receptors can exist as both monomers and non-covalently associated dimers/oligomers, the steady-state proportion of each form and whether this is regulated by receptor ligands is unknown.
Godin, Antoine G. +4 more
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Rates and equilibria for a photoisomerizable antagonist at the acetylcholine receptor of Electrophorus electroplaques. [PDF]
, 1985 Voltage-jump and light-flash experiments have been performed on isolated Electrophorus electroplaques exposed simultaneously to nicotinic agonists and to the photoisomerizable compound 2,2'-bis-[α-(trimethylammonium)methyl]-azobenzene (2BQ).
Mauri E. Krouse +3 more
openalex +5 more sources
Effects of NAD at purine receptors in isolated blood vessels [PDF]
, 2014 Nicotinamide adenine dinucleotide (NAD) belongs to the family of naturally occurring adenine dinucleotides, best known for their various intracellular roles.
Alefishat, Eman +2 more
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