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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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
core +2 more sources
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
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Frontiers in Immunology, 2023 Chemokine G-protein coupled receptors are validated drug targets for many diseases, including cancer, neurological, and inflammatory disorders. Despite much time and effort spent on therapeutic development, very few chemokine receptor antagonists are ...
Patrick Grudzien +3 more
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Vasopressin receptor antagonists [PDF]
Kidney International, 2006 The first non-peptide vasopressin receptor antagonist (VRA) was recently approved by the United States Food and Drug Administration, and several others are now in late stages of clinical development. Phase 3 trials indicate that these agents predictably reduce urine osmolality, increase electrolyte-free water excretion, and raise serum sodium ...
Greenberg, A., Verbalis, J.G.
openaire +2 more sources
Kinin-B1 receptors in ischaemia-induced pancreatitis: Functional importance and cellular localisation [PDF]
, 2003 In this study we compare the role of kininB1 and B2 receptors during ischaemia/reperfusion of rat pancreas. Our investigations were prompted by the observation that infusion of a kininB2 receptor antagonist produced significant improvement in acute ...
Ahluwalia A. +9 more
core +1 more source
Aldosterone receptor antagonists [PDF]
Annales d'Endocrinologie, 2021 Blocking the mineralocorticoid receptor (MR) is one of the most effective ways of reducing blood pressure in patients with resistant hypertension and improving cardiovascular prognosis in patients with heart failure with reduced ejection fraction and left ventricular dysfunction after myocardial infarction.
openaire +3 more sources
The relevance of theobromine for the beneficial effects of cocoa consumption
Frontiers in Pharmacology, 2015 Cocoa consumption began in America and in the mid 16th Century it quickly spread to Europe. Beyond being considered a pleasant habit due to its rich sweet lingering taste, chocolate was considered a good nutrient and even a medicine.
Eva eMartínez-Pinilla +2 more
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Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands [PDF]
, 2015 Short chain fatty acids (SCFAs) are produced in the gut by bacterial fermentation of poorly digested carbohydrates. A key mediator of their actions is the G protein-coupled Free Fatty Acid 2 (FFA2) receptor and this has been suggested as a therapeutic ...
Hansen, Anders Højgaard +6 more
core +2 more sources
The Tricyclic Antidepressant Clomipramine Increases Plasma Glucose Levels of Mice
Journal of Pharmacological Sciences, 2003 : Effects of the tricyclic antidepressant clomipramine on plasma glucose levels in mice were studied. Clomipramine at doses ranging 5 – 20 mg/kg elicited significant hyperglycemia in mice.
Yumi Sugimoto, Kiyo Inoue, Jun Yamada
doaj +1 more source