Functional deficiency in endogenous interleukin‐1 receptor antagonist in patients with febrile infection‐related epilepsy syndrome
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DOI: 10.1002/ana.25439
Abstract: We recently reported successful treatment of a child with febrile infection‐related epilepsy syndrome (FIRES), a subtype of new onset refractory status epilepticus, with the recombinant interleukin‐1 (IL1) receptor antagonist (IL1RA) anakinra. On this basis, we… read more here.
Keywords: receptor antagonist; febrile infection; infection related; related epilepsy ... See more keywords
Clinical Formulation Bridging of Gefapixant, a P2X3‐Receptor Antagonist, for the Treatment of Chronic Cough
Sign Up to like & getrecommendations! Published in 2022 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.1105
Abstract: Gefapixant is a P2X3‐receptor antagonist being developed for treatment of refractory or unexplained chronic cough. Four phase 1 studies were conducted in healthy participants that bridged the early‐phase gefapixant formulation (F01) to the phase 3… read more here.
Keywords: receptor antagonist; formulation; chronic cough; p2x3 receptor ... See more keywords
Confirmation of the Cardiac Safety of PGF2α Receptor Antagonist OBE022 in a First‐in‐Human Study in Healthy Subjects, Using Intensive ECG Assessments
Sign Up to like & getrecommendations! Published in 2018 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.447
Abstract: OBE022, a new orally active prostaglandin F2α receptor antagonist (OBE022) with myometrial selectivity is being developed to reduce uterine contractions during preterm labor. This first‐in‐human study evaluated the effect of OBE022 following multiple doses on… read more here.
Keywords: receptor antagonist; study; effect; human study ... See more keywords
Safety, Pharmacokinetics, and Pharmacodynamics of Trazpiroben (TAK‐906), a Novel Selective D2/D3 Receptor Antagonist: A Phase 1 Randomized, Placebo‐Controlled Single‐ and Multiple‐Dose Escalation Study in Healthy Participants
Sign Up to like & getrecommendations! Published in 2021 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.906
Abstract: Gastroparesis is a chronic neuromuscular disorder of the upper gastrointestinal tract in which episodic exacerbation can lead to frequent hospitalizations and severe disability. Dopamine D2/D3 receptor antagonists have been used to treat patients with gastroparesis… read more here.
Keywords: receptor antagonist; trazpiroben tak; healthy participants; safety ... See more keywords
Safety and Dosing Study of a Cholecystokinin Receptor Antagonist in Non‐alcoholic Steatohepatitis
Sign Up to like & getrecommendations! Published in 2022 at "Clinical Pharmacology and Therapeutics"
DOI: 10.1002/cpt.2745
Abstract: High saturated fat diets have been shown to raise blood levels of cholecystokinin (CCK) and induce nonalcoholic steatohepatitis (NASH). CCK receptors are expressed on stellate cells and are responsible for hepatic fibrosis when activated. The… read more here.
Keywords: safety; receptor antagonist; steatohepatitis; fibrosis ... See more keywords
Combined treatment with a β3‐adrenergic receptor agonist and a muscarinic receptor antagonist inhibits detrusor overactivity induced by cold stress in spontaneously hypertensive rats
Sign Up to like & getrecommendations! Published in 2017 at "Neurourology and Urodynamics"
DOI: 10.1002/nau.23061
Abstract: This study determined if combined treatment with the muscarinic receptor (MR) antagonist solifenacin and the β3‐adrenergic receptor (AR) agonist mirabegron could inhibit detrusor overactivity induced by cold stress in spontaneously hypertensive rats (SHRs). read more here.
Keywords: receptor antagonist; receptor agonist; muscarinic receptor; receptor ... See more keywords
The leukotriene receptor antagonist montelukast and its possible role in the cardiovascular field
Sign Up to like & getrecommendations! Published in 2017 at "European Journal of Clinical Pharmacology"
DOI: 10.1007/s00228-017-2242-2
Abstract: BackgroundCysteinyl leukotrienes (LTC4, LTD4, and LTE4) are pro-inflammatory mediators of the 5-lipooxygenase (5-LO) pathway, that play an important role in bronchoconstriction, but can also enhance endothelial cell permeability and myocardial contractility, and are involved in… read more here.
Keywords: receptor antagonist; leukotriene receptor; antagonist montelukast; role ... See more keywords
Caspase-1 inhibition by VX-765 administered at reperfusion in P2Y12 receptor antagonist-treated rats provides long-term reduction in myocardial infarct size and preservation of ventricular function
Sign Up to like & getrecommendations! Published in 2018 at "Basic Research in Cardiology"
DOI: 10.1007/s00395-018-0692-z
Abstract: Patients with acute myocardial infarction receive a P2Y12 receptor antagonist prior to reperfusion, a treatment that has reduced, but not eliminated, mortality, or heart failure. We tested whether the caspase-1 inhibitor VX-765 given at reperfusion… read more here.
Keywords: reperfusion; infarction; p2y12 receptor; receptor antagonist ... See more keywords
Efficacy of mineralocorticoid receptor antagonist for central serous chorioretinopathy: a meta-analysis
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DOI: 10.1007/s10792-020-01479-1
Abstract: Purpose To evaluate the efficacy of mineralocorticoid receptor antagonist (MRA) for patients with central serous chorioretinopathy (CSCR). Methods The Pubmed, Embase, and the Cochrane Central Register of Controlled Trials were comprehensively searched up to February… read more here.
Keywords: receptor antagonist; central serous; efficacy; mineralocorticoid receptor ... See more keywords
Effects of Ketoconazole on the Pharmacokinetics of Mifepristone, a Competitive Glucocorticoid Receptor Antagonist, in Healthy Men
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DOI: 10.1007/s12325-017-0621-9
Abstract: IntroductionMifepristone, a competitive glucocorticoid receptor antagonist approved for Cushing syndrome, and ketoconazole, an antifungal and steroidogenesis inhibitor, are both inhibitors of and substrates for cytochrome P450 (CYP3A4). This study evaluated the pharmacokinetic effects of concomitant… read more here.
Keywords: receptor antagonist; mifepristone; exposure; period ... See more keywords
The Influence of H2-Receptor Antagonist Administration to the 24-h Uptake of I-131 in the Thyroid Gland
Sign Up to like & getrecommendations! Published in 2021 at "Nuclear Medicine and Molecular Imaging"
DOI: 10.1007/s13139-020-00676-1
Abstract: Purpose The aim of this study was to determine the influence of H2RAs to the 24-h I-131 uptake in the thyroid gland. Material and Methods A prospective study with quasi-experimental pre- and post-study design was… read more here.
Keywords: receptor antagonist; thyroid gland; uptake 131;