Glucocorticoid receptor antagonist drugs
Is serotonin an agonist or antagonist?
Both antagonists and agonists act on the post-synaptic neuron. Antagonists and agonists will "pretend" to be serotonin and engage the 5-HT receptors. The agonist will activate the receptor as serotonin would and the antagonist will not activate the receptor but will block serotonin from from acting on the receptor.
What is the primary glucocorticoid?
A glucocorticoid is a type of steroid hormone which is produced in the cortex of the adrenal gland: cortisol is probably the most well known and common example of a glucocorticoid.
Is Singulair a glucocorticoid?
Singulair ( montelukast) and Flonase (fluticasone) are used to treat allergic rhinitis. Singulair is also used in to treat asthma and to prevent exercise-induced narrowing of the airways. Singulair and Flonase belong to different drug classes. Singulair is a leukotriene receptor antagonist and Flonase is glucocorticoid.
What is the agonist and antagonist?
In pharmacology the term agonist-antagonist or mixed agonist/antagonist is used to refer to a drug which under some conditions behaves as an agonist (a substance that fully activates the receptor that it binds to) while under other conditions, behaves as an antagonist (a substance that binds to a receptor but does not activate and can block the ...
[PDF File]Effect of the glucocorticoid receptor antagonist RU486 on ...
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RESEARCH ARTICLE Effect of the glucocorticoid receptor antagonist RU486 on MK-801 induced behavioural sensitisation Emilia M. Lefevre1, Gregory A. Medley1,2, Timothy Reeks1, Suzy Alexander1,2, Thomas H. J. Burne1,2, Darryl W. Eyles1,2* 1 Queensland Brain Institute, The University of Queensland, St Lucia, Queensland, Australia, 2 Queensland Centre for Mental …
[PDF File]Glucocorticoid receptor signaling in health and disease
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Glucocorticoid receptor signaling in health and disease Mahita Kadmiel and John A. Cidlowski ... glucocorticoids are drugs that resemble natu-ral glucocorticoids. Prednisone/prednisolone, dexametha- ... bind glucocorticoid agonists, one antagonist, RU486 (mifepristone), has been shown to bind to hGRb and regu- ...
[PDF File]Mifepristone, a Glucocorticoid Receptor Antagonist ...
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Mifepristone, a Glucocorticoid Receptor Antagonist, Produces Clinical and Metabolic Benefits in Patients with Cushing’s Syndrome Maria Fleseriu, Beverly M. K. Biller, James W. Findling, Mark E. Molitch, David E. Schteingart, and Coleman Gross, on behalf of the SEISMIC Study Investigators
[PDF File]Review Glucocorticoid antagonists in neuropsychotic …
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Synthetic mineralocorticoid receptor agonists – e.g., fludrocor-tisone – can increase blood pressure and are used to treat orthostatic hypotension; in contrast the antagonist, spiranolac-tone, is used to treat hypertension. Glucocorticoid receptors can be activated by administering high doses of cortisol or
[DOC File]Drug/Application
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Which of the following drugs finds use in the treatment of nausea and emesis (5 pts ea) Dimenhydramine. Finasteride. Scopolamine. Metoclopramide. Ceterizine. Pirenzepine. High glucocorticoid concentrations during therapy lead also to the stimulation of mineralcorticoid receptor, causing Na+ and water retention and consequently hypertension.
[DOC File]1 .edu
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Katz ER, Stowe ZN, Newport DJ, Kelley ME, Pace TW, Cubells JF, Binder EB. Regulation of mRNA expression encoding chaperone and co-chaperone proteins of the glucocorticoid receptor in peripheral blood: Association with depressive symptoms during pregnancy. Psychol Med, 42(5) 943-56, 2012. PMID:21995950
Regarding chapter, we could
cortisol (11(-hydroxylase) Fludrocortisone Mineralocorticoid deficiency HTN, hypokalemia 10X affinity for MR than GR Spironolactone MR antagonist Mineralocorticoid excess Hyperkalemia, hyperchloremia High doses inhibit AR Calcium homeostasis Calcitriol 1,25-(OH)2-vit.D Vit.D-dependent rickets
[DOCX File]SEDA-19 - CEBM
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Antidepressants which increase serotonin cause increases in glucocorticoid receptor number and can reverse the increased glucocorticoid secretion seen in depressed humans and in transgenic mice who have been genetically altered to demonstrate reduced glucocorticoid receptors and increased glucocorticoid secretion (partial GR knockout) (Barden ...
[DOC File]Drug Name
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For each type of receptor, there is a specific group of drugs or endogenous substances (known as ligands) that are capable of binding to the receptor, producing a pharmacological effect. ... (glucocorticoid and mineralocorticoid) ... agonist, a 5HT reuptake inhibitor and releaser, a noradrenaline reuptake inhibitor, an NMDA receptor antagonist ...
[DOCX File]van Kammen DP, Kelley M. Dopamine and norepinephrine ...
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, Gallagher M. Evaluation of hypothalamic-pituitary-adrenal axis function and hippocampal glucocorticoid receptor expression in behaviorally characterized young and aged rats. Euro J Neuroscience 2001 14 1739-1751. 16. Nicolle M, Gonzalez J, Sugaya K, Bryan D, Lund PK
[DOC File]Pharmacy Benefits Management Services Home
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H2 receptor antagonist; blocks HCl release from parietal cells ... Dexamethazone Anti-emetic at high mg doses Glucocorticoid: acts as CNS membrane stabilizer (?) Ondansetron (Zofran®) and other “-setron” drugs Used to prevent chemotherapy-induced vomiting. Blocks 5-HT3 receptors on afferent vagal terminals in upper GI tract, at the CTZ ...
[DOC File]398 Form Pages
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Drugs. Mechanism of Action. Anti-Tuberculosis Drugs. Tuberculocidal. Isoniazid . CYP450 Inhibitor . Metabolize through acetylation, highly genetic polymorphism . Side Effects . Peripheral neuropathy – supply Vit B6. Hepatotoxic . Mycolic Acid synthesis inhibitor . Spectrum of Activities . Kill extracellular bacteria . Weakens intracellular ...
[DOC File]Drug
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Acetylcholine receptor antagonist. Muscarinic antagonist side effects: Atropine - from belladonna or jimson weed plants. ... (Sympatholytic drugs) HTN. Cardiac arrhythmias (AF - after cardiac inversion) ... Diagnostic agent to suppress endogenous secretion of mineralcorticoid activity Potent glucocorticoid.
Selective glucocorticoid receptor modulator - Wikipedia
At low doses, mifepristone is a selective antagonist of the progesterone receptor. At higher doses, it blocks the glucocorticoid receptor. Mifepristone has more than 3x the binding affinity to the glucocorticoid receptor than dexamethasone. It has little affinity for the mineralocorticoid receptor. Pharmacokinetics
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