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14 Cards in this Set
- Front
- Back
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Estrogen Receptor
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NR3A1, NR3A2
Ligand: 17-ß-Estradiol fn: maintenance of repro, CV, musculoskeletal systems Two isoforms: ER-alpha, ER-beta agonists: ethinyl estradiol, diethylstilbestrol antagonists: tamoxifen, clomiphene, fulvestant |
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Androgen Receptor
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NR3C4
ligand: dihydrotestosterone (DHT), testosterone fn: development and maintenance of the male repro tract. agonists: methyltestosterone, fluoxymesterone, stanozolol antagonists: bicalutamide, spironolactone |
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Progesterone Receptor
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NR3C3
ligand: progesterone fn: maintenance of uterus and mammary glands agonists: norethindrone, medroxyprogesterone antagonist: mifepristone |
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Glucocorticoid Receptor
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NR3C1
ligand: cortisol, hydrocortisone fn: stress response, glucose uptake, destruction of muscles and skeleton agonists: prednisone, betamethasone antagonist: mifepristone |
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Thyroid Hormone Receptors
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NR1A1/2
ligand: T3 and T4 fn: regulate metabolism agonists: T4, mixtures of T3 and T4 antagonists: none |
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Vitamin D receptor
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NR1L1
ligand: Vitamin D3 (calcitrol) fn: regulation of Calcium and phosphorous absorption and homeostasis, bone development, control of cell growth and development drugs: calcitrol, dihydrotachsterol antagonists: none |
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Mineralocorticoid Receptor
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NR3C2
ligand: aldosterone fn: slat and water balance, sodium reabsorption, electrolyte regulation agonist: fludrocortisone antagonist: spironolactone Cortisol can also be an agonist but 11ß-hydroxysteroid dehydrogenase is produced by the kidneys and degrades |
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Retinoic Acid Receptor
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NR1B1/2/3
ligand: all trans- and cis-9 retinoic acid fn: embryo dev, and maintenance of visual pigments and skin agonists: trans - retinoic acids antagonists: none |
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Retionoic acid x receptor
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NR2B1,2,3
ligand: 9-cis retinoic acid drugs: same as RAR; is the dimerization partner for group 1 drugs |
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peroxisome proliferator activated receptor
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NR1C1,2,3
ligand: select fatty acids, eicosanoids, prostanoids ppar- alpha: uptake, utilization, catabolism of fatty acids agonists: hypolipidemic agents ppar-beta: promotes formation fo type 1 muscle fibres drugs: none ppar-gamma: plays a role in fat cell differentiation agonists: thiazoladinediones, rosiglitazone antagonists: none |
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liver x receptors
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NR1H2/3
ligands: - cholesterol fn: controls cholesterol intestinal absorption, catabolism drugs: none |
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farnesoid X receptors
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NR1H4/5
ligands: bile acids fn: regs. bile acid home agonists: [unofficial] obeticholic acid (phase 2) antagonists: guugulsterone |
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Pregnane X receptor
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NR1L2
ligands: pregnane fn: promiscuous, has a large binding pocket and is very flexible -→ regulates phase 1 and 2 enzymes, esp CYP3A4, P-gp agonists: rifampcin, phenobarbital, nifedipine, antagonists: sulforphane |
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Constitutive Androstane Receptor
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NR1L3
lignad: no know high affin one; high concs. of bile acids and bilirubin act as agonists; steroids as inverse agonists: phenobarbital (through phosphorylation) antagonists: none inverse agonist: medizine |
