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20 Cards in this Set
- Front
- Back
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Mineralocorticoid receptor agonists (2)
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1.) aldosterone
2.) corticosterone |
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MOA of MC
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Steroid binds to receptor (HSP off), complex translocates to the nucleus to interact with DNA, makes Na/K ATPase to kick out potassium and retain Na and H2O
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21-OH amino acid + interaction (2)
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1.) Asn (C=O, H-bond acceptor);
2.) Thr (-OH, H-bond donor) |
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3-keto amino acid + interaction (2)
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1.) Gln (C=O-NH2, H-bond donor)
2.) Arg (N=H, h-bond donor) |
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11beta-OH interaction and aa
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11beta-OH is a DONOR. Need Asn (C=O) like in 21-OH
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17alpha-OH
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Gln (like 3-keto)
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GC synthesis
a.) hypothalamus b.) anterior pituitary c.) end organ |
a.) hypothalamus releases CRF (corticotropin releasing factor) to the anterior pituitary
b.) anterior pituitary makes peptide hormones like corticotropin and ACTH to the adrenal gland c.) Adrenal gland has cholesterol that gets oxidized to make glucocorticoids |
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11-oxo oxidation/reduction
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to 11B-OH: 11Bhydroxysteroid dehydrogenase
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Metabolism of glucocorticoid (2)
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1.) 11beta hydroxysteroid dehalogenase (changes OH to 11-oxo)
2.) 5beta dehydrogenase saturates the 4-ene and makes it inactive (U-shape, not flat, cis) |
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What significantly increases both GC and MC?
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9alpha fluro or Cl (counter with 16 alpha OH)
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What significantly decreases MC?
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16alpha OH (counter with (alpha F)
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What halogen doubles GC?
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6alpha fluro
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Groups that decrease metabolism (3)
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1.) 9alpha fluro only: decreases oxidation of 11B-OH to ketone (11Bhydroxysteroid dehalogenase)
2.) 6alpha methyl: decreases 4-ene reduction 3.) 16alpha or beta methyl |
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6alpha methyl
1.) GC:MC 2.) duration |
1.) SLIGHT increase in GC. Max MC decrease if combo with C-16 sub
2.) decreases reduction of 4-ene |
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16alpha or beta methyl
a.) duration |
decreases metabolism of 17B-ketol
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How to stop oxidation of 11B-OH?
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add 9alphafluro
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9alpha chlorine
a.) GC:MC |
Significantly increases GC and MC
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Which groups need a combo C-16sub for max decrease in MC?
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6alpha fluro, 6alphamethyl
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21-Cl
a.) GC:MC |
increase lipophilicity via dipole-dipole, increase GC only
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6alpha Cl
a.) GC:MC |
no GC: decrease MC
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