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Adrenocorticoid Info

Adrenocorticoid Structure Activity

QuestionAnswer
C and D rings are ________ important than A and B rings for receptor binding. More
Bulky substituents on the B-side of molecule ________ glycogenic activity, but not if on ..... abolishes, the alpha side
Needed components required for sodium retaining activity Alpha side interaction at the A, C, and D rings plus ketol side chain
Alpha methyl groups in position 6 and 16 ________ glucocorticoid activity. Increase
2 Alpha methyl _________ sodium retention Reduces
Important for drug - glucocorticoid receptor interaction 11 beta -OH
Increases glucocorticoid activity and slows oxidation of 11 beta -OH 9 alpha -F
Relationship from greatest to least glucocorticoid activity with 6 and 9 alpha -F and the presence of both 6 + 9 > 9 > 6
Relationship of urinary sodium increase with 9 alpha halogens F > Cl > Br
Relationship for topical inflammatory activity with 9 alpha halogens Br > Cl > F
Making the 17 alpha hydroxy an ester or tying it up as an acetonide _________ glucocorticoid receptor affinity and ___________ activity enhances, anti-inflammatory
Created by: gillesec
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