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