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Adrenocorticoid Structure Activity

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Question
Answer
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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