The following structure is more active than morphine as an analgesic. H3C H. CH3 H3C´ O Il.. O Il..

Biochemistry
6th Edition
ISBN:9781305577206
Author:Reginald H. Garrett, Charles M. Grisham
Publisher:Reginald H. Garrett, Charles M. Grisham
Chapter27: Metabolic Integration And Organ Specialization
Section: Chapter Questions
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The following structure is more active than morphine as an
analgesic.
H3C
CH3
H.
H3C'
O Il..
What is the principal reason for this?
The extra acetyl group binds to cell surface receptors improving
active internalization.
The acetyl groups mask a polar group allowing the structure to
cross the blood brain barrier more efficiently.
The extra acetyl group masks an alcohol group which would
otherwise undergo a phase Il metabolic conjugation reaction
leading to rapid excretion of the drug.
The acetyl groups increase the stability of the drug in the
cellular environment.
O Il..
Transcribed Image Text:The following structure is more active than morphine as an analgesic. H3C CH3 H. H3C' O Il.. What is the principal reason for this? The extra acetyl group binds to cell surface receptors improving active internalization. The acetyl groups mask a polar group allowing the structure to cross the blood brain barrier more efficiently. The extra acetyl group masks an alcohol group which would otherwise undergo a phase Il metabolic conjugation reaction leading to rapid excretion of the drug. The acetyl groups increase the stability of the drug in the cellular environment. O Il..
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