Which carbon is methylated to increase muscarinic selectivity in acetylcholine derivatives?

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Multiple Choice

Which carbon is methylated to increase muscarinic selectivity in acetylcholine derivatives?

Explanation:
Methylation at the beta-carbon changes how the molecule sits in the receptor binding sites, biasing toward muscarinic receptors. The beta-carbon is the second carbon away from the positively charged nitrogen in the cholinergic molecule. Nicotinic receptors require a particular chain length and conformation to fit their binding pocket, so adding a methyl at beta can hinder that fit, reducing nicotinic activity. Muscarinic receptors, on the other hand, tolerate or even prefer this kind of bulk in their binding region, so the modification preserves or enhances muscarinic binding. That makes beta-carbon methylation the best way to increase muscarinic selectivity.

Methylation at the beta-carbon changes how the molecule sits in the receptor binding sites, biasing toward muscarinic receptors. The beta-carbon is the second carbon away from the positively charged nitrogen in the cholinergic molecule. Nicotinic receptors require a particular chain length and conformation to fit their binding pocket, so adding a methyl at beta can hinder that fit, reducing nicotinic activity. Muscarinic receptors, on the other hand, tolerate or even prefer this kind of bulk in their binding region, so the modification preserves or enhances muscarinic binding. That makes beta-carbon methylation the best way to increase muscarinic selectivity.

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