Question

In etheylene bridge incorporation of beta-substitution leads to reduction​

Answer 1

Answer:

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Answer 2

Ethylene bridge incorporation

Explanation:

• The ethylene bridge has been modified.
• The muscarinic potency of acetylmethylcholine HO H (methacholine) is about (R) comparable to that of acetylcholine, with substantially stronger (S) (S) N+(CH3)3 Cl muscarinic than nicotinic selectivity (S) (S) N+(CH3)3 Cl muscarinic than nicotinic selectivity (S) (S) N+(CH3)3 Cl  

• Cholinesterase rapidly hydrolyzes the methyl ester to choline and acetic acid.
• Carbamate esters of choline (carbachol) were created to lower susceptibility to hydrolysis and were found to be more stable than carboxylate esters.

• The -substitution in the choline moiety reduces both nicotinic and muscarinic activity, but muscarinic activity is reduced more than nicotinic activity.

• The incorporation of -substitution results in a larger reduction of nicotinic activity.