[MEDORG-LEC-SEMIS-02] STRUCTURAL MODIFICATION (SIDE-BY-SIDE SAR RULES)
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32 Terms
Increase muscarinic selectivity
Structural Change: Increase nitrogen bulk
Parasympathetic Agonists: ?
Prevents CNS entry
Structural Change: Quaternary ammonium
Parasympathetic Agonists: ?
Increase muscarinic selectivity
Structural Change: Add B-methyl group
Parasympathetic Agonists: ?
Produces antagonism
Structural Change: Add aromatic rings
Parasympathetic Agonists: ?
Not required
Structural Change: Catechol OH groups
Parasympathetic Agonists: ?
Little effect
Structural Change: Remove OH groups
Parasympathetic Agonists: ?
Increases stability
Structural Change: Carbamate substitution
Parasympathetic Agonists: ?
Reduce nicotinic effect
Structural Change: Bulky substituents
Parasympathetic Agonists: ?
Strengthens blockade
Structural Change: Increase nitrogen bulk
Parasympathetic Antagonists: ?
Peripheral-only drugs
Structural Change: Quaternary ammonium
Parasympathetic Antagonists: ?
Not applicable
Structural Change: Add B-methyl group
Parasympathetic Antagonists: ?
Essential for activity
Structural Change: Add aromatic rings
Parasympathetic Antagonists: ?
Not required
Structural Change: Catechol OH groups
Parasympathetic Antagonists: ?
Little effect
Structural Change: Remove OH groups
Parasympathetic Antagonists: ?
Sometimes used
Structural Change: Carbamate substitution
Parasympathetic Antagonists: ?
Increase antagonism
Structural Change: Bulky substituents
Parasympathetic Antagonists: ?
Increase B selectivity
Structural Change: Increase nitrogen bulk
Sympathetic Agonists: ?
Rare
Structural Change: Quaternary ammonium
Sympathetic Agonists: ?
Increases indirect activity
Structural Change: Add B-methyl group
Sympathetic Agonists: ?
Increases binding
Structural Change: Add aromatic rings
Sympathetic Agonists: ?
Increase potency, decreases duration
Structural Change: Catechol OH groups
Sympathetic Agonists: ?
Increase duration, Increase CNS entry
Structural Change: Remove OH groups
Sympathetic Agonists: ?
Not important
Structural Change: Carbamate substitution
Sympathetic Agonists: ?
Reduce agonism
Structural Change: Bulky substituents
Sympathetic Agonists: ?
Required for receptor blocking
Structural Change: Increase nitrogen bulk
Sympathetic Antagonists: ?
Sometimes used
Structural Change: Quaternary ammonium
Sympathetic Antagonists: ?
Not applicable
Structural Change: Add B-methyl group
Sympathetic Antagonists: ?
Essential
Structural Change: Add aromatic rings
Sympathetic Antagonists: ?
Usually removed
Structural Change: Catechol OH groups
Sympathetic Antagonists: ?
Improves lipophilicity
Structural Change: Remove OH groups
Sympathetic Antagonists: ?
Not important
Structural Change: Carbamate substitution
Sympathetic Antagonists: ?
Required for antagonism
Structural Change: Bulky substituents
Sympathetic Antagonists: ?
