Structure-Activity Relationship (SAR) of the Phenethylamines: A ...
Structure-Activity Relationship (SAR) of the Phenethylamines: A ...
Structure-Activity Relationship (SAR) of the Phenethylamines: A ...
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Just Nine Little Carbons…<br />
2-Carbon<br />
Bridge<br />
Amine<br />
(Basic N)<br />
Aromatic<br />
Ring<br />
Phenethylamine Description<br />
• Alpha-methylphenethylamine<br />
• Amphetamine<br />
• Alpha-methylphenethylamine<br />
• 1-phenyl-2-aminopropane<br />
• Phenylisopropylamine<br />
Initial <strong>SAR</strong><br />
β <br />
α <br />
2-Phenethylamine<br />
Amphetamine<br />
• 2-Phenethylamine largely lacks CNS<br />
effects with systemic administration<br />
• Little difference in lipophilicity between <strong>the</strong><br />
two compounds<br />
• Both are capable <strong>of</strong> CNS penetration<br />
2
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