Comparisons of hallucinogenic phenylisopropylamine binding affinities at cloned human 5-HT2A, 5-HT2B and 5-HT2C receptors

A notable positive correlation (r>0.9) exists between the affinities of 17 phenylisopropylamines at human 5-HT2A, 5-HT2B, and 5-HT2C receptors.

• Structural modifications in phenylisopropylamines resulted in small differences in affinity for 5-HT2B receptors, with a range of only about 50-fold.
• There is a significant correlation (r>0.9, n=8) between 5-HT2B receptor affinity and human hallucinogenic potency.
• Despite the binding affinities to 5-HT2B receptors, 5-HT2A receptors are likely to play a more prominent role in the behavioral effects of hallucinogens.
• Previous findings indicate that antagonists targeting 5-HT2A and 5-HT2C receptors block the stimulus effects of hallucinogenic phenylisopropylamines.

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