What question did this study set out to answer?

To evaluate the binding affinities and selectivity profiles of 21 indolealkylamine derivatives across 5-HT1A, 5-HT2A, and 5-HT2B receptor recognition sites.

March 1, 1990NeuropharmacologyOpen Access

Differential interactions of indolealkylamines with 5-hydroxytryptamine receptor subtypes

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Authors

DMDennis J. McKennaScience Museum of Minnesota DRDavid B. RepkeRoche (United States)LLLindsay A. LoUniversity of Toronto

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Implication

In vitro assay reveals high-affinity binding of 4-hydroxy indolealkylamines to 5-HT2A receptors in mammalian cortex, suggesting a key role in hallucinogenic action.

Key Points

To evaluate the binding affinities and selectivity profiles of 21 indolealkylamine derivatives across 5-HT1A, 5-HT2A, and 5-HT2B receptor recognition sites.
Assessed 21 indolealkylamine derivatives using radioligand competition assays with [125I]R-(-)DOI in rat cortex (5-HT2A) and [3H]ketanserin in bovine cortex (5-HT2B), alongside 5-HT1A binding sites.
4-hydroxylated derivatives demonstrated 25- to 380-fold selectivity for 5-HT2A sites over 5-HT1A sites, whereas 5-substituted derivatives exhibited approximately equal affinity across both subtypes.
All tested compounds showed lower affinities at the 5-HT2B site (>300 nM), and 6-substituted derivatives showed micromolar (>1 µM) affinities across all evaluated serotonin receptor sites.
N,N-dialkyl substituents larger than N,N-diisopropyl caused a marked reduction in binding affinity at both 5-HT2A and 5-HT1A recognition sites.

Cite This Study

McKenna et al. (1990) studied this question.

synapsesocial.com/papers/6aa93d9aa9624f76b4cdcda9 https://doi.org/10.1016/0028-3908(90)90001-8

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Implication

In vitro assay reveals high-affinity binding of 4-hydroxy indolealkylamines to 5-HT2A receptors in mammalian cortex, suggesting a key role in hallucinogenic action.

Differential interactions of indolealkylamines with 5-hydroxytryptamine receptor subtypes

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Implication

Key Points

Cite This Study

Differential interactions of indolealkylamines with 5-hydroxytryptamine receptor subtypes

Discussion

Member takes

Implication

Key Points

Cite This Study

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