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Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT_2A and 5-HT_2B serotonin receptors.

ABSTRACT: Certain 4-substituted analogs of 1-(2,5-dimethoxyphenyl)isopropylamine (2,5-DMA) are psychoactive classical hallucinogens or serotonergic psychedelic agents that function as human 5-HT_2A (h5-HT_2A) serotonin receptor agonists. Activation of a related receptor population, h5-HT_2B receptors, has been demonstrated to result in adverse effects including cardiac valvulopathy. We previously published on the binding of several such agents at the two receptor subtypes. We hypothesized that, due to their structural similarity, the 5-HT_2A and 5-HT_2B receptor affinities of these agents might be related, and that QSAR studies might aid future studies. For a series of 13 compounds, it is demonstrated here that i) their published rat brain 5-HT₂

SUBMITTER: Hemanth P

PROVIDER: S-EPMC9902381 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature

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Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT_2A and 5-HT_2B serotonin receptors.

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Dataset Information

Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT2A and 5-HT2B serotonin receptors.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT_2A and 5-HT_2B serotonin receptors.