Effect of Bulky N-Dibenzofuranylmethyl Substitution on the 5-HT2 Receptor Affinity and Efficacy of a Psychedelic Phenethylamine.
ACS Chemical Neuroscience February 7, 2024 Breno A. Soares, Thirumal Yempala, Darío Martínez-afani et al. 4 citations
The introduction of arylmethyl substituents on the amine nitrogen atom of phenethylamines and tryptamines often results in profound increases in their affinity and functional activity at 5-HT2 serotonin receptors. To probe the sensitivity of this effect to substantially larger N-substituents, ten derivatives of the well-characterized psychedelic phenethylamine 2C-B were prepared by appending...
DOI: 10.1021/acschemneuro.3c00639 (opens in new tab)
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5-ht2 receptor agonism
5-ht2 receptor binding
Bulky n-substituents
Docking poses
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