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Structure activity relationships of 5-HT_2B and 5-HT_2C serotonin receptor antagonists: N⁶, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.

ABSTRACT: (N)-Methanocarba adenosine derivatives were structurally modified to target 5-HT_2B serotonin receptors as antagonists, predominantly containing branched N⁶-alkyl groups. N⁶-Dicycloalkyl-methyl groups, including their asymmetric variations, as well as 2-iodo, were found to generally favor 5-HT₂Rs, while only N⁶-dicyclohexyl-methyl derivative 35 showed weak 5-HT_2AR affinity (K_i 3.6 μM). The highest 5-HT_2BR affinities were K_i 11-23 nM (N⁶-dicyclopropyl-methyl-2-iodo 11, 2-chloro-5'-deoxy-5'-methylthio 15 and N⁶-((R)-cyclobuty-cyclopropyl-methyl)-2-iodo 43), and K_i 73 nM at 5-HT_2CR for 36. Direct comparison of adenine ribosides and their corresponding r

SUBMITTER: Tosh DK

PROVIDER: S-EPMC10529765 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature

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Structure activity relationships of 5-HT_2B and 5-HT_2C serotonin receptor antagonists: N⁶, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.

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Dataset Information

Structure activity relationships of 5-HT2B and 5-HT2C serotonin receptor antagonists: N6, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Structure activity relationships of 5-HT_2B and 5-HT_2C serotonin receptor antagonists: N⁶, C2 and 5'-Modified (N)-methanocarba-adenosine derivatives.