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Can I read Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT~2A~ Receptor Agonist on EtoBox?
Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT~2A~ Receptor Agonist by Emil Marcher-Rørsted; Jitka Nykodemová; Kasper Harpsøe; Anders A. Jensen; Jesper L. Kristensen is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT~2A~ Receptor Agonist about?
The N-benzylphenethylamines (NBOMes) are a class of ligands from which compounds with impressive selectivity for the serotonin 2A receptor (5-HT 2A R) over the closely related serotonin 2C receptor (5-HT 2C R) have emerged. These include 4-(2-((2hydroxybenzyl)amino)ethyl)-2,5-dimethoxybenzonitrile (25CN-NBOH, 1) and 2-(2,5-dimethoxy-4-bromobenzyl)-6-(2-methoxyphenyl)piperidine (DMPMBB, 2). The present work entails the synthesis and characterization of ligands wherein the structures of these two molecules have been fused. The desired compounds were accessed by a six-step synthetic procedure followed by the chiral resolution of the resulting racemic mixtures, giving one active ((S,S)-3) and three essentially inactive stereoisomers. In silico experiments support that one of the four possible stereoisomers would be active. Further in silico investigations showed that 1, 2, and (S,S)-3 share a common binding mode, further supporting the shared stereochemistry between the active enantiomer ((S,S)-3) and 2.
Who reads Introducing Conformational Restraints on 25CN-NBOH: A Selective 5-HT~2A~ Receptor Agonist?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Emil Marcher-Rørsted; Jitka Nykodemová; Kasper Harpsøe; Anders A. Jensen; Jesper L. Kristensen
- Publisher
- American Chemical Society (ACS)
- Published
- 2023
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)