Abstract
Several new 2-vinyl-Nb,Nb-dimethyltryptamines were prepared using Fischer indole synthesis followed by simple functional group transformations and evaluated on 5-HT4, 5-HT5, 5-HT6 and 5-HT7 serotonin receptors. It was found that 2-vinyl substitution conferred a potent and selective 5-HT6 binding activity to these molecules which could be enhanced by Na-arylsulfonyl substituents.
MeSH terms
-
Animals
-
Binding Sites
-
CHO Cells
-
Cricetinae
-
Drug Evaluation, Preclinical
-
Guinea Pigs
-
Humans
-
Indoles / chemical synthesis
-
Indoles / chemistry
-
Ligands
-
Male
-
Molecular Structure
-
Receptors, Serotonin / drug effects*
-
Stereoisomerism
-
Structure-Activity Relationship
-
Tryptamines / chemical synthesis
-
Tryptamines / chemistry
-
Tryptamines / pharmacology*
-
Vinyl Compounds / chemical synthesis
-
Vinyl Compounds / chemistry
-
Vinyl Compounds / pharmacology*
Substances
-
Indoles
-
Ligands
-
Receptors, Serotonin
-
Tryptamines
-
Vinyl Compounds
-
serotonin 6 receptor