ms-245 has been researched along with tryptamine* in 1 studies
1 other study(ies) available for ms-245 and tryptamine
Article | Year |
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Conformationally constrained N1-arylsulfonyltryptamine derivatives as 5-HT6 receptor antagonists.
Several series of conformationally constrained N1-arylsulfonyltryptamine derivatives were prepared and tested for 5-HT6 receptor binding affinity and ability to modulate cAMP production in a cyclase assay. The 3-piperidin-3-yl-, 3-(1-methylpyrrolidin-2-ylmethyl)-, and 3-pyrrolidin-3-yl-1H-indole arrays (8-13) appear to be able to adopt a conformation that allows high affinity 5-HT6 receptor binding, while the beta-carboline array 14 binds with a significantly weaker (10- to 100-fold) affinity. N1-Benzenesulfonyl-3-piperidin-3-yl-1H-indole 9a is a high affinity full agonist with EC50 = 24 nM. Several of the N1-arylsulfonyl-3-(1-methylpyrrolidin-2-ylmethyl)-1H-indole derivatives behave as very potent antagonists ((S)-11r, (S)-11t; IC50 = 0.8, 1.0 nM). Topics: Adenylyl Cyclases; Cyclic AMP; Humans; Molecular Conformation; Protein Binding; Receptors, Serotonin; Serotonin Antagonists; Serotonin Receptor Agonists; Structure-Activity Relationship; Tryptamines | 2005 |