Details

Autor(en) / Beteiligte

• CHANG-FONG, Jean
• RANGISETTY, Jagadeesh B
• DUKAT, Malgorzata
• SETOLA, Vincent
• RAFFAY, Thomas
• ROTH, Bryan
• GLENNON, Richard A

Titel

1,2,3,4-tetrahydrocarbazoles as 5-HT6 serotonin receptor ligands

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2004-04, Vol.14 (8), p.1961-1964

Ort / Verlag

Oxford: Elsevier

Erscheinungsjahr

2004

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• An investigation of the structure-affinity relationships for the binding of 4-(N,N-dimethylaminomethyl)-N(9)-arylsulfonyl-9H-1,2,3,4-tetrahydrocarbazoles (conformationally-constrained analogues of the benzenesulfonyltryptamine 5-HT(6) antagonist MS-245) at human 5-HT(6) receptors revealed that various arylsulfonyl substituents are tolerated and that the 4-(N,N-dimethylaminomethyl) group is not required for binding. In particular, N(9)-(4-aminobenzenesulfonyl)-9H-1,2,3,4-tetrahydrocarbazole (20, K(i)=29 nM) was found to bind with high affinity and represents the first member of a new structural class of agents with 5-HT(6) antagonist properties (pA(2)=7.0; cAMP hydrolysis assay).