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4,6-Di(heteroaryl)-2-(N-methylpiperazino)pyrimidines as New, Potent 5-HT2A Receptor Ligands: A Verification of the Topographic Model

Mokrosz, M. J. ; Strekowski, L. ; Kosak, W. X. ; Duszynska, B. ; Bojarski, A. J. ; Klodzinska, A. ; Czarny, A. ; Cegla, M. T. ; Deren-Wesolek, A. ; Chojnacka-Wojcik, E. ; Dove, Stefan ; Mokrosz, J. L.


A series of new 4,6-di(heteroaryl)pyrimidines containing an N-methylpiperazino group (6-13) or an ethylenediamine chain (15-20) in position 2 were synthesized and their 5-HT1A and 5-HT2A receptor affinities were determined. It was shown that the substituent effects on the 5-HT2A affinity are additive and could be described quantitatively. In a behavioral model it was also demonstrated that 6-11 ...


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