Mokrosz, M.J. and Strekowski, L. and Kosak, W.X. and Duszynska, B. and Bojarski, A.J. and Klodzinska, A. and Czarny, A. and Cegla, M.T. and Deren-Wesolek, A. and Chojnacka-Wojcik, E. and Dove, Stefan and Mokrosz, J.L. (1995) 4,6-Di(heteroaryl)-2-(N-methylpiperazino)pyrimidines as New, Potent 5-HT2A Receptor Ligands: A Verification of the Topographic Model. Archiv der Pharmazie 328 (9), pp. 659-666.
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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 are 5-HT2A receptor antagonists. The molecular modelling results suggested that the distances between the basic nitrogen atom and the two aromatic centers (d1 = 5.2-8.4 Å, d2 = 5.7-8.5 Å, and d3 = 4.6-7.3 Å) define the molecular topography of the 5-HT2A receptor antagonists under study.
|Institutions:||Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)|
|Subjects:||500 Science > 570 Life sciences|
500 Science > 540 Chemistry & allied sciences
|Refereed:||Yes, this version has been refereed|
|Created at the University of Regensburg:||Partially|
|Owner:||Prof. Dr. Stefan Dove|
|Deposited On:||20 Jan 2009 15:55|
|Last Modified:||05 Aug 2009 13:50|