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

@inproceedings{Mokrosz199546Diheteroaryl2Nmethylpiperazinopy,
  title={4,6-Di(heteroaryl)-2-(N-methylpiperazino)pyrimidines as New, Potent 5-HT2A Receptor Ligands: A Verification of the Topographic Model},
  author={Maria J. Mokrosz and Lucjan Strekowski, and Werner Kosak and Beata Duszyńska and Andrzej J. Bojarski and Aleksandra Kłodzińska and Agnieszka Czarny and Marek T. Cegła and A. Dereń-Wesołek and E. Chojnacka-w{\'o}jcik and Stefan Dove and Jerzy L. Mokrosz},
  year={1995}
}
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… Expand
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References

Structure‐Activity Relationship Studies of CNS Agents, Part 25: 4,6‐Di(heteroaryl)‐2‐(N‐methylpiperazino)pyrimidines as New, Potent 5‐HT2A Receptor Ligands: A Verification of the Topographic Model
TLDR
A series of new 4,6‐di(heteroaryl)pyrimidines containing an N‐methylpiperazino group or an ethylenediamine chain in position 2 were synthesized and it was shown that the substituent effects on the 5‐HT2A affinity are additive and could be described quantitatively. Expand