Mokrosz, Maria J. and Strekowski, Lucjan and Kozak, Wei Xing and Duszyńska, Beata and Bojarski, Andrzej J. and Kłodzinska, Aleksandra and Czarny, Agnieszka and Cegła, Marek T. and Dereń-Wesołek, Anna and Chojnacka-Wójcik, Ewa and Dove, Stefan and Mokrosz, Jerzy 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. ISSN 0365-6233, 1521-4184
Full text not available from this repository.Abstract
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 (d(1) = 5.2-8.4 Angstrom, d(2) = 5.7-8.5 Angstrom, and d(3) = 4.6-7.3 Angstrom) define the molecular topography of the 5-HT2A receptor antagonists under study.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | CONFORMATIONAL-ANALYSIS; PARAMETERS; AFFINITY; DNA; 4,6-di(heteroaryl)-2-(N-methylpiperazino)pyrimidines; structure-5-HT2A affinity relationships; 5-HT2A receptor antagonists; topographic model of 5-HT2A receptors |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 16 Jan 2024 06:51 |
| Last Modified: | 16 Jan 2024 06:51 |
| URI: | https://pred.uni-regensburg.de/id/eprint/52324 |
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