A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists. Export

@article{citeulike:3815392, abstract = {A series of potent 4-substituted tetrahydroquinolines has been synthesized and biologically tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [3H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when additional hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism.}, author = {Dannhardt, G. and von Gruchalla, M. and Kohl, B. K. and Parsons, C. G.}, citeulike-article-id = {3815392}, citeulike-linkout-0 = {http://view.ncbi.nlm.nih.gov/pubmed/11008377}, citeulike-linkout-1 = {http://www.hubmed.org/display.cgi?uids=11008377}, issn = {0365-6233}, journal = {Archiv der Pharmazie}, keywords = {nmda, nr1}, month = {August}, number = {8}, pages = {267--274}, posted-at = {2008-12-21 13:11:26}, priority = {2}, title = {A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists.}, url = {http://view.ncbi.nlm.nih.gov/pubmed/11008377}, volume = {333}, year = {2000} }

TY - JOUR ID - citeulike:3815392 L3 - citeulike-article-id:3815392 N2 - A series of potent 4-substituted tetrahydroquinolines has been synthesized and biologically tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [3H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when additional hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism. IS - 8 JF - Archiv der Pharmazie SN - 0365-6233 EP - 274 TI - A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists. VL - 333 SP - 267 KW - nmda KW - nr1 AU - Dannhardt, G AU - von Gruchalla, M AU - Kohl, BK AU - Parsons, CG PY - 2000/08// UR - http://view.ncbi.nlm.nih.gov/pubmed/11008377 ER -