Biomedical Engineering Reference
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development of new ligands. Similar detailed information about GABA receptors are still awaited.
Many selective ligands have been developed as experimental tools and have been important for the
understanding of many brain functions and pathophysiological aspects. However, the success as
new therapeutic agents, especially within the Glu area, is still small. The knowledge about what
subtypes of receptors is involved in the neurological disorders is still limited, and further elucida-
tion of this and development of new subtype selective ligands may eventually lead to new and better
therapeutic agents.
FURTHER READINGS
A.C. Foster and J.A. Kemp, Glutamate- and GABA-based CNS therapeutics, Curr. Opin. Pharmacol . 2006,
6: 7-17.
B.H. Kaae, K. Harpsøe, J.S. Kastrup, A.C. Sanz, D.S. Pickering, B. Metzler, R.P. Clausen, M. Gajhede,
P. Sauerberg, T. Liljefors, and U. Madsen, Structural proof of a dimeric positive modulator bridging two
identical AMPA receptor-binding sites, Chem. Biol . 2007, 14: 1294-1303.
J.N.C. Kew and J.A. Kemp, Ionotropic and metabotropic glutamate receptor structure and pharmacology,
Psychopharmacology 2005, 179: 4-29.
C. Madsen, A.J. Jensen, T. Liljefors, U. Kristiansen, B. Nielsen, C.P. Hansen, M. Larsen, B. Ebert, B. Bang-Andersen,
P. Krogsgaard-Larsen, and B. Frølund, 5-Substituted imidazole-4-acetic acid analogues: Synthesis, mod-
eling and pharmacological characterization of a series of novel γ-aminobutyric acid receptor agonists.
J . Med. Chem . 2007, 50: 4147-4161.
U. Madsen, H. Bräuner-Osborne, J.R. Greenwood, T.N. Johansen, P. Krogsgaard-Larsen, T. Liljefors,
M. Nielsen, and B. Frølund, GABA and Glutamate receptor ligands and their therapeutic potential in
CNS disorders, in S.C. Gad (ed.) Drug Discovery Handbook , Wiley, Hoboken, 2005, pp. 797-907.
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