Gmeiner P, Hübner H (2000)
Publication Type: Journal article
Publication year: 2000
Publisher: American Chemical Society
Book Volume: 43
Pages Range: 4563-4569
DOI: 10.1021/jm0009989
Traceless linking of diethoxymethyl (DEM)-protected 5- and 6-cyanoindoles and subsequent incorporation of phenylpiperazine derivatives led to the 2- and 3-piperazinylmethyl-substituted cyanoindoles 3a-m. Dopamine receptor binding studies on the final products 3a-m clearly indicated strong and selective recognition of the D4 subtype which is known as a promising target for the treatment of neuropsychiatric disorders. The most interesting binding properties were observed for the 2-aminomethyl-5-cyanoindoles FAUC 299 (3f) and FAUC 316 (3j) (Ki = 0.52 and 1.0 nM, respectively) when the fluoro derivative 3j proved extraordinary selectivity over D1, D2long, D2short, and D3 (>8600). To determine ligand efficacy, mitogenesis experiments were performed indicating partial agonist effects for the test compounds 3fj (35% and 30%, when compared to the full agonist quinpirole).
APA:
Gmeiner, P., & Hübner, H. (2000). Cyanoindole Derivatives as Highly Selective Dopamine D4 Receptor Partial Agonists: Solid-Phase Synthesis, Binding Assays, and Functional Experiments. Journal of Medicinal Chemistry, 43, 4563-4569. https://doi.org/10.1021/jm0009989
MLA:
Gmeiner, Peter, and Harald Hübner. "Cyanoindole Derivatives as Highly Selective Dopamine D4 Receptor Partial Agonists: Solid-Phase Synthesis, Binding Assays, and Functional Experiments." Journal of Medicinal Chemistry 43 (2000): 4563-4569.
BibTeX: Download