Huber D, Löber S, Hübner H, Gmeiner P (2012)
Publication Language: English
Publication Type: Journal article, Original article
Publication year: 2012
Original Authors: Huber D., Lober S., Hubner H., Gmeiner P.
Publisher: Elsevier
Book Volume: 20
Pages Range: 455-466
Journal Issue: 1
DOI: 10.1016/j.bmc.2011.10.063
Merging two arylamidoalkyl substituted phenylpiperazines as prototypical recognition elements for dopamine D -like receptors by oligoethylene glycol linkers led to a series of bivalent ligands. These dimers were investigated in comparison to their monomeric analogues for their dopamine D , D , D and D receptor binding. Radioligand binding experiments revealed strong bivalent effects for some para-substituted benzamide derivatives. For the D subtype, the target compounds 32, 34 and 36 showed an up to 70-fold increase of affinity and a substantial enhancement of subtype selectivity when compared to the monovalent analogue 24. Analysis of the binding curves displayed Hill slopes very close to one indicating that the bivalent ligands displace 1 equiv of radioligand. Obviously, the two pharmacophores occupy an orthosteric and an allosteric binding site rather than adopting a receptor-bridging binding mode. © 2011 Elsevier Ltd. All rights reserved.
APA:
Huber, D., Löber, S., Hübner, H., & Gmeiner, P. (2012). Bivalent molecular probes for dopamine D2-like receptors. Bioorganic & Medicinal Chemistry, 20(1), 455-466. https://doi.org/10.1016/j.bmc.2011.10.063
MLA:
Huber, Daniela, et al. "Bivalent molecular probes for dopamine D2-like receptors." Bioorganic & Medicinal Chemistry 20.1 (2012): 455-466.
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