Löber S, Hübner H, Tschammer N, Gmeiner P (2011)
Publication Language: English
Publication Type: Journal article, Review article
Publication year: 2011
Original Authors: Lober S., Hubner H., Tschammer N., Gmeiner P.
Publisher: Elsevier
Book Volume: 32
Pages Range: 148-157
Journal Issue: 3
DOI: 10.1016/j.tips.2010.12.003
Dopamine D -like receptors (including D , D and D ) belong to the rhodopsin-like family of G protein-coupled receptors (GPCRs), which represent the largest group of targets for bioactive molecules. Due to their high sequence similarity, the design of subtype-selective ligands requires rational and effective strategies. The general formula of 1,4-disubstituted aromatic piperidines and piperazines (1,4-DAPs) was extracted from classical dopaminergic drugs. The biological properties of this compound family are encoded by an aromatic head group that controls intrinsic activity, an amine moiety and a lipophilic appendage. D - and D -selective molecular probes and drug candidates were generated from the general formula of 1,4-DAP. Formal structural rearrangement led to investigational drugs beyond the 1,4-DAP structure. The very recent publication of the X-ray crystal structure of D should facilitate efficient discovery of unprecedented chemotypes. However, the development of D -selective agonists, functionally selective ligands and the exploitation of homo- and heteromers remain challenging. © 2010 Elsevier Ltd.
APA:
Löber, S., Hübner, H., Tschammer, N., & Gmeiner, P. (2011). Recent advances in the search for D3- and D4- selective drugs: Probes, models and candidates. Trends in Pharmacological Sciences, 32(3), 148-157. https://doi.org/10.1016/j.tips.2010.12.003
MLA:
Löber, Stefan, et al. "Recent advances in the search for D3- and D4- selective drugs: Probes, models and candidates." Trends in Pharmacological Sciences 32.3 (2011): 148-157.
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