Koschatzky S, Gmeiner P (2012)
Publication Language: English
Publication Type: Journal article, Original article
Publication year: 2012
Original Authors: Koschatzky S., Gmeiner P.
Publisher: Wiley-VCH Verlag
Book Volume: 7
Pages Range: 509-514
Journal Issue: 3
The neuromodulatory peptide neurotensin has been described to functionally interact with dopaminergic pathways of the human brain. We employed radioligand binding studies to investigate the physical interaction between co-expressed dopamine D or D and neurotensin NTS or NTS receptors. Substantial cross-inhibitory effects of both receptor subtypes NTS and NTS on the agonist binding of D or D were detected in the presence of neurotensin. To identify ligand-specific modulation and subtype-dependent differences, the novel dopamine receptor agonists 5 and 6 bearing the 7-OH-DPAT pharmacophore were synthesized. Exceptional ligand specificity was observed for D -NTS co-expression, which gave a 20-fold decrease in affinity for biphenylcarboxamide 5 in the presence of neurotensin. Comparing the binding properties of dopaminergic compounds in the presence of neurotensin, dopamine receptor subtype-selective profiles of the cross-inhibitory effect of neurotensin were observed. © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
APA:
Koschatzky, S., & Gmeiner, P. (2012). Selective Agonists for Dopamine/Neurotensin Receptor Heterodimers. ChemMedChem, 7(3), 509-514. https://doi.org/10.1002/cmdc.201100499
MLA:
Koschatzky, Susanne, and Peter Gmeiner. "Selective Agonists for Dopamine/Neurotensin Receptor Heterodimers." ChemMedChem 7.3 (2012): 509-514.
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