1367455-89-7Relevant academic research and scientific papers
Selective Agonists for Dopamine/Neurotensin Receptor Heterodimers
Koschatzky, Susanne,Gmeiner, Peter
, p. 509 - 514 (2012)
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 D2L or D3 and neurotensin NTS1 or NTS2 receptors. Substantial cross-inhibitory effects of both receptor subtypes NTS1 and NTS2 on the agonist binding of D2L or D3 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 D3-NTS2 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.
