sr-48527 and Pain

sr-48527 has been researched along with Pain* in 1 studies

Other Studies

1 other study(ies) available for sr-48527 and Pain

Article	Year
The amide linker in nonpeptide neurotensin receptor ligands plays a key role in calcium signaling at the neurotensin receptor type 2. Bioorganic & medicinal chemistry letters, 2015, Volume: 25, Issue:10 Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesia in relevant preclinical models. The amide bond in nonpeptide NTS1 antagonists plays a central role in receptor recognition and molecular conformation. Using NTS2 FLIPR and binding assays, we found that it is also a key molecular structure for binding and calcium mobilization at NTS2. We found that reversed amides display a shift from agonist to antagonist activity and provided examples of the first competitive nonpeptide antagonists observed in the NTS2 FLIPR assay. These compounds will be valuable tools for determining the role of calcium signaling in vitro to NTS2 mediated analgesia. Topics: Amides; Biological Assay; Calcium Signaling; Dose-Response Relationship, Drug; Ligands; Molecular Structure; Pain; Protein Binding; Receptors, Neurotensin	2015

Article

Year

The amide linker in nonpeptide neurotensin receptor ligands plays a key role in calcium signaling at the neurotensin receptor type 2.

Bioorganic & medicinal chemistry letters, 2015, Volume: 25, Issue:10

Compounds acting via the GPCR neurotensin receptor type 2 (NTS2) display analgesia in relevant preclinical models. The amide bond in nonpeptide NTS1 antagonists plays a central role in receptor recognition and molecular conformation. Using NTS2 FLIPR and binding assays, we found that it is also a key molecular structure for binding and calcium mobilization at NTS2. We found that reversed amides display a shift from agonist to antagonist activity and provided examples of the first competitive nonpeptide antagonists observed in the NTS2 FLIPR assay. These compounds will be valuable tools for determining the role of calcium signaling in vitro to NTS2 mediated analgesia.

Topics: Amides; Biological Assay; Calcium Signaling; Dose-Response Relationship, Drug; Ligands; Molecular Structure; Pain; Protein Binding; Receptors, Neurotensin

2015