Search results for "neurotensin"
showing 5 items of 15 documents
Design of Bimodal Ligands of Neurotensin Receptor 1 for Positron Emission Tomography Imaging and Fluorescence-Guided Surgery of Pancreatic Cancer
2020
International audience; Neurotensin receptor 1 (NTSR1) is overexpressed in most human pancreatic ductal adenocarcinomas. It makes it an attractive target for the development of pancreatic cancer imaging agents. In this study, we sought to develop a bimodal PET-fluorescent imaging agent capable of specifically targeting these receptors. Starting from the structure of a known NTSR1 agonist, a series of tracers was synthesized, radiometalated with gallium-68 and evaluated in vitro and in vivo, in mice bearing an AsPC-1 xenograft. PET imaging allowed us to identify the compound [ 68 Ga]Ga-NODAGA-Lys(Cy5**)-AEEAc-[Me-Arg 8 , Tle 12 ]-NT(7-13) as the one with the most promising biodistribution pr…
Inhibition of neuronally mediated secretion in rat colonic mucosa by prostaglandin D2
1992
Abstract The effect of prostaglandin D 2 (PGD 2 ) on ion transport across the mucosa of the descending colon was studied in rats. PGD 2 dose-dependently decreased baseline short-circuit current of mucosa-submucosal preparations mounted either in the Ussing chamber or mounted as an everted sac. However, with the everted sac technique, the tissue was about 1000 times more sensitive to PGD 2 . Concomitant with the decrease in short-circuit current, PGD 2 increased the mucosal-to-serosal fluxes of sodium and chloride and decreased the serosal-tomucosal flux of chloride. PGD 2 inhibited the secretory action of the PGI 2 analogue iloprost, PGD 2α , and neurotensin. The action of these secretagogu…
From Bench to Bedside—The Bad Berka Experience With First-in-Human Studies
2019
Precision oncology is being driven by rapid advances in novel diagnostics and therapeutic interventions, with treatments targeted to the needs of individual patients on the basis of genetic, biomarker, phenotypic, or psychosocial characteristics that distinguish a given patient from other patients with similar clinical presentations. Inherent in the theranostics paradigm is the assumption that diagnostic test results can precisely determine whether an individual is likely to benefit from a specific treatment. As part and integral in the current era of precision oncology, theranostics in the context of nuclear medicine aims to identify the appropriate molecular targets in neoplasms (diagnost…
Antagonism by SR 48692 of mechanical responses to neurotensin in rat intestine.
1996
Abstract 1. The effects of SR 48692 on neurotensin (NT)-induced mechanical responses were investigated in rat duodenum and proximal colon by use of isometric, isovolumic preparations. 2. SR 48692 inhibited the relaxant responses to NT in duodenal circular and longitudinal muscle. It also antagonized the NT-induced contractile effects in duodenal circular muscle and in proximal colon (both muscular layers). 3. From Schild analysis and pA2 value for SR 48692 was 8.2 in tissues where NT induced relaxant effects and 7.5 in tissues where NT induced contractile effects and the slope of the regression line was not significantly different from unity, indicating competitive antagonism. 4. SR 48692 d…
Regulation of NT Receptors after Chronic Treatment with Typical and Atypical Neuroleptic Drugs
1991
Neurotensin is a tridecapeptide, which produces central effects such as hypotension, hypothermia, muscle relaxation, analgesia, antinociception, and reduces locomotor activity (Nemeroff et al., 1977). In the recent years, several lines of evidences indicated the great importance of the dopamine (DA)- neurotensin (NT) interaction taking place mostly in the mesolimbocortical areas, both at cell bodies (A10 DA-ergic group located in the ventral tegmental area -VTA-) and nerve terminal level (cerebral cortex, n. accumbens, olfactory tubercle, ventral n. caudato-putamen) (Quirion, 1983; Nemeroff, et al., 1984; Nemeroff, 1986). Immunocytochemical data indicated the presence of NT-like immunoreact…