Agonists of the neuropeptide neurotensin have been proposed as potential novel antipsychotics based on their ability to modulate neurotransmission in brain regions associated with schizophrenia. To test this hypothesis, we examined the effects of a neurotensin mimetic with improved metabolic stability in an animal model with strong predictive validity for antipsychotic activity. Subcutaneous in...

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BACKGROUND The frequent expression of neurotensin receptors (NT-R) in primaries of pancreatic ductal carcinomas has triggered the development of radioactive neurotensin analogs for possible in vivo targeting of these tumors. However, the complete lack of information regarding NT-R in liver metastases of pancreatic cancer and pancreatic intraepithelial neoplasia (PanIN) makes an in vitro study o...

Neurotensin receptor 1 (NTSR1) is a G protein-coupled receptor that is important for signaling in the brain and the gut. Its agonist ligand neurotensin (NTS), a 13-amino-acid peptide, binds with nanomolar affinity from the extracellular side to NTSR1 and induces conformational changes that trigger intracellular signaling processes. Our goal is to monitor the conformational dynamics of single fl...

Twelve endocrine cell types immunoreactive for either 5-hydroxytryptamine (5-HT), somatostatin, gastrin, motilin, neurotensin, bovine pancreatic polypeptide (BPP), avian pancreatic polypeptide (APP), pancreatic glucagon, enteroglucagon, glicentin, secretin or cholecystokinin (CCK) were found in gastrointestinal mucosa of Caiman latirostris. Moderate numbers of enteroglucagon-immunoreactive cell...

Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like t...

Dispersed pancreatic acini were studied to assess the function of junctional coupling between adult secretory cells. Nonstimulated control cells were extensively coupled to their neighbors throughout each acinus. Addition of heptanol caused their uncoupling and increased their basal amylase release. Neurotensin, secretin, and vasoactive intestinal peptide (VIP) stimulated amylase secretion with...

This work demonstrates the expression of two different proteins (47 and 44 kDa) from the rat high-affinity neurotensin receptor cDNA, observed after both translation in vitro and transient transfection into eukaryotic COS-7 cells. These two proteins are the consequence of two initiation sites of translation present in the corresponding mRNA. Site-directed mutagenesis indicated that the 47 kDa p...