Neurotensin modulates central muscarinic receptors, an effect which does not involve the high-affinity neurotensin receptor (NTS1)

The role of neurotensin in physiologic and pathologic processes

“…These findings were even more pronounced in tumors from women treated with sex steroids for fertilization, consistent with the fact that E2 stimulates neurotensin expression in breast and neuroendocrine tissue [76,77]. Alifano (8)(9)(10)(11)(12)(13). This compound led to increased phosphorylation of the Na þ /H þ exchanger 1, and increases in IL-8 that were at least partially dependent on the resultant changes in intercellular and intracellular pH.…”

“…These neurons express variable levels of neurotensin receptors throughout the brain, and neurotensin binding can have stimulatory or inhibitory effects. Schneider et al [13] recently investigated the effect of neurotensin on the muscarinic acetylcholine receptors of the rat CNS, and found that neurotensin mainly decreased ligand binding to these receptors. Pretreatment with the NTS1 antagonist SR48692 failed to affect this decreased binding affinity, suggesting the possible role of NTS2.…”

Neurotensin decreases high affinity [3H]-ouabain binding to cerebral cortex membranes

“…Neurotensin effect here described on high affinity [ 3 H]-ouabain binding may be due to a direct effect, similar to other actions described for peptides on ligand binding. To illustrate, both neurotensin [18] and calcitonin [19] diminish the binding of ligand [ 3 H]-quinuclidinyl benzilate (QNB) to muscarinic cholinergic receptor. Present results suggested an interaction of the peptide with Na + , K + -ATPase at the enzyme K + site.…”

Simple validated method of LC–MS/MS determination of BZ agent in rat plasma samples

“…5 As it is a very potent and selective muscarinic ligand with higher affinity for the M2 subtype of muscarinic receptors when administered in vivo, 6 nowadays it is used especially to identify muscarinic receptors in various studies. A radioactive labeled BZ compound was used, for example, as a model agent for the development of a total serum anticholinergic activity assay based on cultured Chinese hamster ovary cells, 7 to investigate the ability of selected drugs to affect the binding characteristics of muscarinic receptors [8][9][10] or to detect changes in the expression of muscarinic receptors during inflammation 11 or organophosphate poisoning. 12 Due to its anticholinergic activity, BZ agent can also be used for the pharmacologic induction of cognitive impairment in rats in order to evaluate the pro-cognitive effects of newly developed potential drugs for the therapy of Alzheimer's disease and other neurodegenerative diseases.…”

“…As it is a very potent and selective muscarinic ligand with higher affinity for the M2 subtype of muscarinic receptors when administered in vivo, nowadays it is used especially to identify muscarinic receptors in various studies. A radioactive labeled BZ compound was used, for example, as a model agent for the development of a total serum anticholinergic activity assay based on cultured Chinese hamster ovary cells, to investigate the ability of selected drugs to affect the binding characteristics of muscarinic receptors or to detect changes in the expression of muscarinic receptors during inflammation or organophosphate poisoning …”