Neurotensin receptors: Binding properties, transduction pathways, and structure

  title={Neurotensin receptors: Binding properties, transduction pathways, and structure},
  author={Jean Pierre Vincent},
  journal={Cellular and Molecular Neurobiology},
  • J. Vincent
  • Published 1 October 1995
  • Biology
  • Cellular and Molecular Neurobiology
SummaryNeurotensin is a 13-amino acid peptide (pGlu-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu) originally isolated from hypothalami (Carraway and Leeman, 1973) and later from intestines (Kitabgiet al., 1976) of bovine. The peptide is present throughout the animal kingdom, suggesting its participation to important processes basic to animal life (Carrawayet al., 1982). Neurotensin and its analogue neuromedin-N (Lys-Ile-Pro-Tyr-Ile-Leu) (Minaminoet al., 1984) are synthesized by a common… 

Therapeutic approaches targeting the neurotensin receptors

An overview of over four decades of research is provided and the drug discovery approaches and patented strategies targeting NTSR in the past decade are detailed.

Low-Affinity Neurotensin Receptor (NTS2) Signaling: Internalization-Dependent Activation of Extracellular Signal-Regulated Kinases 1/2

This study demonstrates that NTS2 is a bona fide NT receptor and that activation of this receptor by NT or NT analogs results in an internalization-dependent activation of the ERK1/2 signaling cascade.

Activation of B2 bradykinin receptors by neurotensin.

Postnatal Nitric Oxide Inhibition Modifies Neurotensin Effect on ATPase Activity

It is postulated that early postnatal NO dysfunction may exert a permanent change in neurotensin system that influence later Na+, K+-ATPase response to neurotensin.

The actions of neurotensin in rat bladder detrusor contractility

Evidence is provided suggesting that bladder NTs may play an important role in the regulation of micturition, and that the administration of NTSR antagonists can potentially relieve the symptoms of OAB by coordination with antimuscarinic pharmacotherapy.

Specific involvement of neurotensin type 1 receptor in the neurotensin‐mediated in vivo dopamine efflux using knock‐out mice

Using in vivo differential pulse amperometry, it is shown that, in wild‐type mice, neurotensin application into the ventral tegmental area dose‐dependently evokes dopamine efflux in the nucleus accumbens.

Effects of the Hybridization of Opioid and Neurotensin Pharmacophores on Cell Survival in Rat Organotypic Hippocampal Slice Cultures

The results indicate that PK20 is a potent anti-neurodegenerative agent, co-administered with NMDA, which dose-dependently reduced hippocampal cell death, determined by a decrease in the propidium iodide signal.



The Neurotensin Receptor from Mammalian Brain

The structural and functional properties of neurotensin binding sites have been characterized in a number of tissue preparations and cell cultures of neural or nonneural origin and some of these sites represent functional neurotensIn receptors since they are coupled to GTP-binding proteins and regulate intracellular levels of second messengers such as cAMP, cGMP, and inositol phosphates.

High‐Affinity Receptor Sites and Rapid Proteolytic Inactivation of Neurotensin in Primary Cultured Neurons

The binding parameters as well as the specificity of these receptors toward neurotensin analogues reveal close similarities between the binding sites present in primary cultured neurons and those described in other membrane preprations or cells.

In vivo and in vitro structure-activity studies with peptide and pseudopeptide neurotensin analogs suggest the existence of distinct central neurotensin receptor subtypes.

The results show that NT receptors in homogenates from newborn mouse and rat brain and from COS 7 cells transfected with the cloned high-affinity NT receptor from the adult rat brain displayed virtually identical structure-activity relationships toward a series of 12 peptide and pseudopeptide NT analogs.


NT is a substance that derives from neuroectodermal cells of the primitive neural crest, which is destined to form the nervous system and part of the gastrointestinal tract, and in this respect NT is typical of its class.

Monoiodo-[ Trp " ] neurotensin , a Highly Radioactive Ligand of Neurotensin Receptors

The binding isotherm was biphasic and could be described by postulating the existence of two different classes of independent binding sites with dissociation constants of 0.1 and 4.7 m; the specificity of a series of neurotensin analogues for both high and low affinity binding sites was the same as that previously observed in other neurotensIn radioreceptor assays.

Phospholipase C activation by neurotensin and neuromedin N in Chinese hamster ovary cells expressing the rat neurotensin receptor.