Molecular cloning of a levocabastine‐sensitive neurotensin binding site

Chalon, Pascale; Vita, Natalio; Kaghad, Mourad; Guillemot, Marie; Bonnin, Jacques; Delpech, B; Fur, G. Le; Ferrara, Pascual; Caput, Daniel

doi:10.1016/0014-5793(96)00397-3

Cited by 247 publications

(195 citation statements)

References 27 publications

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“…NTS2 was cloned from three species: mouse [49], rat [15] and human [76]. However, probably based on this history, but also reinforced by its very unexpected properties, recognition of NTS2 as a true NT receptor has not been so easy to achieve.…”

Section: Interactions Between Nts2 and G Proteinsmentioning

confidence: 99%

“…Very little is known about cloned rat NTS2 [15]. In a first study on this receptor expressed in CHO cells, SR 48692 and levocabastine, but not NT, were found to increase intracellular calcium [78].…”

Section: One Receptor Several Cells Several Independent Pathways; Omentioning

confidence: 99%

“…NTS2 corresponds to the previously described "low affinity NT binding site". Rodent NTS2s bind the histamine H1 antagonist levocabastine with high affinity, whereas human NTS2 presents lower affinity for this compound [15,49,76]. Affinity of NT for NTS2 is poorly sensitive to Na + and insensitive to GTP.…”

Section: Introductionmentioning

confidence: 99%

“…Rodent [15,49] and human [76] NTS2s (416 and 410 amino acids, respectively) share only around 40% amino acid identities with the corresponding NTS1s, have shorter Nterminal extracellular tails and longer third intracellular loops. NTS2 corresponds to the previously described "low affinity NT binding site".…”

Section: Introductionmentioning

confidence: 99%

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Interactions between neurotensin receptors and G proteins

Pélaprat

2006

Peptides

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Abstract:Three neurotensin (NT) receptors have been cloned to date, two of which, NTS1 and NTS2, belonging to the family of seven transmembrane domain receptors coupled to G proteins (GPCRs). NTS1 and NTS2 may activate multiple signal transduction pathways, involving several G proteins. However, whereas NT acts as an agonist towards all NTS1-mediated pathways, this peptide exerts agonist or antagonist activities depending on the considered NTS2-mediated pathway. Studies on these receptors reinforce the concept of independence between multiple signals potentially mediated through a single GPCR, generating a wide diversity of functional responses depending on the host cell and the ligand.

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Section: Interactions Between Nts2 and G Proteinsmentioning

confidence: 99%

Section: One Receptor Several Cells Several Independent Pathways; Omentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Interactions between neurotensin receptors and G proteins

Pélaprat

2006

Peptides

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“…Three subtypes of NT receptors, NT receptor type-1, type-2, and type-3 (Ntsr1, Ntsr2, and Ntsr3), are known thus far. Both Ntsr1 and Ntsr2 are G-protein-coupled cell surface receptors (Chalon et al, 1996;Tanaka et al, 1990), whereas Ntsr3 is a single-transmembrane domain protein that mainly localizes intracellularly (Mazella et al, 1998;Sarret et al, 2003). Among these three receptors, Ntsr1 is the main receptor subtype that mediates NT-DA interactions (Binder et al, 2001a;Caceda et al, 2005).…”

Section: Introductionmentioning

confidence: 99%

Heightened Amygdala Long-Term Potentiation in Neurotensin Receptor Type-1 Knockout Mice

Amano

Wada

Yamada

et al. 2008

Neuropsychopharmacol

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Neurotensin receptor type-1 (Ntsr1) is the main receptor subtype that underlies neurotensin (NT)-mediated modulation of the dopamine (DA) system. Although NT and DA coexist in the basolateral nucleus of the amygdala (BLA), the function of Ntsr1 in the amygdala is not well characterized. In the present study, we utilized Ntsr1 knockout (Ntsr1-KO) mice to examine the role of Ntsr1 in the amygdala. In acute brain slices of Ntsr1-KO mice, synaptic currents elicited in BLA pyramidal neurons by electrical stimulation of the lateral nucleus of the amygdala (LA) were greatly potentiated by tetanic stimulation (BLA-long-term potentiation (LTP)). Such potentiation was not evident in pyramidal neurons of wild-type mice. In the presence of an antagonist of Ntsr1, SR48692, BLA-LTP was consistently observed in the neurons of wild-type mice, suggesting that both inherited deletion and acute pharmacological blockade of Ntsr1 induce BLA-LTP. BLA-LTP in Ntsr1-KO mice was impaired by sulpiride, a DA D 2 -like receptor antagonist. Conversely, quinpirole, a D 2 -like receptor agonist, induced pronounced BLA-LTP in wild-type mice, suggesting the upregulation of D 2 -like receptor activity in Ntsr1-KO mice. The ratio of NMDA receptor-mediated to non-NMDA receptor-mediated synaptic currents in Ntsr1-KO mouse BLA neurons was approximately double that measured in wild-type mouse neurons. Furthermore, quinpirole potentiated NMDA receptormediated synaptic currents in the BLA of wild-type mice. These results suggest that, without Ntsr1, synaptic responses from the LA to BLA pyramidal neurons undergo LTP in response to tetanus stimulation through facilitation of D 2 -like receptor-induced activation of NMDA receptors.

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Regional and cellular distribution of low affinity neurotensin receptor mRNA in adult and developing mouse brain

et al. 1998

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Levocabastine-sensitive neurotensin receptor (NTRL) mRNAs were localized by in situ hybridization in adult and developing mouse brain. NTRL hybridization signal was widely distributed throughout the neuraxis. The highest concentrations of NTRL mRNA were detected in the olfactory system, olfactory tubercle, cerebral and cerebellar cortices, hippocampal formation, and selective hypothalamic nuclei. Moderate to dense hybridization signal was also observed in association with a variety of auditory, visual, and somatosensory relay nuclei, suggesting that the NTRL might be involved in a widespread modulation of primary afferent pathways. Finally a high expression of NTRL was evident in brainstem structures implicated in descending antinociceptive influences (e.g., the periaqueductal gray, nucleus raphe magnus, gigantocellular reticular nucleus, pars alpha, and lateral paragigantocellular nucleus) consistent with the proposed mediation of NT-induced analgesia by the NTRL. Although most of the regions found here to express NTRL mRNA were previously reported to be devoid of mRNA encoding the high affinity NT receptor (NTRH), a few areas (e.g., the anterior olfactory nucleus, medial septum, diagonal band of Broca, reticular thalamic nucleus, suprachiasmatic hypothalamic nucleus, and pontine nucleus) were enriched in both receptor subtypes, suggesting a possible coexpression of these receptors by the same cells. Ontogenic studies revealed that in the mouse brain, NTRL mRNA was detected only from postnatal day 14 and did not reach adulthood concentrations before day 30. In cerebral cortex, the developmental increase in NTRL expression was correlated over time with the decrease in NTRH expression previously documented in the rat, suggesting a progressive takeover of the latter by the former for transduction of the effects of NT in this structure.

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Molecular cloning of a levocabastine‐sensitive neurotensin binding site

Cited by 247 publications

References 27 publications

Interactions between neurotensin receptors and G proteins

Interactions between neurotensin receptors and G proteins

Heightened Amygdala Long-Term Potentiation in Neurotensin Receptor Type-1 Knockout Mice

Regional and cellular distribution of low affinity neurotensin receptor mRNA in adult and developing mouse brain

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