Neurotensin receptor
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The neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin.[1][2] Two of the receptors encoded by the NTSR1 and NTSR2 genes contain seven transmembrane helices and are G protein coupled. The third receptor has a single transmembrane domain and is encoded by the SORT1 gene.
Ligands
Agonists
- Peptide
- Beta-lactotensin (NTS2 selective)[3]
- JMV-449
- Neurotensin
- Neuromedin N (NTS1 selective)
- PD-149,163 (NTS1 selective, reduced amide bond 8-13 fragment of neurotensin)
- Non-peptide
- Partial agonists derived from SR-48692[4]
Antagonists
- Levocabastine (NTS2 selective, also H1 histamine antagonist)[5]
- SR-48692 (NTS1 selective)[6]
- SR-142,948 (unselective, CAS# 184162-64-9)
References
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External links
- "Neurotensin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- MeSH Neurotensin+Receptors
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- ↑ Vincent JP, Mazella J, Kitabgi P (1999). "Neurotensin and neurotensin receptors". Trends Pharmacol. Sci. 20 (7): 302–9. doi:10.1016/S0165-6147(99)01357-7. PMID 10390649.
- ↑ Pelaprat D (2006). "Interactions between neurotensin receptors and G proteins". Peptides. 27 (10): 2476–87. doi:10.1016/j.peptides.2006.04.027. PMID 16919370.
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