View source for Neurotensin receptor

{{infobox protein
| Name = [[neurotensin receptor 1]] (high affinity)
| caption = 
| image = 
| width = 
| HGNCid = 8039
| Symbol = NTSR1
| AltSymbols = NTR
| EntrezGene = 4923
| OMIM = 162651
| RefSeq = NM_002531
| UniProt = P30989
| PDB = 
| ECnumber = 
| Chromosome = 20
| Arm = q
| Band = 13
| LocusSupplementaryData = -20q13
}}
{{infobox protein
| Name = [[neurotensin receptor 2]]
| caption = 
| image = 
| width = 
| HGNCid = 8040
| Symbol = NTSR2
| AltSymbols = NTR2
| EntrezGene = 23620
| OMIM = 605538
| RefSeq = NM_012344
| UniProt = O95665
| PDB = 
| ECnumber = 
| Chromosome = 2
| Arm = p
| Band = 25.1
| LocusSupplementaryData = 
}}
{{infobox protein
| Name = [[sortilin 1]]
| caption = 
| image = 
| width = 
| HGNCid = 11186
| Symbol = SORT1
| AltSymbols = Gp95, NT3
| EntrezGene = 6272
| OMIM = 602458
| RefSeq = NM_002959
| UniProt = Q99523
| PDB = 
| ECnumber = 
| Chromosome = 1
| Arm = p
| Band = 21.3
| LocusSupplementaryData = -1p13.1
}}
The '''neurotensin receptor'''s are transmembrane receptors that bind the  [[neurotransmitter]] [[neurotensin]].<ref name="pmid10390649">{{cite journal |vauthors=Vincent JP, Mazella J, Kitabgi P | title = Neurotensin and neurotensin receptors | journal = Trends Pharmacol. Sci. | volume = 20 | issue = 7 | pages = 302–309 | year = 1999 | pmid = 10390649 | doi = 10.1016/S0165-6147(99)01357-7 }}</ref><ref name="pmid16919370">{{cite journal | author = Pelaprat D | title = Interactions between neurotensin receptors and G proteins | journal = Peptides | volume = 27 | issue = 10 | pages = 2476–2487 | year = 2006 | pmid = 16919370 | doi = 10.1016/j.peptides.2006.04.027 | url = http://www.hal.inserm.fr/inserm-00519739/document }}</ref> Two of the receptors encoded by the {{gene|NTSR1}} and {{gene|NTSR2}} genes contain seven transmembrane helices and are [[G protein-coupled receptor|G protein coupled]].  The third receptor has a single transmembrane domain and is encoded by the {{gene|SORT1}} gene.

== Ligands ==

=== Agonists ===

;Peptide
* Beta-lactotensin (NTS<sub>2</sub>)<ref name="pmid12784648">{{cite journal |vauthors=Yamauchi R, Usui H, Yunden J, Takenaka Y, Tani F, Yoshikawa M |title=Characterization of beta-lactotensin, a bioactive peptide derived from bovine beta-lactoglobulin, as a neurotensin agonist |journal=Bioscience, Biotechnology, and Biochemistry |volume=67 |issue=4 |pages=940–3 |date=April 2003 |pmid=12784648 |doi= 10.1271/bbb.67.940|url=http://joi.jlc.jst.go.jp/JST.JSTAGE/bbb/67.940?lang=en&from=PubMed}}</ref>
* JMV-449
* [[Neurotensin]]
* [[Neuromedin N]] (NTS<sub>1</sub> selective)
* PD-149,163 (NTS<sub>1</sub> selective, reduced amide bond 8-13 fragment of neurotensin)

;Non-peptide
* Partial agonists derived from SR-48692<ref name="pmid19195889">{{cite journal |vauthors=Thomas JB, Navarro H, Warner KR, Gilmour B |title=The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay |journal=Bioorganic & Medicinal Chemistry Letters |volume=19 |issue=5 |pages=1438–1441 |date=March 2009 |pmid=19195889 |pmc=4418176 |doi=10.1016/j.bmcl.2009.01.024 |url= |issn=}}</ref>

=== Antagonists ===

* [[Levocabastine]] (NTS<sub>2</sub> selective, also H<sub>1</sub> histamine antagonist)<ref name="pmid17074405">{{cite journal |vauthors=Bredeloux P, Costentin J, Dubuc I |title=Interactions between NTS2 neurotensin and opioid receptors on two nociceptive responses assessed on the hot plate test in mice |journal=Behavioural Brain Research |volume=175 |issue=2 |pages=399–407 |date=December 2006 |pmid=17074405 |doi=10.1016/j.bbr.2006.09.016 |url= |issn=}}</ref>
* [[SR-48692]] (NTS<sub>1</sub> selective)<ref name="pmid18096238">{{cite journal |vauthors=Ferraro L, Tomasini MC, Mazza R, Fuxe K, Fournier J, Tanganelli S, Antonelli T |title=Neurotensin receptors as modulators of glutamatergic transmission |journal=Brain Research Reviews |volume=58 |issue=2 |pages=365–373 |date=August 2008 |pmid=18096238 |doi=10.1016/j.brainresrev.2007.11.001 |url= |issn=}}</ref>
* [[SR-142,948]] (unselective, CAS# 184162-64-9)

== Biophysical Investigation ==
Unusually for GPCRs, NTS1 can be expressed in an active form in the bacteria ''E. coli''.<ref name="pmid18976711">{{cite journal |vauthors=Attrill H, Harding PJ, Smith E, Ross S, Watts A |title=Improved yield of a ligand-binding GPCR expressed in E. coli for structural studies. |journal=Protein Expr Purification |volume=64 |issue=1 |pages=32–38 |year=2009 |pmid=18976711 |doi=10.1016/j.pep.2008.10.001 }}</ref>  It can be purified and analysed ''in vitro'' and has been analysed by a number of biophysical techniques such as surface plasmon resonance,<ref name="pmid16708210">{{cite journal |vauthors=Harding PJ, Hadingham TC, McDonnell JM, Watts A |title=Direct analysis of a GPCR-agonist interaction by surface plasmon resonance. |journal=Eur Biophys J. |volume=35 |issue=8 |pages=709–712 |year=2006 |pmid=16708210 |doi=10.1007/s00249-006-0070-x }}</ref> FRET<ref name="pmid19186134">{{cite journal |vauthors=Harding PJ, Attrill H, Boehringer J, Ross S, Wadhams GH, Smith E, Armitage JP, Watts A |title=Constitutive dimerization of the G-protein coupled receptor, neurotensin receptor 1, reconstituted into phospholipid bilayers. |journal=Biophys. J. |volume=96 |issue=3 |pages=964–973 |year=2009 |pmid=19186134 |doi=10.1016/j.bpj.2008.09.054 |pmc=2716571}}</ref> and cryo-electron microscopy.<ref name="pmid21218848">{{cite journal |vauthors=Selmi DN, Adamson RJ, Attrill H, Goddard AD, Gilbert RJ, Watts A, Turberfield AJ |title=DNA-templated protein arrays for single-molecule imaging. |journal=Nano Lett. |volume=11 |issue=2 |pages=657–660 |year=2011 |pmid=21218848 |doi=10.1021/nl1037769 }}</ref>

== References ==
{{Reflist}}

== External links ==
*{{cite web | url = http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1342 | title = Neurotensin Receptors | accessdate = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | language = | archiveurl = | archivedate = | quote = }}
* {{MeshName|Neurotensin+Receptors}}

{{G protein-coupled receptors}}
{{Neuropeptide receptors}}
{{Neuropeptidergics}}

{{DEFAULTSORT:Neurotensin Receptor}}
[[Category:G protein-coupled receptors]]
{{transmembranereceptor-stub}}