Neurotensin receptor

neurotensin receptor 1 (high affinity)
Identifiers
Symbol NTSR1
Alt. symbols NTR
Entrez 4923
HUGO 8039
OMIM 162651
RefSeq NM_002531
UniProt P30989
Other data
Locus Chr. 20 q13-20q13
neurotensin receptor 2
Identifiers
Symbol NTSR2
Alt. symbols NTR2
Entrez 23620
HUGO 8040
OMIM 605538
RefSeq NM_012344
UniProt O95665
Other data
Locus Chr. 2 p25.1
sortilin 1
Identifiers
Symbol SORT1
Alt. symbols Gp95, NT3
Entrez 6272
HUGO 11186
OMIM 602458
RefSeq NM_002959
UniProt Q99523
Other data
Locus Chr. 1 p21.3-1p13.1

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.

Contents

Ligands

Agonists

Peptide
  • Beta-lactotensin (NTS2)[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

  1. ^ Vincent JP, Mazella J, Kitabgi P (1999). "Neurotensin and neurotensin receptors". Trends Pharmacol. Sci. 20 (7): 302–309. doi:10.1016/S0165-6147(99)01357-7. PMID 10390649. 
  2. ^ Pelaprat D (2006). "Interactions between neurotensin receptors and G proteins". Peptides 27 (10): 2476–2487. doi:10.1016/j.peptides.2006.04.027. PMID 16919370. 
  3. ^ Yamauchi R, Usui H, Yunden J, Takenaka Y, Tani F, Yoshikawa M (April 2003). "Characterization of beta-lactotensin, a bioactive peptide derived from bovine beta-lactoglobulin, as a neurotensin agonist". Bioscience, Biotechnology, and Biochemistry 67 (4): 940–3. doi:10.1271/bbb.67.940. PMID 12784648. http://joi.jlc.jst.go.jp/JST.JSTAGE/bbb/67.940?lang=en&from=PubMed. 
  4. ^ Thomas JB, Navarro H, Warner KR, Gilmour B (March 2009). "The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay". Bioorganic & Medicinal Chemistry Letters 19 (5): 1438–1441. doi:10.1016/j.bmcl.2009.01.024. PMID 19195889. 
  5. ^ Bredeloux P, Costentin J, Dubuc I (December 2006). "Interactions between NTS2 neurotensin and opioid receptors on two nociceptive responses assessed on the hot plate test in mice". Behavioural Brain Research 175 (2): 399–407. doi:10.1016/j.bbr.2006.09.016. PMID 17074405. 
  6. ^ Ferraro L, Tomasini MC, Mazza R, Fuxe K, Fournier J, Tanganelli S, Antonelli T (August 2008). "Neurotensin receptors as modulators of glutamatergic transmission". Brain Research Reviews 58 (2): 365–373. doi:10.1016/j.brainresrev.2007.11.001. PMID 18096238. 

External links