- 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
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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
- "Neurotensin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1342.
- MeSH Neurotensin+Receptors
Neuropeptide receptors G protein-coupled receptor OtherOther neuropeptide receptorsAngiotensin · Bradykinin (B1, B2) / Tachykinin (TACR1) · Calcitonin gene-related peptide · Galanin · GPCR neuropeptide (B/W, FF, S, Y) · NeurotensinType I cytokine receptor Enzyme-linked receptor Other B trdu: iter (nrpl/grfl/cytl/horl), csrc (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd; path (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp) Neuropeptidergics Cholecystokinin Agonists: Cholecystokinin • CCK-4
Antagonists: Asperlicin • Proglumide • Lorglumide • Devazepide • DexloxiglumideCRH Agonists: Corticotropin releasing hormoneGalanin Agonists: Galanin • Galanin-like peptide • Galmic • GalnonAgonists: Galanin • Galanin-like peptide • Galmic • GalnonAgonists: Galanin • Galmic • GalnonGhrelin MCH Agonists: Melanin concentrating hormone
Antagonists: ATC-0175 • GW-803,430 • NGD-4715 • SNAP-7941 • SNAP-94847Agonists: Melanin concentrating hormoneMelanocortin Agonists: alpha-MSH • Afamelanotide • Bremelanotide • Melanotan II
Antagonists: Agouti signalling peptideAgonists: alpha-MSH • Bremelanotide • Melanotan IIAgonists: alpha-MSH • Melanotan IINeuropeptide S Agonists: Neuropeptide S
Antagonists: SHA-68Neuropeptide Y Neurotensin Opioid see Template:OpioidsOrexin Oxytocin Agonists: Carbetocin • Demoxytocin • Oxytocin • WAY-267,464
Antagonists: Atosiban • Epelsiban • L-371,257 • L-368,899Tachykinin Agonists: Substance P
Antagonists: Aprepitant • Befetupitant • Casopitant • CI-1021 • CP-96,345 • CP-99,994 • CP-122,721 • Dapitant • Ezlopitant • FK-888 • Fosaprepitant • GR-203,040 • GW-597,599 • HSP-117 • L-733,060 • L-741,671 • L-743,310 • L-758,298 • Lanepitant • LY-306,740 • Maropitant • Netupitant • NKP-608 • Nolpitantium • Orvepitant • RP-67,580 • SDZ NKT 343 • Vestipitant • VofopitantVasopressin Agonists: Desmopressin • Felypressin • Ornipressin • Terlipressin • Vasopressin
Antagonists: Conivaptan • Demeclocycline • RelcovaptanAgonists: Felypressin • Ornipressin • Terlipressin • Vasopressin
Antagonists: Demeclocycline • NelivaptanAgonists: Desmopressin • Ornipressin • Vasopressin
Antagonists: Conivaptan • Demeclocycline • Lixivaptan • Mozavaptan • Satavaptan • Tolvaptan
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