SNAPshots of the MCHR1: a Comparison Between the PET-Tracers [
Animals
Blood Proteins
/ metabolism
CHO Cells
Carbon Radioisotopes
/ chemistry
Chromatography, Affinity
Cricetinae
Cricetulus
Fluorine Radioisotopes
/ chemistry
Humans
Kinetics
Metabolome
Mice
Piperidines
/ chemistry
Positron-Emission Tomography
Protein Binding
Pyrimidines
/ chemistry
Rats
Receptors, Somatostatin
/ metabolism
Tissue Distribution
Ex vivo
In vitro
In vivo
MCHR1
PET
Small animal imaging
[11C]SNAP-7941
[18F]FE@SNAP
Journal
Molecular imaging and biology
ISSN: 1860-2002
Titre abrégé: Mol Imaging Biol
Pays: United States
ID NLM: 101125610
Informations de publication
Date de publication:
04 2019
04 2019
Historique:
pubmed:
28
6
2018
medline:
2
8
2019
entrez:
28
6
2018
Statut:
ppublish
Résumé
The melanin-concentrating hormone receptor 1 (MCHR1) has become an important pharmacological target, since it may be involved in various diseases, such as diabetes, insulin resistance, and obesity. Hence, a suitable positron emission tomography radiotracer for the in vivo assessment of the MCHR1 pharmacology is imperative. The current paper contrasts the extensive in vitro, in vivo, and ex vivo assessments of the radiotracers [ Kinetic real-time cell-binding studies with [ [ Both radiotracers demonstrate appropriate imaging properties for the MCHR1. However, the pronounced metabolic stability as well as superior selectivity and affinity of [
Identifiants
pubmed: 29948643
doi: 10.1007/s11307-018-1212-0
pii: 10.1007/s11307-018-1212-0
pmc: PMC6449294
doi:
Substances chimiques
Blood Proteins
0
Carbon Radioisotopes
0
Carbon-11
0
Fluorine Radioisotopes
0
MCHR1 protein, human
0
Piperidines
0
Pyrimidines
0
Receptors, Somatostatin
0
SNAP7941
0
Fluorine-18
GZ5I74KB8G
Types de publication
Comparative Study
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Pagination
257-268Références
Nature. 1999 Jul 15;400(6741):261-5
pubmed: 10421367
Nature. 1999 Jul 15;400(6741):265-9
pubmed: 10421368
Biochem Biophys Res Commun. 1999 Aug 11;261(3):622-6
pubmed: 10441476
Nat Cell Biol. 1999 Sep;1(5):267-71
pubmed: 10559938
Nature. 2000 Apr 6;404(6778):661-71
pubmed: 10766253
Diabetes. 2000 Jul;49(7):1073-7
pubmed: 10909960
Biochem Biophys Res Commun. 2000 Aug 28;275(2):709-12
pubmed: 10964727
Endocrinology. 2001 Feb;142(2):680-6
pubmed: 11159839
J Biol Chem. 2001 Jun 8;276(23):20125-9
pubmed: 11274220
Proc Natl Acad Sci U S A. 2001 Jun 19;98(13):7564-9
pubmed: 11404457
Proc Natl Acad Sci U S A. 2001 Jun 19;98(13):7576-81
pubmed: 11416225
J Biol Chem. 2001 Sep 14;276(37):34664-70
pubmed: 11459838
Proc Natl Acad Sci U S A. 2002 Mar 5;99(5):3240-5
pubmed: 11867747
Nat Med. 2002 Aug;8(8):825-30
pubmed: 12118247
Am J Physiol Endocrinol Metab. 2002 Sep;283(3):E584-92
pubmed: 12169453
FEBS Lett. 2002 Sep 11;527(1-3):205-10
pubmed: 12220661
Neuroscience. 2002;115(3):899-915
pubmed: 12435428
Am J Physiol Endocrinol Metab. 2003 May;284(5):E940-5
pubmed: 12554598
Brain Res Mol Brain Res. 2004 Sep 28;128(2):150-9
pubmed: 15363890
J Endocrinol. 2005 Jul;186(1):193-201
pubmed: 16002548
Neuropsychopharmacology. 2006 Jun;31(6):1135-45
pubmed: 16205780
Regul Pept. 2007 Oct 4;143(1-3):104-8
pubmed: 17537530
Life Sci. 2007 Jul 19;81(6):423-40
pubmed: 17655875
Proc Natl Acad Sci U S A. 2008 Jul 29;105(30):10613-8
pubmed: 18650383
Eur J Pharmacol. 2009 Dec 10;624(1-3):77-83
pubmed: 19836369
Gen Comp Endocrinol. 2011 Jun 1;172(2):185-97
pubmed: 21463631
Bioorg Med Chem Lett. 2012 Apr 1;22(7):2464-9
pubmed: 22377519
Appl Radiat Isot. 2012 Oct;70(10):2287-94
pubmed: 22858577
Bioorg Med Chem. 2012 Oct 1;20(19):5936-40
pubmed: 22921745
J Biomol Screen. 2013 Mar;18(3):309-20
pubmed: 23093571
Nat Neurosci. 2013 Jul;16(7):845-7
pubmed: 23708141
Nucl Med Biol. 2013 Oct;40(7):919-25
pubmed: 23829932
Molecules. 2013 Sep 30;18(10):12119-43
pubmed: 24084017
Sci Pharm. 2013 Jul 01;81(3):625-39
pubmed: 24106662
Front Endocrinol (Lausanne). 2013 Nov 25;4:182
pubmed: 24324458
Eur J Pharmacol. 2014 Jul 15;735:177-83
pubmed: 24780646
EJNMMI Res. 2016 Dec;6(1):31
pubmed: 27033361
Eur J Pharmacol. 2017 Feb 5;796:45-53
pubmed: 27986627
Curr Radiopharm. 2017;10(1):35-40
pubmed: 28034352
EJNMMI Res. 2017 Dec;7(1):22
pubmed: 28271461
Sci Rep. 2017 Aug 14;7(1):8054
pubmed: 28808288
Nucl Med Biol. 2018 May;60:29-36
pubmed: 29529532