125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors

European Journal of Pharmacology
S SiehlerDaniel Hoyer

Abstract

Human somatostatin (somatotropin release inhibiting factor = SRIF) receptor subtypes sst2 and sst5 were stably expressed in Chinese hamster lung fibroblast (CCL39) cells. [125I][Tyr3]octreotide labelled with high affinity and in a saturable manner both sst2 (pKd = 9.89+/-0.02, Bmax = 210+/-10 fmol/mg, n = 3) and sst5 sites (pKd = 9.64+/-0.04, Bmax = 920+/-170 fmol/mg, n = 3). The pharmacological profile of sst2 sites established in CCL39 cells using SRIF and various peptide analogues was very similar to that described previously in CHO cells and in human cortex: SRIF14 = SRIF28 > or = seglitide > BIM 23014 = RC 160 > octreotide > CGP 23996 > or = L362,855 > BIM 23052 > L361,301 = cortistatin14 > BIM 23030 > BIM 23056 > cycloantagonist SA. However, peptides classically perceived as sst2 receptor selective (e.g., seglitide, octreotide, vapreotide) showed also high affinity for human sst5 receptors labelled with [125I][Tyr3]octreotide: SRIF28 > seglitide > SRIF14 > L361,301 = octreotide > cortistatin14 = BIM 23014 = BIM 23052 > L362,855 = RC160 > CGP 23996 > BIM 23056 > cycloantagonist SA > BIM 23030. Further radioligand binding studies were performed with [Leu8,D-Trp22,125I-Tyr25]SRIF28 ([125I]LTT-SRIF28) and [125I]CGP 23996. At ...Continue Reading

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Citations

Dec 16, 2004·Naunyn-Schmiedeberg's Archives of Pharmacology·Laura Piqueras, Vicente Martínez
Feb 23, 2002·European Journal of Pharmacology·Caroline NunnDaniel Hoyer
Mar 11, 2000·British Journal of Pharmacology·C PetrucciP Bagnoli
Dec 3, 1999·The European Journal of Neuroscience·A Vezzani, D Hoyer
Oct 16, 2015·Psychopharmacology·A Faron-GóreckaM Dziedzicka-Wasylewska
Jan 10, 2008·International Journal of Cancer. Journal International Du Cancer·Genady KostenichArie Orenstein
Feb 13, 2014·British Journal of Pharmacology·Stephen P H AlexanderUNKNOWN CGTP Collaborators
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Jun 22, 1999·Journal of Neuroscience Research·J R CriadoL de Lecea
Nov 9, 2005·Pharmacology & Therapeutics·Kyriaki ThermosDaniel Hoyer
Aug 18, 2009·Neurochemistry International·Franck TalmontCatherine Mollereau

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