PMID: 8587429Jan 1, 1995Paper

Characterization of endothelin receptors in human brain cortex, gliomas, and meningiomas

Journal of Cardiovascular Pharmacology
S P HarlandA P Davenport

Abstract

We have characterized the endothelin (ET) receptor subtypes present within normal human cerebral cortex (CC), glioblastoma multiforme (GBM), and meningiomas (MGs), using two subtype-selective radioligands, [125I]-PD151242 (ETA) and [125I]-BQ3020 (ETB). For saturation experiments, sections of tissue were incubated with increasing concentrations (8 pM-4 nM) of either [125I]-PD151242 or [125I]-BQ3020 in incubation buffer (22 degrees C, 2 h). In saturation binding assays, [125I]-PD151242 bound with high affinity to a single population of ET receptors (n = individuals; +/- SEM) in normal CC (n = 3; Kd 1.23 +/- 0.20 nM; Bmax 28.10 +/- 9.04 fmol/mg protein), GBM (n = 5; Kd 1.62 +/- 0.20 nM; Bmax 147.04 +/- 62.8 fmol/mg protein), and MGs (n = 3; Kd 3.10 +/- 0.44 nM; Bmax 290.3 +/- 105.8 fmol/mg protein). [125I]-BQ3020 also bound with high affinity to a single population of ET receptors in normal CC (n = 3; Kd 4.54 +/- 1.58 nM; Bmax 190.5 +/- 88.8 fmol/mg protein), GBM (n = 4; Kd 1.38 +/- 0.28 nM; Bmax 234.0 +/- 153.6 fmol/mg protein), and MGs (n = 3; Kd 0.25 +/- 0.09 nM; Bmax 22.8 +/- 18.0 fmol/mg protein). To determine receptor subtype localization, autoradiography was performed after incubation of sections with 0.1 nM [125I]-ET-1 (ET...Continue Reading

Citations

May 15, 2008·Neuro-oncology·Surasak PhuphanichUNKNOWN New Approaches to Brain Tumor Therapy (NABTT) CNS Consortium
Apr 23, 2004·Pain Medicine : the Official Journal of the American Academy of Pain Medicine·D M CainD A Simone
Mar 10, 2016·Pharmacological Reviews·Anthony P DavenportJanet J Maguire
May 26, 2005·Brain Research. Brain Research Reviews·Lyle W Ostrow, Frederick Sachs
Aug 19, 2014·British Journal of Pharmacology·J J Maguire, A P Davenport
Jan 15, 1998·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·U KoedelH W Pfister
Feb 13, 2014·British Journal of Pharmacology·Stephen P H AlexanderUNKNOWN CGTP Collaborators

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