Synthesis and preliminary evaluation of [3H]PSB-0413, a selective antagonist radioligand for platelet P2Y12 receptors

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 24, 2005, Pages 5450-5452

  El Tayeb, Ali ^a   Griessmeier, Kerstin J ^a   Müller, Christa E ^a  

^a UNIVERSITY OF BONN   (Germany)

Author keywords

3H PSB 0413; AR C67085MX; Nucleotide analog; P2Y12 receptor; Platelets; Radioligand

Indexed keywords

2 PROPYLTHIOADENOSINE 5' ADENYLIC ACID(1,1 DICHLORO 1 PHOSPHONOMETHYL 1 PHOSPHONYL)ANHYDRIDE; ACID ANHYDRIDE; PSB 0413; PURINE P2Y12 RECEPTOR; RADIOLIGAND; RECEPTOR BLOCKING AGENT; THROMBOCYTE RECEPTOR; TRITIUM; UNCLASSIFIED DRUG;

ANION EXCHANGE CHROMATOGRAPHY; ARTICLE; BINDING AFFINITY; CARBON NUCLEAR MAGNETIC RESONANCE; CATALYSIS; DRUG SCREENING; DRUG SYNTHESIS; ELECTROSPRAY MASS SPECTROMETRY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN CELL; HYDROGENATION; LIQUID CHROMATOGRAPHY; PHOSPHORUS NUCLEAR MAGNETIC RESONANCE; PROTON NUCLEAR MAGNETIC RESONANCE; RADIOACTIVITY; THROMBOCYTE;

ADENOSINE MONOPHOSPHATE; BLOOD PLATELETS; HUMANS; KINETICS; RADIOLIGAND ASSAY; RECEPTORS, PURINERGIC P2; THIONUCLEOSIDES; TRITIUM;

EID: 27644583393     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.08.104     Document Type: Article

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19. 3 buffer yielding the nucleotides as white powders. Retention times were 16.5 and 13.6 min for AR-C67085MX and PSB-0412, respectively.
20. +) for PSB-0412 in negative and positive modes, respectively.
21. Custom-labeling was performed by Amersham Biosciences, The Maynard Centre, Whitchurch, Cardiff, UK.
22. 3 in water (solvent A) and acetonitrile (solvent B) applying a gradient from 0% B to 25% B over 25 min at a flow rate of 1 ml/min. UV absorption was detected at 254 nm.
23. 2, and 100 mM NaCl (pH 7.4). Bound and free radioactivity was separated by rapid filtration through Whatman GF/B glass-fiber filters using a Brandel cell harvester. Filter-bound radioactivity was counted using a liquid scintillation counter. Non-specific binding was defined in the presence of 1 mM ADP. Assays were performed in duplicate in three independent experiments.