Chemical Name: N-[2-[2-(1,1-Dimethylethyl)phenoxy]-3-pyridinyl]-N'-[4-(trifluoromethoxy)phenyl]urea
Biological ActivityBPTU is an allosteric antagonist of P2Y1 (EC50 = 0.06-0.3 μM). Non-nucleotide ligand. Binds receptor outside of the helical bundle. Blocks inhibition of spontaneous contraction of rat and mouse colon induced by electrical field stimulation, nicotine and P2Y agonists. Antithrombotic; reduces platelet aggregation.
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Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.
Chao et al.
Two disparate ligand-binding sites in the human P2Y1 receptor.
Zhang et al.
BPTU, an allosteric antagonist of P2Y1 receptor, blocks nerve mediated inhibitory neuromuscular responses in the gastrointestinal tract of rodents.
Mañé et al.
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