Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors

…, TK Harden, JL Boyer, G Dubyak, BF King…

文献索引：Kim; Brown; Harden; Boyer; Dubyak; King; Burnstock; Jacobson Journal of Medicinal Chemistry, 2001 , vol. 44, # 3 p. 340 - 349

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被引用次数: 85

摘要

Novel analogues of the P2 receptor antagonist pyridoxal-5'-phosphate 6-azophenyl-2', 5'- disulfonate (2) were synthesized and studied as antagonists in functional assays at recombinant rat P2X1, P2X2, and P2X3 receptors expressed in Xenopus oocytes (ion flux stimulation) and at turkey erythrocyte P2Y1 receptors (phospholipase C activation). Selected compounds were also evaluated as antagonists of ion flux and the opening of a large pore ...