NF 279

Использование

NF 279 is a potent and selective P2X1 antagonist.

Общее описание

A suramin analog that acts as a highly selective, competitive, and reversible ATP-antagonist of P2X receptor (IC₅₀/K_B ~1 μM in smooth muscle). Effectively discriminates between P2Y and P2X receptors with no discernible effects on α_1A adrenoceptors, adenosine A₁ and A_2B receptors, histamine H₁, muscarinic M₃ and neuronal nicotinic acetylcholine receptors. Displays a selectivity profile of P2X₁ >P2X₂ >P2X₃ >P2X₄ (IC₅₀ = 19 nM, 770 nM, 1.62 μM and >300 μM, respectively) in Xenopus oocytes pre-incubated with ATP. In rat and human tissues, exhibits a potency profile of rat P2X₁ > human P2X₁ ? rat P2X₂ > rat P2X₃ ~human P2X₇ ? human P2X₄. Not degraded by ecto-nucleotidases.

Биологическая активность

A potent and selective P2X 1 antagonist (IC 50 = 19 nM). Displays good selectivity over P2X 2 ,(IC 50 = 0.76 μ M), P2X 3 (IC 50 = 1.62 μ M), P2X 4 (IC 50 > 300 μ M), P2Y receptors and ecto-nucleotidases.