NECA

Химические свойства

White Solid

Использование

A potent adenosine receptor agonist. Inhibits platelet aggregation and is centrally active in vivo

Определение

ChEBI: A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group.

Общее описание

A cell-permeable adenosine analog that acts a potent non-selective agonist of adenosine receptors (K_i = 14 nM, 20 nM, 2.4 μM and 6.2 nM for A₁, A_2A, A_2B, A₃, respectively). Increases intracellular cAMP production (EC₅₀ = 3.1 μM in A_2B expressing CHO cells). Shown to increase glucagon release in a dose-dependent manner and inhibit insulin release at low concentrations. Although at higher concentration some insulin release is observed. Also, displays a wide range adenosine-dependent effects, such as blocking platelet aggregation and inhibiting DNA synthesis. When administered at reperfusion, it is shown reduce infarction and block the formation of the mitochondrial permeability transition pore by activating p70S6 kinase.

Биологическая активность

Potent adenosine receptor agonist (K i values are 14, 20 and 6.2 nM for human A 1 , A 2A and A 3 receptors respectively; EC 50 = 2.4 μ M for human A 2B ). Inhibits platelet aggregation and is centrally active in vivo .