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MRS 1523

CAS No. : 212329-37-8

MCE 站：MRS 1523

产品活性：MRS 1523 是一种有效的选择性腺苷 A₃ 受体拮抗剂，对人和大鼠 A₃ 受体的 K_i 值分别为 18.9 nM 和 113 nM。在大鼠中，MRS 1523 对 A₃ 的选择性分别是 A₁ 和 A_2A 受体的 140 倍和 18 倍。MRS 1523 可以通过 N-type Ca channel 阻滞和抑制大鼠背根神经节神经元的动作电位而发挥抗痛觉过敏作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Membrane Transporter/Ion Channel

作用靶点：Adenosine Receptor  |  Calcium Channel

In Vitro: MRS 1523 (0.1-1 μM) treatment significantly antagonizes cell numbers to 40.7% and 57.4% of the control values, respectively, 30 min before the addition of cordycepin (60 μM). MRS1523 (1 μM) alone has any effect on tumor cell growth.
A partial blockade of the adenosine-5'-N-ethylcarboxamide (NECA)-induced migration is observed when human endothelial progenitor cells (hEPC) are co-incubated with MRS 1523 (1 nM). Furthermore, in 3-days hEPC, the treatment with MRS 1523 100 nM inhibits the NECA-induced migration by 70%. NECA-induced migration is blocked in dose-response fashion by MRS 1523 with calculated K_i of 147 nM.

In Vivo: The expression and functional effects of A3 adenosine receptor (A3AR) on the excitability of small- to medium-sized, capsaicin-sensitive, dorsal root ganglion (DRG) neurons isolated from 3- to 4-week-old rats are investigated. The endogenous agonist adenosine reduces N-type Ca currents, and its effect is inhibited by 56% in the presence of A3AR antagonist MRS 1523. Current-clamp recordings demonstrated that neuronal firing of rat DRG neurons was also significantly reduced by A3AR activation in a MRS 1523-sensitive but PD173212-insensitive manner.

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