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PSB 0777 ammonium hydrate

CAS No. :

MCE 國際站：PSB 0777 ammonium hydrate

產(chǎn)品活性：PSB 0777 ammonium hydrate 是一種有效的選擇性腺苷 A_2A 受體激動劑，對大鼠和人 A_2A 受體的 K_i 值分別為 44.4 nM，360 nM。PSB 0777 ammonium hydrate 對大鼠和人的 A₁ 受體的 K_i 值分別 ≥10000 nM，541 nM。PSB 0777 ammonium hydrate 顯示出較差的大腦滲透性和口服生物利用度。PSB 0777 ammonium hydrate 具有用于炎性腸病 (IBS) 研究的潛力。

研究領(lǐng)域：GPCR/G Protein

作用靶點：Adenosine Receptor

In Vitro: PSB 0777 ammonium hydrate (compound 7) shows high selectivity for the A_2AAR (>225-fold) versus the other AR subtypes (K_i values of >10000 nM and ?10000 for human A_2B receptor and A₃ receptor, respectively). PSB 0777 ammonium hydrate acts as an full agonist at A_2AAR with an EC₅₀ value of 117 nM in CHO-K1 cells.
PSB-0777 ammonium binds human β1 (K_i=4.4 μM) and β3 (K_i=3.3 μM) adrenergic receptors.
PSB 0777 ammonium hydrate (0.1 µM, 1 µM, 10 µM) increases concentration-dependently Acetylcholine (Ach, 1 mM) contractions in untreated and inflamed rat ileum/jejunum preparations in ex vivo experiments.

In Vivo: PSB 0777 ammonium hydrate (0.4 mg/kg/day; oral gavage; from the day 5 to 10) causes a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture.
PSB 0777 ammonium hydrate (0.03, 0.3, 3 mg/kg; i.p.) causes dose-dependent hypothermia and hypoactivity in C57BL/6J mice.
PSB 0777 ammonium hydrate cannot be absorbed systemically by the digestive mucosa once administered by the oral route. PSB 0777 ammonium hydrate (0.4 mg/kg/day; PO) has very low plasma concentrations in rats at 30 min (below 5 nM), and there is no plasma concentrations at 60 min after administration. PSB 0777 ammonium hydrate (0.4 mg/kg/day; IP) makes plasma concentrations well evident at 30 min, and decreases after 60 min, and is not detectable at 120 and 240 min.

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