|S2790||Istradefylline||<1 mg/mL||6 mg/mL||<1 mg/mL|
|S2153||CGS 21680 HCl||<1 mg/mL||100 mg/mL||<1 mg/mL|
|S8575||A2AR antagonist 1||<1 mg/mL||61 mg/mL||<1 mg/mL|
|S8105||ZM241385||<1 mg/mL||67 mg/mL||<1 mg/mL|
|S8314||5-Iodotubercidin||<1 mg/mL||78 mg/mL||<1 mg/mL|
|S8104||SCH58261||<1 mg/mL||69 mg/mL||<1 mg/mL|
|S7588||Reversine||<1 mg/mL||5 mg/mL||<1 mg/mL|
- Adenosine Receptor抑制剂（7）
- 新Adenosine Receptor产品
Istradefylline是腺苷A2A受体(A2AR)选择性拮抗剂，Ki为2.2 nM。Phase 3。
The effect of caffeine (CAF) and adenosine A1 and A2A receptor antagonists, DPCPX and KW 6002 (KW) on DA release induced by MDMA in the mouse striatum.KW (1.25 and 2.5 mg/kg) were injected simultaneously with MDMA 20 or 40 mg/kg as indicated with an arrow. Values are the mean ± SEM (n = 6–8 animals). *P < 0.0001 represents a significant difference in comparison to control group; “a” P < 0.0002 represents a significant difference in comparison to MDMA group (repeated measures ANOVA and Tukey’s post-hoc test)
CGS 21680 HCl是一种adenosine A2 receptor激动剂，Ki为27 nM，比作用于A1受体选择性高140倍。
Effects of CGS-21,680 and forskolin on caffeine inhibited the expression of leptin in the human BeWo cells. The cells were treated with CGS-21,680 (2 μM, adenosine receptor A2a (ADORA2A) agonist)/forskolin (4 μM, adenylyl cyclase (AC) agonist, cAMP activator) and/or caffeine (20 μM) for 7 d. (A and B) The mRNA expression of leptin and ADORA2A was detected by quantitative real-time PCR, n = 3. (C) The protein expression of ADORA2A was detected by Western blotting, n = 2. (D) At the end of the treatment, the mRNA expression of leptin was detected by real-time PCR, n = 3. GAPDH was used as an internal control. The results are expressed as the mean ± S.E.M. of three independent experiments; *P < 0.05 and **P < 0.01 vs. control.
SCH 58261是一个高效的选择性的A2a adenosine receptor拮抗剂，其对rat A2a和bovine A2a的Ki值分别为2.3 nM和2 nM。
Reversine是一种强效human A3 adenosine receptor拮抗剂，Ki为0.66 μM，也是一种泛aurora A/B/C kinase抑制剂，IC50分别为12 nM/13 nM/20 nM。也用于干细胞分化。
Immunofluorescence of acetylated a-tubulin (red) in control (a), reversin-treated (b), and BI 2536/Reversin mixture-treated embryos (c).The embryos treated with Reversine completed first mitosis, but the nuclei of their blastomeres were fragmented (b, arrows). Embryos inhibited withthe BI 2536/Reversine mixture arrested before the onset of anaphase. Microtubules of the spindle are disorganized (c, double-arrow) and thechromosomes are misaligned (c, arrows) in these inhibited embryos. DNA is counter-stained with DAPI (blue). Scale bar, 10 μm.