2',5'-Dideoxyadenosine effectively inhibits adenylyl cyclase in a non-competitive manner by binding to the P-site, with an IC50 of 3 µM. It is a nucleoside analog and exhibits strong antiadrenergic effects in the heart[1][2].
体内研究
2',5'-Dideoxyadenosine (0.1 mg/kg; IP; 15 min pre-treated) completely blocks the diuretic, natriuretic, and K+ and Cl- sparing effects of Fr EtOAc in rats[4].
体外研究
2',5'-Dideoxyadenosine (10 μM, 30 min) decreases cAMP production and inhibits the phosphorylation of GluA1 at Ser845, which is induced by carbachol (CCh)[3].
2',5'-Dideoxyadenosine (10 μM, 30 min) inhibits the carbachol (CCh)-induced increase in Akt phosphorylation and reduces CCh-induced phosphorylation at Ser2448[3].
2',5'-Dideoxyadenosine (20-150 mM), like adenosine, dependently and reversibly reduces the positive inotropic and chronotropic effects of beta-adrenergic stimulation with isoproterenol (8-54 pmol) by up to 70% and 50%, respectively[2].
2',5'-Dideoxyadenosine 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MIN6 β-cells
100 μM
inhibited glucose-induced [cAMP]pm oscillations
Diabetes. 2011 May;60(5):1535-43.
Human T lymphocytes
100 μM - 1 mM
5 min
Partially inhibited the directed movement (capping process) of CD3, CD4, and CD8 molecules; at 1 mM ddAdo, only half of the cells were able to cap.
Proc Natl Acad Sci U S A. 1988 Feb;85(3):792-6
L6 myotubes
50 μM
30min
Inhibited adenylate cyclase, significantly reducing cAMP accumulation stimulated by zinterol (100 nM) or forskolin (10 μM), and partially inhibited zinterol-stimulated glucose uptake.
Br J Pharmacol. 2006 Feb;147(4):446-54
mouse pancreatic islet β-cells
100 μM
suppressed the glucose- and hormone-induced [cAMP]pm elevations
Diabetes. 2011 May;60(5):1535-43.
SH-SY5Y cells
300 μM
48 h
To investigate the effect of 2',5'-Dideoxyadenosine on neurite branching and length in SH-SY5Y cells, results showed that the compound attenuated the promoting effect of VILIP-1 overexpression on neurite branching and length.
Transl Psychiatry. 2011 Jul 19;1(7):e22
rat thoracic aorta endothelial cells
50 μM
inhibited adenyl cyclase activity, thereby reducing NO release evoked by adenosine via A1 and A2A receptors
J Physiol. 2002 Oct 1;544(Pt 1):195-209
SPG15 patient-derived fibroblasts
10 μM
24 h
Reduced autophagosome accumulation and decreased LC3-II levels
Brain. 2023 Mar 1;146(3):1103-1120
2',5'-Dideoxyadenosine 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Drosophila
SPG15 loss of function model
Oral
30 μM
Chronic treatment
Improved lysosome biogenesis and function, reduced autophagosome accumulation
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