An adenosine A3 receptor agonist
Namodenoson (CF-102) is a selective A3 adenosine receptor agonist (Ki = 0.33 nM). Displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.
In human ADF cells of astroglial lineage, 100 nM Namodenoson (2-Cl-IB-MECA) caused a marked reorganization of the cytoskeleton, with appearance of stress fibres and numerous cell protrusions. High concentrations of Namodenoson (2-Cl-IB-MECA) directly cause influx of Ca2+[2].
Intravenous administration of 200 μg/kg Namodenoson (2-Cl-IB-MECA) resulted in a short-lasting hypotension, which was accompanied by a 50-100-fold increase in plasma histamine concentrations. Administration of a second dose of Namodenoson (2-Cl-IB-MECA) did not elicit any hemodynamic effects[1].
参考文献:
[1]. Van Schaick EA et al. Hemodynamic effects and histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats. Eur J Pharmacol. 1996 Jul 25;308(3):311-4.
[2]. Jacobson KA et al. Adenosine A3 receptors: novel ligands and paradoxical effects. Trends Pharmacol Sci. 1998 May;19(5):184-91.
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