Catalog Number: 4167
Alternate Names: Rolofylline
Chemical Name: 8-(Hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione
Biological Activity
Selective adenosine A1 receptor antagonist; displays 890-fold selectivity for rat A1 receptors over A2A receptors (Ki values are 0.19 and 170 nM respectively). Displays no effect on recombinant rat A3 receptors expressed on CHO cells at concentrations up to 10 μM. Exhibits diuretic and renal protective effects in rats.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in DMSO and to 25 mM in ethanol
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. 8-polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
    Shimada et al.
    J.Med.Chem., 1992;35:924
  2. KW-3902, a selective high affinity antagonist for adenosine A1 receptors.
    Nonaka et al.
    Br.J.Pharmacol., 1996;117:1645
  3. Adenosine A1 receptor antagonist KW-3902 prevents hypoxia-induced renal vasoconstriction.
    Nishiyama et al.
    J.Pharmacol.Exp.Ther., 1999;291:988
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