PD 81723

Biological Activity

PD 81723 is an allosteric potentiator at the adenosine A₁ receptor; acts via agonist-dependent and -independent mechanisms. Enhances agonist affinity for, and increased t_½ of dissociation from, the receptor. Also inhibits basal and forskolin-stimulated adenylyl cyclase (AC) activity in A₁ receptors expressed in CHO cells, possibly via direct potentiation of constitutive receptor activity or by direct inhibition of AC. Active in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
   Fox JT, Sakamuru S, Huang R
   Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
2. Structure-activity relationships for enhancement of adenosine A₁ receptor binding by 2-amino-3-benzoylthiophenes.
   Bruns et al.
   Mol.Pharmacol., 1990;38:950
3. Adenosine A₁ receptor-dependent and -independent effects of the allosteric enhancer PD 81,723.
   Musser et al.
   J.Pharmacol.Exp.Ther., 1999;288:446
4. PD 81,723, an allosteric enhancer of the A₁ adenosine receptor, lowers the threshold for ischemic preconditioning in dogs.
   Mizumura et al.
   Circ.Res., 1996;79:415
5. Agonist-independent effect of an allosteric enhancer of the A₁ adenosine receptor in CHO cells stably expressing the recombinant human A₁ receptor.
   Kollias-Baker et al.
   J.Pharmacol.Exp.Ther., 1997;281:761

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