8-Cyclopentyl-1,3-dipropylxanthine (DPCPX, PD-116,948) acts as an antagonist at the adenosine A₁ receptor. This receptor is part of a group of adenosine GPCRs, is implicated in sleep promotion and breathing, and is a potential drug target for sleep apnea.

We offer both agonist and antagonist radioligands for autoradiographic visualization or performing saturation and competition assays to determine receptor expression levels (B_max), dissociation constants (K_d), association and dissociation rates (k_on and k_off), and inhibitor constants (K_i) for a variety of receptors. We develop our radioligands to the highest specific activity possible and provide high purity resulting in low non-specific binding products. Each of our ultra-pure radioligands is fully characterized for pharmacological action and validated in receptor binding assays.

Radiolabeled ligands remain the most sensitive method for probing receptor binding biology; yielding unprecedented sensitivity gives results that technicians and scientists can trust. For over 50 years, Revvity has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NET974:

1. Schetz, J. A. and Sibley, D. R. (1997), Zinc Allosterically Modulates Antagonist Binding to Cloned D1 and D2 Dopamine Receptors. Journal of Neurochemistry, 68: 1990–1997.
2. Qinye Dong, Jennifer Schuchman, Gale B. Carey, Characterization of the swine adipocyte A1 adenosine receptor using an optimized assay system, In Comparative Biochemistry and Physiology Part C: Pharmacology, Toxicology and Endocrinology, Volume 108, Issue 3, 1994, Pages 269-280.