CGS 21680, [Carboxyethyl-³H(N)]-, 250µCi (9.25MBq)

CGS 21680 is an agonist for the adenosine A_2A receptor. Adenosine A_2A receptors are GPCRs that regulate myocardial blood flow as well as glutamate and dopamine release in the brain. These receptors are potential drug targets for insomnia, pain, depression, drug addiction, and Parkinson's disease.

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 NET1021:

1. Varani, K., Gessi, S., Dalpiaz, A. and Borea, P. A. (1996), Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. British Journal of Pharmacology, 117: 1693–1701.
2. Michael F. Jarvis, Michael Williams, Direct autoradiographic localization of adenosine A2 receptors in the rat brain using the A2-selective agonist, [3H]CGS 21680, In European Journal of Pharmacology, Volume 168, Issue 2, 1989, Pages 243-246.