RX 821002, [6,7-3H(N)]-

RX 821002 acts as an antagonist at α2-adrenoceptors. These receptors belong to a group of GPCRs that are potential drug targets for hypertension and opiate addiction.

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 NET1153:

1. Staffan Uhlén, Helgi B. Schiöth, Jan Anker Jahnsen, A new, simple and robust radioligand binding method used to determine kinetic off-rate constants for unlabeled ligands. Application at α2A- and α2C-adrenoceptors, European Journal of Pharmacology, Volume 788, 2016, Pages 113-121.
2. Jan Anker Jahnsen, Staffan Uhlén, The predicted N-terminal signal sequence of the human α2C-adrenoceptor does not act as a functional cleavable signal peptide, European Journal of Pharmacology, Volume 684, Issues 1–3, 2012, Pages 51-58.