SR141716A, [³H]

SR141716A acts as an antagonist at the cannabinoid CB₁ receptor, and is used to treat obesity. Cannabinoid receptors are a group of GPCRs that are potential drug targets for smoking sessation and weight loss.

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 NET1158:

1. Bisset, K.M., Dhopeshwarkar, A.S., Liao, C., Nicholson, R.A. (2011) The G protein-coupled cannabinoid-1 (CB1) receptor of mammalian brain: Inhibition by phthalate esters in vitro, Neurochemistry International, 59 (5): 706-713.
2. Liao, C., Zheng, J., David, L. S. and Nicholson, R. A. (2004), Inhibition of Voltage-Sensitive Sodium Channels by the Cannabinoid 1 Receptor Antagonist AM 251 in Mammalian Brain. Basic & Clinical Pharmacology & Toxicology, 94: 73–78.