Naloxone, [N-allyl-2,3,-³H]-

Naloxone functions as a non-selective, competitive antagonist at opioid receptors. It commonly used to reverse the effects of opioid overdose and to prevent opioid abuse.

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 NET719:

1. Andrei Sonnabend, Viola Spahn, Marlitt Stech, Anne Zemella, Christoph Stein, Stefan Kubick. Production of G protein-coupled receptors in an insect-based cell-free system. Biotechnology and Bioengineering. October 2017. Volume 114, Issue 10, pages 2328-2338.
2. Peter Heusler, Stephanie Tardif, Didier Cussac. Agonist stimulation of human µ opioid receptors in a [³⁵S]GTPγS incorporation assay: observation of “bell-shaped” concentration-response relationships under conditions of strong receptor G protein coupling. Journal of Receptors and Signal Transduction. 2016. Volume 36, Issue 2, pages 158-166.
3. Michael B Gatch, Alexey Kozlenkov, Ren-Qi Huang, Wenjuan Yang, Jacques D Nguyen, Javier Gonzalex-Maeso, Kenner C Rice, Charles P France, Glenn H Dillon, Michael J Forster, John A Schetz. The HIV Antiretroviral Drug Egavierenz has LSD-like Properties. Neuropsychopharmacology. May 2013.