250µCi quantity of Diprenorphine [15,16-³H]-, is available for your research. Diprenorphine acts as an antagonist at the μ-opioid receptor (MOR), κ-opioid (KOR), and δ-opioid receptor (DOR) and is used to reverse the effects of potent opioid analgesics in veterinary medicine. The opioid receptors are a group of GPCRs that are potential drug targets for pain, depression, and drug 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 NET1121:

1. Floettmann E, Bui K, Sostek M, Payza K, Eldon M. (2017), Pharmacologic Profile of Naloxegol, a Peripherally Acting µ-Opioid Receptor Antagonist, for the Treatment of Opioid-Induced Constipation. J Pharmacol Exp Ther, 361(2): 280-291.
2. Marino, S. F. (2009), High-level production and characterization of a G-protein coupled receptor signaling complex. FEBS Journal, 276: 4515–4528.