Nisoxetine Hydrochloride, [N-Methyl-³H]-, 250µCi (9.25MBq)

Nisoxetine is a selective norepinephrine reuptake inhibitor, and has been used to study obesity. Norepinephrine reuptake inhibitors (NRI, NERI) block the action of the norepinephrine transporter (NET), which is a potential drug target for ADHD and narcolepsy in addition to obesity.

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 NET1084:

1. Tsuruda, P., Yung, J., Martin, W. J., Chang, R., Mai, N., Smith, J.A.M. (2010) Influence of ligand binding kinetics on functional inhibition of human recombinant serotonin and norepinephrine transporters. Journal of Pharmacological and Toxicological Methods, 61 (2): 192-204.
2. Wersinger, C., Jeannotte, A. and Sidhu, A. (2006), Attenuation of the norepinephrine transporter activity and trafficking via interactions with α-synuclein. European Journal of Neuroscience, 24: 3141–3152.