MK-801, (+)-[3-³H]-, 250µCi (9.25MBq)

MK-801 functions as a non-competitive N-Methyl-D-aspartate (NMDA) antagonist. It binds inside the ion channel of the receptor at several of PCP’s binding sites, in turn preventing the flow of ions through the channel. It is the most frequently used non-competitive NMDA receptor antagonist in animal models to mimic psychosis for experimental purposes. MK-801 has also been found to act as an antagonist at the nicotinic acetylcholine receptor and to bind to and inhibit the serotonin and dopamine transporters.

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 NET972:

1. Flavie Bidel, Carole Di Poi, Helene Budzinki, Patrick Pardon, William Callewaert, Adeline Arini, Niadri Basu, Ludovic Dickel, Cecile Bellanger, Christelle Jozet-Alves. The antidepressant venlafaxine may act as a neurodevelopmental toxicant in cuttle hish (Sepia officinalis). NeuroToxicology. Volume 55, July 2016, pages 142-153
2. Asya Makhro, Rick Huisjes, Liesbeth P. Verhagen, María del Mar Mañú-Pereira, Esther Llaudet-Planas, Polina Petkova-Kirova, Jue Wang, Hermann Eichler, Anna Bogdanova, Richard van Wijk, Joan-Lluís Vives-Corrons, and Lars Kaestner. Red Cell Properties after Different Modes of Blood Transportation. Front. Physiol. 2016; 7:288
3. PaleahBlack, LijieNiu, Manisha Sachdeva, David Lean, Raymond Poon, Wayne J. Bowers, Hing Man Chan, John T. Arnason, Guillaume Pelletier. Modulation of the effects of methylmercury on rat neurodevelopment by co-exposure with Labrador Tea (Rhododendron tomentosum ssp. Subarcticum). Food and Chemical Toxicology. September 2011. Volume 49, issue 9, pages 2336-2342