(+)-MK-801 radioligand tritriated at the 3 position. MK-801 acts as a non-competitive antagonist at the glutamate receptor, N-Methyl-D-aspartate (NMDA).
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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 (Bmax), dissociation constants (Kd), association and dissociation rates (kon and koff), and inhibitor constants (Ki) 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, PerkinElmer has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.
References for NET972:
|Concentration||1.0 - 10 mCi/mL|
|Label Position||Specifically Labeled|
|Product Brand Name||NEN Radiochemicals|
|Shipping Condition||Dry Ice|
|Special Ordering Information||This is a radioactive product - shipping address must have a license to receive radioactive materials.|
|Therapeutic Area||CNS & Neurologic, Pain|
|Unit Size||250 µCi|