CGP 39653, [Propyl-2,3,³H]-, 1mCi (37MBq)

CGP 39653 (D,L-(E)-2-amino-4-propyl-5-phosphono-3-pentenoic acid) inhibits the binding of glutatmate to NMDA receptors and binds to rat frontal cortical membranes in a saturable and reversible manner. NMDA receptors are glutamate receptors involved in synaptic plasticity and memory function, and are targets for legal and illicit anesthetic drugs.

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, PerkinElmer has been a leading supplier of New England Nuclear (NEN) radiochemicals, liquid scintillation cocktails, vials and nuclear counting detection instruments.

References for NET1050:

1. Kawakami, Z., Ikarashi, Y. & Kase, Y. Isoliquiritigenin is a Novel NMDA Receptor Antagonist in Kampo Medicine Yokukansan. Cell Mol Neurobiol (2011) 31: 1203.
2. Mugnaini, M., Giberti, A., Ratti, E. and van Amsterdam, F. Th. M. (1993), Allosteric Modulation of [3H]CGP 39653 Binding by Glycine in Rat Brain. Journal of Neurochemistry, 61: 1492–1497