PK 11195, [N-Methyl-³H]-, 250µCi (9.25MBq)

250 µCi quantities of PK 11195, [N-Methyl-³H]-, are available for your research. PK-11195 acts as an antagonist at peripheral benzodiazepine receptors (PBRs), and is used as a marker of neuronal damage in animal models of central nervous system (CNS) damage. PBRs are potential drug targets for cancer, autoimmune, infectious disease, and neurodegenerative disease.

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 NET885:

1. V Papadopoulos, P Guarneri, K E Kreuger, A Guidotti, and E Costa. Pregnenolone biosynthesis in C6-2B glioma cell mitochondria: regulation by a mitochondrial diazepam binding inhibitor receptor. PNAS, vol. 89, no. 11, 1992, Pages 5113-5117.
2. Benavides, J., Quarteronet, D., Plouin, P., Imbault, F., Phan, T., Uzan, A., Renault, C., Dubroeucq, M., Gueremy, C., Le Fur, G. Characterization of peripheral type benzodiazepine binding sites in human and rat platelets by using [3H]PK 11195. Studies in hypertensive patients, Biochemical Pharmacology, vol 33, issue 15, 1984, Pages 2467-2472.