Methylhistamine Dihydrochloride, N-α-[methyl-³H]-, 250µCi (9.25MBq)

α-Methylhistamine is a selective agonist for the histamine H₃ receptor. This receptor is a GPCR that is a potential drug target for central nervous system disorders.

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 NET1027:

1. Griebel, G., Pichat, P., Pruniaux, M., Beeské, S., Lopez-Grancha, M., Genet, E., Terranova, J.P., Castro, A., Sánchez, J.A., Black, M., Varty, G. B., Weiner, I., Arad, M., Barak, S., De Levie, A., Guillot, E. (2012), SAR110894, a potent histamine H3-receptor antagonist, displays procognitive effects in rodents, Pharmacology Biochemistry and Behavior, 102 (2): 203-214.
2. Jin, C. Y., Kalimo, H. and Panula, P. (2002), The histaminergic system in human thalamus: correlation of innervation to receptor expression. European Journal of Neuroscience, 15: 1125–1138.