Pyrilamine (Mepyramine), [pyridinyl 5-³H]-, 250µCi (9.25MBq)

Pyrilamine is an antihistamine that acts as an antagonist at the histamine H₁ receptor. These receptors belong to a family of GPCRs that are potential drug targets for allergy.

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 NET594:

1. 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.
2. Ohta, K., Hayashi, H., Mizuguchi, H., Kagamiyama, H., Fujimoto, K., Fukui, H. (1994), Site-Directed Mutagenesis of the Histamine H1 Receptor: Roles of Aspartic Acid107, Asparagine198 and Threonine194. Biochemical and Biophysical Research Communications, 203 (2): 1096-1101.