4-DAMP, [N-Methyl-³H]-, 250µCi (9.25MBq)

4-DAMP is a highly selective antagonist of muscarinic M₃ acetylcholine receptors. These receptors are part of a group of acetylcholine G-protein coupled receptors (GPCRs) found in neurons and play a role in the parasympathetic nervous system. The M₃ receptor is a therapeutic target in Alzheimer's disease, schizophrenia, Parkinson's disease and chronic obstructive pulmonary disease (COPD).

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 NET1040:

1. Tsang, S.W.Y., Francis, P.T., Esiri, M.M. et al. Loss of [3H]4-DAMP binding to muscarinic receptors in the orbitofrontal cortex of Alzheimer’s disease patients with psychosis. Psychopharmacology , 2008, Volume 198, Pages 251-259.
2. Won Je Jeon, A.S., Gibbons, B.D. The use of a modified [3H]4-DAMP radioligand binding assay with increased selectivity for muscarinic M3 receptor shows that cortical CHRM3 levels are not altered in mood disorders, Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2013, Volume 47, Pages 7-12.