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

4-DAMP (1,1-dimethyl-4-diphenylacetoxypiperidinium iodide) tritiated at the N-methyl position. 4-DAMP is a selective muscarinic acetylcholinenergic receptor M3 antagonist.

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NET1040250UC
3634.00 EUR
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Detail Information

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 (Bmax), dissociation constants (Kd), association and dissociation rates (kon and koff), and inhibitor constants (Ki) 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.

Specifications

Detection Method Radiometric
Label Position Specifically Labeled
Molecular Weight 451.5
Product Brand Name NEN Radiochemicals
Radioisotope H-3
Radionuclide 3H
Receptor Type Acetylcholine (Muscarinic)
Shipping Condition Dry Ice
Special Ordering Information This is a radioactive product - shipping address must have a license to receive radioactive materials.
Therapeutic Area CNS & Neurologic, Cardiovascular, Gastrointestinal
Unit Size 250 µCi
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Using the NENSure Packaging System from PerkinElmer

Since 1985, the unique NENSure system has set the standard for radiochemical packaging. Based on proven performance over millions of shipments, the system provides: Ease of use, Safe storage of unused product and Reduced radiation exposure. Many NEN brand research products, including 32P-, 33P-, 35S-, 3H-, 14C- and 125I-labeled compounds, are packaged in the NENSure System, as are most radionuclides.

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