PerkinElmer
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Pirenzepine, [N-Methyl-3H]-, 250µCi (9.25MBq)

Pirenzepine, tritiated on the N-methyl group. Pirenzepine acts as a selective antagonist of the muscarinic M1 acetylcholine receptor.

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Part Number Unit Size List Price Your Price Quantity
NET780250UC 250 µCi 2730.00 EUR
NET780001MC 1 mCi 6900.00 EUR
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Overview

Pirenzepine (Gastrozepin) acts as an antagonist of the muscarinic M1 receptor, and is used to treat peptide ulcers. The M1 receptor is involved in the rest-and-digest state of the parasympathetic nervous system.

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 NET780:

  1. A.V. Terry, D.A. Gearhart, S.P. Mahadik, S. Warsi, J.L. Waller, Chronic treatment with first or second generation antipsychotics in rodents: Effects on high affinity nicotinic and muscarinic acetylcholine receptors in the brain, In Neuroscience, Volume 140, Issue 4, 2006, Pages 1277-1287.
  2. Weng-Keong Loke, Meng-Kwoon Sim, Mei-Lin Go, O-Substituted derivatives of pralidoxime: muscarinic properties and protection against soman effects in rats, In European Journal of Pharmacology, Volume 442, Issue 3, 2002, Pages 279-287.

Specifications

Concentration 1.0 - 10 mCi/mL
Detection Method Radiometric
Label Position Specifically Labeled
Molecular Weight 351.4
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