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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 (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 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.