Muscarinic Autoreceptors of Torpedo Electric Organ Are of the M₁ Subtype: Evidence by Radioligand Binding Using Selective Antagonists

Abstract

The presynaptic muscarinic autoreceptor of Torpedo marmorata electric organ has been characterised by radioligand binding studies using the subtype-selective antagonists pirenzepine, (+)-telenzepine, methoctramine, and AF-DX 116. The presynaptic receptor had relatively high affinity for the M1 antagonists pirenzepine and (+)-telenzepine (Ki = 35 and 7 nM, respectively) and lower affinities for the M2 antagonists AF-DX 116 and methoctramine (Ki = 311 and 277 nM, respectively). Comparison of these binding data with those from an M2 receptor (rat heart membranes) assayed under identical conditions and with data in the recent literature suggests that the Torpedo muscarinic autoreceptor has a pharmacology most similar to the M1 pharmacological subtype of muscarinic acetylcholine receptor.