CARDIAC MUSCARINIC BLOCKING AND ATROPINIC BLOCKING EFFECTS OF a TETRAMINE DISULFIDE WITH Α-Adrenoceptor BLOCKING ACTIVITY

Antimuscarinic action of quinidine on the heart? A study in myocardial preparations from cat hearts

“…Since then, numerous reports have appeared which are in agreement with the original observations that quinidine has anticholinergic properties (Nathanson, 1934;Hiatt, Brown, Quinn & MacDuffie, 1945;James & Nadeau, 1964;Wallace, Cline, Sealy, Young & Troyer, 1966;Josephson, Seides, Battsford, Weisfogel, Akhtar, Caracta, Lau & Damato, 1974;Mason, Winkle, Rider, Stinson & Harrison, 1977;P&rez, Ledea, Hermandez & Garcia-Barreto, 1977;Benfey, Yong, Belleau & Melchiorre, 1979). However, the mechanism by which the paralytic effect is produced by quinidine remained unclear.…”

Muscarinic Receptor Subtypes: A Critique of the Current Classification and a Proposal for a Working Nomenclature

“…This effect was attributed to an allosteric interaction at the muscarinic receptor and not due to any potential anticholinesterase acuvlty , an effect which would also produce such flattening (Clark & Mitchelson, 1976). However, the allosteric interaction of the neuromuscula blockers at muscarinic receptors has been disputed (Benfey, Yang, Belleau & Melchiorre, 1979). Birdsall, Burgen, Hulme & Stockton, (1981) have concluded that gallamine acts as an allosteric regulator from ligand binding studies.…”

Acetylcholinesterase Noncovalent Inhibitors Based on a Polyamine Backbone for Potential Use against Alzheimer's Disease

“…Furthermore, inhibition of the peripheral binding site would prevent the aggregation of βA induced by AChE. The starting point was the observation that benextramine, a tetraamine disulfide developed as an irreversible α-adrenoreceptor antagonist, displayed also a significant affinity for cardiac muscarinic M 2 receptors and potentiated the effect of ACh on the frog rectus muscle as well. , To verify whether the latter finding might result from an inhibition of AChE activity, we tested benextramine on human erythrocyte AChE. Since benextramine turned out to be a reversible inhibitor of AChE, we thought that it might represent a new lead for the design of ligands displaying affinity for AChE and muscarinic M 2 receptors thus fulfilling our research goal.…”