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Dual effects of muscarinic M2 acetylcholine receptors on the synthesis of cyclic AMP in CHO cells: dependence on time, receptor density and receptor agonists
It is proposed that the Gs‐mediated stimulatory component of the effect of muscarinic M2 receptors on cyclic AMP synthesis only occurs if the density of activated receptors is high enough to saturate the Gi proteins and proportionate to the receptors' low affinity for theGs proteins. Expand
Clozapine interaction with the M2 and M4 subtypes of muscarinic receptors.
It is concluded that clozapine has a high affinity for muscarinic M2 and M4 receptor subtypes, that it associates with the classical and not with the allosteric binding site, and that it acts as a partial agonist on both the M1 and the M2 receptor subtype. Expand
Subtype‐selective inhibition of [methyl‐3H]‐N‐methylscopolamine binding to muscarinic receptors by α‐truxillic acid esters
It is concluded that the esters of α‐truxillic acid act as M2‐selective allosteric modulators of muscarinic receptors and that, by their potency, the tertiary bis‐3‐piperidylpropyl and bis‐4‐pipersidylbutyl aminoesters surpass the other known allostero-modulators of these receptors. Expand
Interactions between Allosteric Modulators and 4-DAMP and Other Antagonists at Muscarinic Receptors: Potential Significance of the Distance between the N and Carboxyl C Atoms in the Molecules of
Positive effects of alcuronium, strychnine and brucine on the affinity of the M2 receptors for 4-DAMP have been confirmed by direct measurements of the binding of [3H]-4-diphenylacetoxy-N-dimethylpiperidinium. Expand