International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors.
Actions of acetylcholine in the periphery are the result of activation of either the ionotropic nicotinic receptor or the metabotropic muscarinic receptor. In the mammalian central nervous system…
Muscarinic receptor subtypes.
The aim of this review is to discuss the structure, function, and binding properties of the different muscarinic receptor species, attempting where possible to coordinate the diverse experimental data into a uniform picture.
Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis.
In an attempt to locate the allosteric site on muscarinic receptors to which gallamine binds, 21 residues in the putative external loops and loop/transmembrane helix interfaces have been mutated to…
Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at…
Novel methods of detecting and quantitating cooperative interactions between an agent and both a tritiated (muscarinic) antagonist and the endogenous agonist (acetylcholine), acting at a common…
Pirenzepine distinguishes between different subclasses of muscarinic receptors
Binding studies using a new anti-muscarinic drug, pirenzepine, are used, in which heterogeneity of binding is found that correlates well with the pharmacological activity and cannot be taken as evidence for different receptor subtypes.
Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia
- W. Y. Chan, D. McKinzie, C. Felder
- Biology, PsychologyProceedings of the National Academy of Sciences
- 5 August 2008
The discovery of a small molecule modulator, LY2033298, that is highly selective for human M4 receptors by virtue of targeting an allosteric site on this receptor is described, indicating its potential use as a first-in-class, selective,allosteric muscarinic antipsychotic agent.
Reconstitution of a calcium pump using defined membrane components.
- G. B. Warren, P. Toon, N. Birdsall, A. Lee, J. Metcalfe
- BiologyProceedings of the National Academy of Sciences…
- 1 March 1974
A fully functional Ca(2+) pump containing essentially a single protein and exogenous lipid has been achieved using a single step centrifugation procedure.
Estimation of competitive antagonist affinity from functional inhibition curves using the Gaddum, Schild and Cheng‐Prusoíf equations
1 The estimation of antagonist affinity from functional experiments in which the effect of a fixed agonist concentration is reduced by a range of antagonist concentrations (‘functional inhibition…
Modification of the binding properties of muscarinic receptors by gallamine.
The effects of gallamine on the binding of muscarinic ligand ligands are much greater in heart than in other tissues, suggesting the possibility of developing novel and selective musCarinic drugs.
Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
- S. Lazareno, P. Gharagozloo, D. Kuonen, A. Popham, N. Birdsall
- Biology, ChemistryMolecular Pharmacology
- 1 March 1998
The results demonstrate the potential for developing allosteric enhancers of acetylcholine affinity at individual subtypes of muscarinic receptor and suggest that minor modification of a compound showing positive, neutral, or low negative cooperativity with acetyl choline may yield compounds with various patterns of cooperativity across the receptor subtypes.