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Editorial Expression of Concern for Poon et al., Targeting the muscarinic M1 receptor with a selective, brain-penetrant antagonist to promote remyelination in multiple sclerosis. [PDF]
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Two affinity states of M1 muscarine receptors
Cellular and Molecular Neurobiology, 19881. The binding of oxotremorine-M to M1 muscarine receptors was examined by measuring competition between the agonist and 3H-pirenzepine, using rabbit hippocampal membranes suspended in 20 mM Tris buffer containing 1 mM Mn2+. 2. Both ligands interacted with a single class of receptors.
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M1 and M3 muscarinic receptors
NeuroReport, 1992P-fluoro-hexahydro-sila-difenidol hydrochloride (p-F-HHSiD) (15, 30 micrograms) and pirenzepine (7.5, 15, 30 micrograms), which are highly selective M3 and M1 muscarinic antagonists, respectively, were injected intracerebroventricularly into freely moving rats.
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