Results 131 to 140 of about 40,413 (202)
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Activation mechanism of the M5 muscarinic acetylcholine receptor.
Biophysical Journal, 2023L. Roy +3 more
semanticscholar +2 more sources
An Improved Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor
Synfacts, 2022semanticscholar +2 more sources
Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators [PDF]
Molecular Pharmacology, 2016 Recently, the first subtype-selective allosteric modulators of the M5 muscarinic acetylcholine receptor (mAChR) have been described, but their molecular mechanisms of action remain unknown. Using radioligand-binding and functional assays of inositol phosphate (IP) accumulation and Ca(2+) mobilization in a recombinant cell line stably expressing the ...
Alice E. Berizzi +6 more
semanticscholar +3 more sources
Functional expression of rat M5 muscarinic acetylcholine receptor in yeast
Biochemical and Biophysical Research Communications, 1992We have produced the rat M5 muscarinic acetylcholine receptor, an integral membrane protein, in the yeast Saccharomyces cerevisiae. This was achieved by placing an M5 gene in the yeast vector under the control of the yeast alpha-factor promoter and leader sequence.
Huang, Hao-Jen +3 more
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Persistent Binding and Functional Antagonism by Xanomeline at the Muscarinic M5 Receptor
The Journal of Pharmacology and Experimental Therapeutics, 2005Xanomeline is a functionally selective M1/M4 muscarinic acetylcholine receptor agonist. We have previously identified a novel mode of interaction of this ligand with the muscarinic M1 receptor that involves persistent binding and activation of the receptor after extensive washout.
Marianne K O, Grant, Esam E, El-Fakahany
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Allosteric regulation of cloned m1–m5 muscarinic receptor subtypes
Biochemical Pharmacology, 1991Allosteric regulation of [3H]N-methylscopolamine [( 3H]NMS) and [3H]quinuclidinyl benzilate [( 3H]QNB) dissociation from the m1-m5 muscarinic receptor subtypes was examined in transfected CHO-K1 cells. Half-times of dissociation of [3H]NMS from cell membranes (at 23 degrees) ranged from less than 5 min for the m2 subtype to more than 60 min for the m5 ...
J, Ellis, J, Huyler, M R, Brann
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The ontogeny of m1–m5 muscarinic receptor subtypes in rat forebrain
Developmental Brain Research, 1992The ontogeny of muscarinic receptor subtypes in rat forebrain has been determined utilizing a panel of antisera recognizing unique epitopes of the m1-m5 receptor proteins. Total receptor density in forebrain, as measured by the non-selective antagonist, [3H]quinuclidinyl benzilate (QNB), was found to increase from 507 fmol/mg in neonates (3.5 days) to ...
S J, Wall +4 more
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The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation.
ACS Chemical Neuroscience, 2018The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) was the most recent mAChR to be cloned and has since emerged as a potential therapeutic target for a number of indications.
Aaron M. Bender +2 more
semanticscholar +1 more source
Linkage of M5 Muscarinic and α7-Nicotinic Receptor Genes on 15q13 to Schizophrenia
Neuropsychobiology, 2004Most antipsychotic drugs act on the forebrain by blocking dopamine receptors. In rodents, the M5 muscarinic receptor (CHRM5) is important for prolonged dopamine release. We typed polymorphisms in CHRM5 and α7-nicotinic receptor (CHRNA7) genes on 15q13 in 82 Canadian families having at least 1 schizophrenic patient.
De Luca V +5 more
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