Results 141 to 150 of about 40,413 (202)
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Increased drinking in mutant mice with truncated M5 muscarinic receptor genes
Pharmacology Biochemistry and Behavior, 2002The rarest and least understood of the muscarinic receptors is the M5 subtype. Recombinant methods were used to create mutant mice with a deletion in the third intracellular loop of the M5 receptor gene. Salivation induced by the nonselective muscarinic agonist pilocarpine (1 mg/kg s.c.) was reduced in homozygous mutants from 15 to 60 min after ...
Junichi, Takeuchi +9 more
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Evaluation of 1,2,5-thiadiazoles as modulators of M₁/M₅ muscarinic receptor subtypes.
Bioorganic & Medicinal Chemistry, 2014Abstract Studies have demonstrated the presence of allosteric binding sites on each of the muscarinic acetylcholine receptor (mAChR) subtypes. Since most drugs targeting muscarinic receptors bind to the highly conserved orthosteric binding site, they fail to achieve appreciable subtype selectivity. Targeting non-conserved allosteric sites may provide
Aditya Maheshwari, P. Rao, W. Messer
semanticscholar +2 more sources
Physical Chemistry, Chemical Physics - PCCP, 2022
Structures of muscarinic acetylcholine receptors illustrate the strikingly high degree of homology of the residues among isoforms, thus leading to difficulty in achieving subtype selectivity when targeting these receptors and causing undesired side ...
Lu Chen +8 more
semanticscholar +1 more source
Structures of muscarinic acetylcholine receptors illustrate the strikingly high degree of homology of the residues among isoforms, thus leading to difficulty in achieving subtype selectivity when targeting these receptors and causing undesired side ...
Lu Chen +8 more
semanticscholar +1 more source
The FASEB Journal, 2022
Obstructive sleep apnea (OSA) is characterized by cessation of breathing during sleep, due to repetitive episodic collapse of the airway or increased airway resistance.
Asha Kurup +4 more
semanticscholar +1 more source
Obstructive sleep apnea (OSA) is characterized by cessation of breathing during sleep, due to repetitive episodic collapse of the airway or increased airway resistance.
Asha Kurup +4 more
semanticscholar +1 more source
Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes
Neuron, 1988The human and rat genes for a fifth muscarinic receptor have been cloned and expressed in mammalian cells. The 532 amino acid human protein has 89% sequence identity to the 531 amino acid rat protein and is most closely related to the m3 receptor. Both proteins are encoded by single exons.
T I, Bonner +3 more
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The FASEB Journal, 2022
Upper airway patency is decreased during rapid eye movement (REM) sleep due to loss of genioglossus (primary tongue protruder) tongue muscle tone.
Sophia M. Koziol +4 more
semanticscholar +1 more source
Upper airway patency is decreased during rapid eye movement (REM) sleep due to loss of genioglossus (primary tongue protruder) tongue muscle tone.
Sophia M. Koziol +4 more
semanticscholar +1 more source
Molecular Pharmacology, 1993
A portion of the cDNA sequence corresponding to the third intracellular loop of either the m4 or m5 muscarinic cholinergic receptor was ligated into the pRIT23 or pET-3a expression vector, respectively. The expressed fusion proteins were purified and used to develop selective polyclonal antisera to the m4 and m5 muscarinic receptors.
R P, Yasuda +8 more
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A portion of the cDNA sequence corresponding to the third intracellular loop of either the m4 or m5 muscarinic cholinergic receptor was ligated into the pRIT23 or pET-3a expression vector, respectively. The expressed fusion proteins were purified and used to develop selective polyclonal antisera to the m4 and m5 muscarinic receptors.
R P, Yasuda +8 more
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Molecular Pharmacology, 1994
Current models of the three-dimensional structures of muscarinic acetylcholine receptors and other G protein-coupled receptors are based primarily on high-resolution electron diffraction data obtained with bacteriorhodopsin, the molecular structure of which is characterized by the presence of seven alpha-helical transmembrane domains (TM I-VII ...
Z, Pittel, J, Wess
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Current models of the three-dimensional structures of muscarinic acetylcholine receptors and other G protein-coupled receptors are based primarily on high-resolution electron diffraction data obtained with bacteriorhodopsin, the molecular structure of which is characterized by the presence of seven alpha-helical transmembrane domains (TM I-VII ...
Z, Pittel, J, Wess
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Naunyn-Schmiedeberg's Archives of Pharmacology, 2018
Firstly, it was determined whether methanthelinium bromide (MB) binds to human M1-M5 (hM1-hM5) muscarinic acetylcholine receptors in comparison to the classical muscarinic antagonist N-methylscopolamine (NMS). [3H]NMS dissociation binding experiments revealed an allosteric retardation of dissociation at 100 μM of MB ranging from none in hM3 to 4.6-fold
Matthias Irmen +3 more
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Firstly, it was determined whether methanthelinium bromide (MB) binds to human M1-M5 (hM1-hM5) muscarinic acetylcholine receptors in comparison to the classical muscarinic antagonist N-methylscopolamine (NMS). [3H]NMS dissociation binding experiments revealed an allosteric retardation of dissociation at 100 μM of MB ranging from none in hM3 to 4.6-fold
Matthias Irmen +3 more
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Localization of the m5 muscarinic cholinergic receptor in rat circle of Willis and pial arteries
Neuroscience, 2003The expression and microanatomical localization of the muscarinic cholinergic m5 receptor subtype was investigated in rat circle of Willis and pial arteries by in situ hybridization, immunoblotting and immunohistochemistry. In situ hybridization histochemistry revealed a strong signal in the endothelium of circle of Willis and pial arteries and a ...
TAYEBATI, Seyed Khosrow +3 more
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