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Characterization of methanthelinium binding and function at human M1–M5 muscarinic acetylcholine receptors [PDF]
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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Functional expression of rat M5 muscarinic acetylcholine receptor in yeast
Biochemical and Biophysical Research Communications, 1992 We 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.
Hao‐Jen Huang +3 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 ...
Zipora Pittel, J. Wess
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Psychopharmacology, 2007 Schizophrenic patients show decreased measures of sensorimotor gating, such as prepulse inhibition of startle (PPI). In preclinical models, these measures may be used to predict antipsychotic activity. While current antipsychotic drugs act largely at dopamine receptors, the muscarinic acetylcholine receptors offer promising novel pharmacotherapy ...
Morgane Thomsen +5 more
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Neurochemical research, 2003 Lymphocytes possess an independent, non-neuronal cholinergic system. Moreover, both T- and B-lymphocytes express multiple muscarinic acetylcholine receptors (mAChR). To obtain a better understanding of the regulatory mechanisms governing mAChR gene expression in the lymphocytic cholinergic system, we examined the effects of lymphocyte activation on ...
Takeshi Fujii +3 more
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Role for M5 muscarinic acetylcholine receptors in cocaine addiction
Journal of Neuroscience Research, 2003AbstractMuscarinic cholinergic receptors of the M5 subtype are expressed by dopamine‐containing neurons of the ventral tegmentum. These M5 receptors modulate the activity of midbrain dopaminergic neurons, which play an important role in mediating reinforcing properties of abused psychostimulants like cocaine.
Fink-Jensen, A. +11 more
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The Journal of Pharmacology and Experimental Therapeutics, 1995 Five subtypes of muscarinic acetylcholine receptors (m1-m5) have been expressed in insect cells (Spodoptera frugiperda, Sf9) using the baculovirus system. Up to 6 nmol of muscarinic acetylcholine receptors were produced by 1 liter culture; 0.3 to 0.6 (human m1), 3 to 6 (human m2), 2 to 4 (rat m3), 1 to 2 (rat m4) and 0.5 to 1 (human m5) nmol ...
Guanzhong Dong +3 more
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Discovery of M5 Muscarinic Acetylcholine Receptor Antagonists: 1‐Methyl‐4‐Phenylpiperidine Analogs
The FASEB Journal, 2015 Na‐Ra Lee +4 more
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