Results 171 to 180 of about 6,339 (219)
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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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Molecular Pharmacology, 1992
The five muscarinic receptors (m1-m5), although structurally closely related, can be distinguished pharmacologically by the use of subtype-selective ligands. Various tricyclic muscarinic antagonists, including the AF-DX derivative AQ-RA 741 and the alkaloid himbacine, for example, have been shown to display up to 200-fold higher affinities for m2 and ...
J, Wess, D, Gdula, M R, Brann
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The five muscarinic receptors (m1-m5), although structurally closely related, can be distinguished pharmacologically by the use of subtype-selective ligands. Various tricyclic muscarinic antagonists, including the AF-DX derivative AQ-RA 741 and the alkaloid himbacine, for example, have been shown to display up to 200-fold higher affinities for m2 and ...
J, Wess, D, Gdula, M R, Brann
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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 ...
Thomsen, M. +5 more
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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 ...
Thomsen, M. +5 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 +2 more
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Immunological Detection of Muscarinic Receptor Subtype Proteins (m1–m5) in Rabbit Peripheral Tissues
Molecular Pharmacology, 1991Employing subtype-specific antisera, we have measured the relative levels of five muscarinic receptor subtype proteins (m1-m5) in rabbit peripheral tissues. Immunoprecipitation assays demonstrated the presence of four distinct receptor proteins (m1-m4), which showed notable differences in their tissue distribution.
F, Dörje, A I, Levey, M R, Brann
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Life Sciences, 2003
Until recently, little was known about the possible physiological functions of the M(5) muscarinic acetylcholine receptor subtype, the last member of the muscarinic receptor family (M(1)-M(5)) to be cloned. To learn more about the potential physiological roles of this receptor subtype, we generated and analyzed M(5) receptor-deficient mice (M5 -/- mice)
Masahisa, Yamada +9 more
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Until recently, little was known about the possible physiological functions of the M(5) muscarinic acetylcholine receptor subtype, the last member of the muscarinic receptor family (M(1)-M(5)) to be cloned. To learn more about the potential physiological roles of this receptor subtype, we generated and analyzed M(5) receptor-deficient mice (M5 -/- mice)
Masahisa, Yamada +9 more
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Sensitization of Adenylyl Cyclase by P2 Purinergic and M5 Muscarinic Receptor Agonists in L Cells
Molecular Pharmacology, 1991Many hormones have been shown to activate phospholipase C, which results in the hydrolysis of membrane polyphosphoinositides, such as phosphatidylinositol 4,5-bisphosphate (PIP2). Two second messengers are known to be produced by PIP2 hydrolysis, 1,2-diacylglycerol, an endogenous activator of a family of enzymes called protein kinase C (PKCs), and ...
J A, Johnson +4 more
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Life Sciences, 2001
Mesopontine cholinergic neurons (Ch5 and Ch6 cell groups) activate the cerebral cortex via thalamic projections, and activate locomotion and reward via dopamine neurons in the substantia nigra and ventral tegmental area (VTA). Nicotinic receptors in VTA activate dopamine neurons quickly, and are needed for the stimulant and rewarding effects of ...
J, Yeomans, G, Forster, C, Blaha
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Mesopontine cholinergic neurons (Ch5 and Ch6 cell groups) activate the cerebral cortex via thalamic projections, and activate locomotion and reward via dopamine neurons in the substantia nigra and ventral tegmental area (VTA). Nicotinic receptors in VTA activate dopamine neurons quickly, and are needed for the stimulant and rewarding effects of ...
J, Yeomans, G, Forster, C, Blaha
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Immunohistochemical study of m1–m5 muscarinic receptors and nNOS in human inferior turbinate mucosa
Acta Oto-Laryngologica, 2007This study suggested that nitric oxide (NO) takes part in the parasympathetic nerve control functions mainly through m3 receptors and subsequently through m1 receptors.The regulation of glandular secretions and vasomotor tone in human nasal mucosa implicates muscarinic receptors. There are five recognized classes (m1-m5) of muscarinic receptor subtypes.
Muneo, Nakaya +2 more
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