Results 161 to 170 of about 39,843 (183)

Structural basis of the subtype selectivity of muscarinic antagonists: a study with chimeric m2/m5 muscarinic receptors.

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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Decreased prepulse inhibition and increased sensitivity to muscarinic, but not dopaminergic drugs in M5 muscarinic acetylcholine receptor knockout mice

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., Wortwein, G., Fink-Jensen, Anders, Woldbye, D.P.D., Wess, J., Caine, S.B.   +5 more
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Immunological localization of m1–m5 muscarinic acetylcholine receptors in peripheral tissues and brain

Life Sciences, 1993
Knowledge of the distributions and functions of native m1-m5 muscarinic acetylcholine receptors in tissues is limited. To characterize the family of m1-m5 proteins directly, a panel of subtype-selective antibodies was generated against divergent i3 loop-fusion proteins. Each antibody was shown to bind a single cloned receptor specifically.
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Role for M₅ muscarinic acetylcholine receptors in cocaine addiction

Journal of Neuroscience Research, 2003
AbstractMuscarinic 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., Fedorova, I., Wörtwein, Gitta, Woldbye, David P. D., Rasmussen, T., Thomsen, M., Bolwig, Tom G., Knitowski, K.M., McKinzie, D.L., Yamada, M., Wess, J., Basile, A.   +11 more
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Identification of m3, m4 and m5 subtypes of muscarinic receptor mRNA in human blood mononuclear cells

Journal of Neuroimmunology, 1995
In this study we made use of the Reverse transcription-polymerase chain reaction to analyze the expression of mRNA for the five subtypes of muscarinic acetylcholine receptors in human blood mononuclear cells. mRNA for m3, m4 and m5 subtypes was detected, while mRNA for m1 and m2 muscarinic receptors was not found.
Costa, P, Auger, C. B, Traver, D. J, Costa, L. G.   +3 more
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Efficient coupling of m5 muscarinic acetylcholine receptors to activation of nitric oxide synthase.

The Journal of Pharmacology and Experimental Therapeutics, 1994
The coupling of m5 muscarinic acetylcholine receptors to the generation and release of nitric oxide (NO) was investigated. Chinese hamster ovary cells, which stably express m5 receptors, were transiently transfected with the gene encoding neuronal NO synthase and used as a model system. Increased generation of NO upon stimulation of cells by muscarinic
S Z, Wang, S Z, Zhu, E E, el-Fakahany
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M1, M3 and M5 muscarinic receptors stimulate mitogen-activated protein kinase.

Pharmacology, 1998
We report here that the M1, M3 and M5 muscarinic acetylcholine receptor subtypes that have been shown to couple to phosphoinositide hydrolysis also activate the mitogen-activated protein kinase (MAPK). Pharmacological characterization as well as mechanistic details of the activation pathway are presented. Carbachol-induced MAPK activation was time- and
D R, Wotta, E V, Wattenberg, R B, Langason, E E, el-Fakahany   +3 more
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Localization of the m5 muscarinic cholinergic receptor in rat circle of Willis and pial arteries

Neuroscience, 2003
The 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, DI TULLIO MA, TOMASSONI, Daniele, AMENTA, Francesco   +3 more
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m1–m5 Muscarinic Receptor Distribution in Rat CNS by RT‐PCR and HPLC

Journal of Neurochemistry, 1994
Abstract: Five muscarinic receptor genes (m1–m5) that encode distinct muscarinic receptor subtypes have been cloned. Because of their structural homology and pharmacological similarity, ligand binding probes currently available do not clearly distinguish among the subtypes. To obtain a clear distribution within the CNS of molecularly defined muscarinic
J, Wei, E A, Walton, A, Milici, J J, Buccafusco   +3 more
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Atypical Muscarinic Allosteric Modulation: Cooperativity between Modulators and Their Atypical Binding Topology in Muscarinic M2 and M2/M5 Chimeric Receptors

Molecular Pharmacology, 2005
The binding and function of muscarinic acetylcholine receptors can be modulated allosterically. Some allosteric muscarinic ligands are "atypical", having steep concentration-effect curves and not interacting competitively with "typical" allosteric modulators. For atypical agents, a second allosteric site has been proposed.
Christian, Tränkle, Andreas, Dittmann, Uwe, Schulz, Oliver, Weyand, Stefan, Buller, Kirstin, Jöhren, Eberhard, Heller, Nigel J M, Birdsall, Ulrike, Holzgrabe, John, Ellis, Hans Dieter, Höltje, Klaus, Mohr   +11 more
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