Results 151 to 160 of about 40,413 (202)

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
openaire   +2 more sources

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
openaire   +2 more sources

Sensitization of Adenylyl Cyclase by P2 Purinergic and M5 Muscarinic Receptor Agonists in L Cells

Molecular Pharmacology, 1991
Many 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, J, Friedman, R D, Halligan, M, Birnbaumer, R B, Clark   +4 more
openaire   +2 more sources

M5 muscarinic receptors are needed for slow activation of dopamine neurons and for rewarding brain stimulation

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
openaire   +2 more sources

Novel insights into M5 muscarinic acetylcholine receptor function by the use of gene targeting technology

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, Anthony S, Basile, Irina, Fedorova, Weilie, Zhang, Alokesh, Duttaroy, Yinghong, Cui, Kathryn G, Lamping, Frank M, Faraci, Chu Xia, Deng, Jürgen, Wess   +9 more
openaire   +2 more sources

Immunological Detection of Muscarinic Receptor Subtype Proteins (m1–m5) in Rabbit Peripheral Tissues

Molecular Pharmacology, 1991
Employing 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
openaire   +2 more sources

Localization of m5 muscarinic receptor mRNA in rat brain examined by in situ hybridization histochemistry

Neuroscience Letters, 1990
The regional distribution of mRNA coding for the m5 muscarinic acetylcholine receptor subtype was investigated in tissue sections of rat brain by in situ hybridization histochemistry. The highest hybridization signal was observed in the hippocampus, but restricted to the ventral subiculum, pyramidal cells of the CA1 and, with lower intensity, of the ...
M T, Vilaró, J M, Palacios, G, Mengod
openaire   +2 more sources

Kinetic assays to characterize fluorescent ligand binding to muscarinic acetylcholine M1 receptor.

Biochemical Pharmacology
Muscarinic acetylcholine receptors (M1-M5), which belong to the superfamily of G protein-coupled receptors (GPCRs), play a crucial role in regulating essential physiological processes and serve as significant targets in pharmaceutical research.
Tõnis Laasfeld, Hana Bláhovcová, Kaspar Hollo, S. Veiksina, A. Rinken, Anni Allikalt   +5 more
semanticscholar   +1 more source

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.
openaire   +2 more sources

Human skin fibroblasts express m2, m4, and m5 subtypes of muscarinic acetylcholine receptors

Journal of Cellular Biochemistry, 1999
Previous studies have demonstrated that muscarinic acetylcholine receptors (mAChRs) are expressed by human skin fibroblasts (HSF). We have identified the molecular subtypes of these receptors by reverse transcription-polymerase chain reaction (RT-PCR), using m1-m5 subtype-specific primers.
R, Buchli, A, Ndoye, J G, Rodriguez, S, Zia, R J, Webber, S A, Grando   +5 more
openaire   +2 more sources