Results 191 to 200 of about 24,286 (211)

A model of the human M2 muscarinic acetylcholine receptor

Journal of Computer-Aided Molecular Design, 2002
The M2 muscarinic acetylcholine receptor belongs to the family of rhodopsin like G-Protein Coupled Receptors. This subtype of muscarinic receptors is of special interest because it bears, aside from an orthosteric binding site, also an allosteric binding site.
Kirstin, Jöhren, Hans-Dieter, Höltje
openaire   +2 more sources

Methoctramine selectively blocks cardiac muscarinic M2 receptors in vivo

Naunyn-Schmiedeberg's Archives of Pharmacology, 1988
The antimuscarinic effects of methoctramine (N, N'-bis[6-[(2-methoxybenzyl)amino]hexyl]-1, 8-octanediamine tetrahydrochloride), a polymethylene tetraamine endowed with high cardioselectivity in vitro, were assessed in two in vivo preparations. Methoctramine (300 micrograms/kg i.v.) strongly inhibited the methacholine- and muscarine-induced bradycardia ...
J, Wess, P, Angeli, C, Melchiorre, U, Moser, E, Mutschler, G, Lambrecht   +5 more
openaire   +2 more sources

Kinetic and biophysical analysis of the m2 muscarinic receptor

Life Sciences, 1995
The recombinant Pm2 muscarinic receptor expressed in Chinese hamster ovary (CHO) cells was used as a model system to examine receptor-effector coupling and ligand binding. In CHO cells, equilibrium binding studies and the dependence on receptor number per cell of the maximum response and EC50 values for agonist stimulation of phosphatidylinositol ...
B T, Hirschberg, V A, Mosser, G L, Peterson, A, Toumadje, W K, Vogel, W C, Johnson, M I, Schimerlik   +6 more
openaire   +2 more sources

Muscarinic M1, M2 receptor binding. Relationship with functional efficacy

European Journal of Pharmacology, 1988
A comparison has been made between [3H]pirenzepine binding to the M1 receptor population of rat cerebral cortex and [3H]N-methylscopolamine binding to M2 receptors in rat cardiac membranes. Several standard muscarinic antagonists including trihexyphenidyl HCl, benztropine, biperidin and 4-DAMP (4-diphenylacetoxy-N-methyl piperidine methiodide) showed ...
S B, Freedman, M S, Beer, E A, Harley
openaire   +2 more sources

Amplification of the rat m2 muscarinic receptor gene by the polymerase chain reaction: Functional expression of the M2 muscarinic receptor

Life Sciences, 1990
A selective amplification of the coding sequence of the rat M2 muscarinic receptor gene was achieved by the polymerase chain reaction. The error rate of this amplification system under conditions specified was 1 nucleotide substitution in 841 base pairs.
J, Lai, J W, Bloom, H I, Yamamura, W R, Roeske   +3 more
openaire   +2 more sources

A novel function of the M2 muscarinic receptor

Trends in Pharmacological Sciences
The M2 muscarinic receptor (M2R) is a prototypic class A G protein-coupled receptor (GPCR). Interestingly, Fasciani et al. recently identified an internal translation start site within the M2 receptor mRNA, directing the expression of a C-terminal receptor fragment.
Jürgen Wess, Liu Liu
openaire   +2 more sources

Muscarinic M2 receptor synthesis: study of receptor turnover with propylbenzilylcholine mustard

European Journal of Pharmacology: Molecular Pharmacology, 1995
We have investigated the rate and the functional responsiveness of the newly synthesised M2 muscarinic receptors in HEL 299 cells following propylbenzilylcholine mustard treatment at 37 degrees C. Propylbenzilylcholine mustard induced a dose-dependent loss of the hydrophilic ligand [3H]N-methylscopolamine binding sites with 80% inactivation at 0.1 ...
E B, Haddad, J, Rousell, P J, Barnes
openaire   +2 more sources

Distribution of m2 muscarinic receptors in rat brain using antisera selective for m2 receptors.

Molecular Pharmacology, 1991
The DNA fragment encoding the third intracellular loop of rat m2 muscarinic receptor was fused to the gene for staphylococcal Protein A. The resultant fusion protein, expressed in bacteria, was purified via IgG affinity chromatography and used as an antigen to raise a polyclonal antiserum.
M, Li, R P, Yasuda, S J, Wall, A, Wellstein, B B, Wolfe   +4 more
openaire   +2 more sources

Prejunctional muscarine receptors in the rabbit ear artery differ from M1, M2 and M3 muscarine receptors

Naunyn-Schmiedeberg's Archives of Pharmacology, 1992
The ability of several selective muscarine receptor antagonists to inhibit the effect of carbachol on prejunctional muscarine receptors on sympathetic nerve endings in the rabbit isolated ear artery was investigated to characterise the receptor subtype involved.
S A, Darroch, L K, Choo, F, Mitchelson
openaire   +2 more sources

Immunohistochemical localization of muscarinic receptors (M2) in the rat skin

Cell and Tissue Research, 2000
Acetylcholine (ACh) produces pain when applied to human skin and excites cutaneous mechanoreceptors and nerve terminals. These effects are partially mediated by activation of muscarinic receptors. The expression of muscarinic receptor subtype M2 has been shown in sensory neurons of rat dorsal root ganglia using reverse transcriptase polymerase chain ...
R V, Haberberger, M, Bodenbenner
openaire   +2 more sources