Results 201 to 210 of about 11,132 (239)

Interactions of agonists with an allosteric antagonist at muscarinic acetylcholine M2 receptors

European Journal of Pharmacology, 1996
The interaction of heptane-1,7-bis(dimethyl-3'-phthalimidopropylammonium bromide) (C7/3'-phth), with several agonists, was investigated at the muscarinic M2 receptor in guinea-pig left atria. C7/3'-phth shifted concentration-response curves for the agonists, carbachol, oxotremorine-M and (+)-cis-dioxolane, to the right in a parallel fashion ...
Fred Mitchelson, Arthur Christopoulos, Alfred Lanzafame   +2 more
openaire   +3 more sources

Acetylcholine hyperpolarizes central neurones by acting on an M2 muscarinic receptor

Nature, 1986
Acetylcholine (ACh) is considered to act as a neurotransmitter in the mammalian brain by binding to membrane receptors and bringing about a change in neurone excitability. In the case of muscarinic receptors, cell excitability is usually increased; this effect results from a closure of membrane potassium channels in cortical cells.
Terrance M. Egan, R.A. North
openaire   +3 more sources

Constitutive Activity and Inverse Agonism at the M2 Muscarinic Acetylcholine Receptor

The Journal of Pharmacology and Experimental Therapeutics, 2006
Introduction of a single-point mutation (Asn to Tyr) at position 410 at the junction between transmembrane domain 6 and the third extracellular loop of the human M(2) muscarinic acetylcholine (mACh) receptor generated a mutant receptor (N410Y) that possesses many of the hallmark features of a constitutively active mutant receptor.
Nelson, Carl P., Nahorski, Stefan R., Challiss, R.A. John   +2 more
openaire   +4 more sources

Structure-Function Studies of Allosteric Agonism at M2 Muscarinic Acetylcholine Receptors

Molecular Pharmacology, 2007
The M2 muscarinic acetylcholine receptor (mAChR) possesses at least one binding site for allosteric modulators that is dependent on the residues (172)EDGE(175), Tyr(177), and Thr(423). However, the contribution of these residues to actions of allosteric agonists, as opposed to modulators, is unknown.
Arthur Christopoulos, Patrick M. Sexton, Martyn D. Wood, Hugh J. Herdon, Vimesh Ashvinkumar Avlani, Christopher J. Langmead, Lauren T. May   +6 more
openaire   +3 more sources

Interaction of Edrophonium with Muscarinic Acetylcholine M2and M3Receptors

Anesthesiology, 2001
Background It has been reported that edrophonium can antagonize the negative chronotropic effect of carbachol. This study was undertaken to evaluate in detail the interaction of edrophonium with muscarinic Mz and M3 receptors. Methods A functional study was conducted to evaluate the
Yasuto Tanito, Yoshihumi Hirose, Masayuki Endou, Takaaki Miwa, Haruaki Nakaya, Masahiro Gamoh, Fukuichiro Okumura   +6 more
openaire   +3 more sources

Nature of the oligomers formed by muscarinic m2 acetylcholine receptors in Sf9 cells

European Journal of Pharmacology, 2001
Wild-type, FLAG-tagged, and c-myc-tagged muscarinic m2 receptors extracted in digitonin-cholate from singly and co-infected Sf9 (Spodoptera frugiperda) cells were indistinguishable in their binding of [3H]quinuclidinylbenzilate, either before or after purification.
Chi Shing Sum, Paul S.-H. Park, David R. Hampson, James W. Wells, Hubert H.M. Van Tol, Hubert H.M. Van Tol   +5 more
openaire   +3 more sources

Intramolecular interactions in muscarinic acetylcholine receptors studied with chimeric m2/m5 receptors.

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 ...
Z, Pittel, J, Wess
openaire   +2 more sources

Identification of a [3H]Ligand for the Common Allosteric Site of Muscarinic Acetylcholine M2 Receptors

Molecular Pharmacology, 1998
Muscarinic acetylcholine receptors bind allosteric modulators at a site apart from the orthosteric site used by conventional ligands. We tested in cardiac tissue whether modulator binding to ligand-occupied muscarinic M2 receptors is a preferential event that can be detected using a radioactive allosteric agent. The newly synthesized dimethyl-W84 (N,N'-
Ulrike Holzgrabe, Klaus Mohr, Christian Tränkle, Elisabeth Mies-Klomfass, Mario H. Botero Cid   +4 more
openaire   +3 more sources

Desensitization of Human Muscarinic Acetylcholine Receptor m2 Subtypes Is Caused by Their Sequestration/Internalization

Journal of Biochemistry, 1998
Desensitization of human muscarinic acetylcholine receptor m2 subtypes (hm2 receptors) stably expressed in chinese hamster ovary cells was measured as decreases in the carbamylcholine-stimulated [35S]GTPgammaS binding activity in membrane preparations after pre-treatment of cells with carbamylcholine.
Hirofumi Tsuga, Tatsuya Haga, Kimihiko Kameyama   +2 more
openaire   +3 more sources

Sialic acid is selectively involved in the interaction of agonists with M2 muscarinic acetylcholine receptors

Biochemical and Biophysical Research Communications, 1988
Neuraminidase and slight acid hydrolysis were used to investigate the role of sialic acid residues in the binding of muscarinic agonists and antagonists to membranes from tissues rich in M1 and M2 receptors. Membranes were pretreated with neuraminidase at pH 5 and the binding parameters were determined from competitive experiments with (3H ...
Yves Landry, Jean-Pierre Gies
openaire   +3 more sources