Results 31 to 40 of about 24,286 (211)

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]

, 2018
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

Modulation of the M2 Muscarinic Acetylcholine Receptor Activity with Monoclonal Anti-M2 Receptor Antibody Fragments [PDF]

Journal of Biological Chemistry, 2004
Antibodies directed against the second extracellular loop of G protein-coupled receptors are known to have functional activities. From a partial agonist monoclonal antibody directed against the M2 muscarinic receptor, we constructed and produced a single chain variable fragment with high affinity for its target epitope.
Jean-Christophe, Peter, Gerd, Wallukat, Jean, Tugler, Damien, Maurice, Jean-Christophe, Roegel, Jean-Paul, Briand, Johan, Hoebeke   +6 more
openaire   +2 more sources

Intrinsic Gating Properties of a Cloned G Protein-activated Inward Rectifier K^+ Channel [PDF]

, 1995
The voltage-, time-, and K^+-dependent properties of a G protein-activated inwardly rectifying K^+ channel (GIRK1/KGA/Kir3.1) cloned from rat atrium were studied in Xenopus oocytes under two-electrode voltage clamp. During maintained G protein activation
Davidson, Norman, Doupnik, Craig A., Kofuji, Paulo, Lester, Henry A., Lim, Nancy F.   +4 more
core   +1 more source

Distribution of Muscarinic Acethylcholine Receptors and Related Signal [PDF]

Türk Biyokimya Dergisi, 2006
Muscarinic receptors are members of G protein coupled receptor family. Molecularcloning studies indicate five intronless genes that encode five muscarinic receptorglycoproteins.
Hülya Cabadak
doaj  

Muscarinic acetylcholine receptor M1 and M3 subtypes mediate acetylcholine-induced endothelium-independent vasodilatation in rat mesenteric arteries

Journal of Pharmacological Sciences, 2016
The present study investigated pharmacological characterizations of muscarinic acetylcholine receptor (AChR) subtypes involving ACh-induced endothelium-independent vasodilatation in rat mesenteric arteries.
Panot Tangsucharit, Shingo Takatori, Yoshito Zamami, Mitsuhiro Goda, Poungrat Pakdeechote, Hiromu Kawasaki, Fusako Takayama   +6 more
doaj   +1 more source

Inhibition of Subsets of G Protein-coupled Receptors by Empty Mutants of G Protein α Subunits in Go, G11, and G16 [PDF]

, 2000
We previously reported that the xanthine nucleotide binding Goα mutant, GoαX, inhibited the activation of Gi-coupled receptors. We constructed similar mutations in G11α and G16α and characterized their nucleotide binding and receptor interaction.
Gu, Lingjie, Simon, Melvin I., Yu, Bo
core   +1 more source

The Spinal Muscarinic M1 Receptors and GABAA Receptors Contribute to the McN-A-343–Induced Antinociceptive Effects During Thermal Stimulation of Mice

Journal of Pharmacological Sciences, 2008
The present study was undertaken to clarify how spinal muscarinic receptors are involved in the antinociceptive effects in thermal stimulation. Intrathecal (i.t.) injection of the muscarinic agonist McN-A-343 inhibited the tail-flick response to noxious ...
Kenji Honda, Keigo Horikawa, Suguru Ando, Kohei Koga, Satoshi Kawata, Keisuke Migita, Yukio Takano   +6 more
doaj   +1 more source

Allosteric modulation in monomers and oligomers of a G protein-coupled receptor

eLife, 2016
The M2 muscarinic receptor is the prototypic model of allostery in GPCRs, yet the molecular and the supramolecular determinants of such effects are unknown.
Rabindra V Shivnaraine, Brendan Kelly, Krishana S Sankar, Dar'ya S Redka, Yi Rang Han, Fei Huang, Gwendolynne Elmslie, Daniel Pinto, Yuchong Li, Jonathan V Rocheleau, Claudiu C Gradinaru, John Ellis, James W Wells   +12 more
doaj   +1 more source

Probing the role of the cation–π interaction in the binding sites of GPCRs using unnatural amino acids [PDF]

, 2009
We describe a general application of the nonsense suppression methodology for unnatural amino acid incorporation to probe drug–receptor interactions in functional G protein-coupled receptors (GPCRs), evaluating the binding sites of both the M2 muscarinic
Ballesteros, Cho, D. A. Dougherty, Dougherty, Dougherty, Dougherty, Doupnik, Gallivan, H. A. Lester, Hibert, Hopkins, Huang, Huang, K. S. Bower, Klabunde, Kofuji, Krapivinsky, Lagerstrom, Lu, Lu, M. M. Torrice, Ma, Mark, Nemeth, Nowak, Palczewski, Rasmussen, Schwartz, Warne, Xiu, Zacharias, Zhong   +31 more
core   +3 more sources

Additive interaction of intrathecal ginsenosides and neostigmine in the rat formalin test [PDF]

Korean Journal of Anesthesiology, 2013
BackgroundThe authors evaluated the effect of intrathecal mixture of ginsenosides with neostigmine on formalin-induced nociception and made further clear the role of the spinal muscarinic (M) receptors on the activity of ginsenosides.MethodsA catheter ...
Cheon-Hee Park, Park-Ne Kim, Seong-Heon Lee, Myung Ha Yoon   +3 more
doaj   +1 more source