Evidence that neuronal G-protein-gated inwardly rectifying K+ channels are activated by Gβγ subunits and function as heteromultimers [PDF]
Guanine nucleotide-binding proteins (G proteins) activate K+ conductances in cardiac atrial cells to slow heart rate and in neurons to decrease excitability. cDNAs encoding three isoforms of a G-protein-coupled, inwardly rectifying K+ channel (GIRK) have
Davidson, Norman +2 more
core
Muscarinic M2‐receptors enhance polyphosphoinositol release in rat gastric mucosal cells
Muscarinic receptor types and their effects on the inositol phosphate second messenger system were studied in enzymatically dispersed rat gastric mucosal cells. Radioreeeptor binding studies indicated the presence of a single class of binding sites (4860 ± 875 ) and affinities of 0.42 ± 0.12 nM, 176 ± 32 nM and 13 μM for N‐methylscopolamine ...
Pfeiffer, Andreas +2 more
openaire +2 more sources
The coupling of the M2 muscarinic receptor to its G protein is voltage dependent.
G protein coupled receptors (GPCRs) participate in the majority of signal transduction processes in the body. Specifically, the binding of an external agonist promotes coupling of the GPCR to its G protein and this, in turn, induces downstream signaling.
Yair Ben-Chaim +2 more
doaj +1 more source
Quantitative surface field analysis: learning causal models to predict ligand binding affinity and pose. [PDF]
We introduce the QuanSA method for inducing physically meaningful field-based models of ligand binding pockets based on structure-activity data alone. The method is closely related to the QMOD approach, substituting a learned scoring field for a pocket ...
Cleves, Ann E, Jain, Ajay N
core
Internalization of the m2 Muscarinic Acetylcholine Receptor [PDF]
Robin Pals-Rylaarsdam +5 more
openaire +1 more source
Molecular mechanisms for fetal cardiac arrhythmia in intrahepatic cholestasis of pregnancy
Intrahepatic cholestasis in pregnancy (ICP) is characterized by raised serum bile acids which can cause fetal complications, including preterm labour and intrauterine death. The fetal death in ICP is not well understood. In this thesis, the mechanisms of
Sheikh Abdul Kadir, Siti Hamimah +1 more
core +1 more source
D₂ Dopamine Receptors Colocalize Regulator of G-Protein Signaling 9-2 (RGS9-2) via the RGS9 DEP Domain, and RGS9 Knock-Out Mice Develop Dyskinesias Associated with Dopamine Pathways [PDF]
Regulator of G-protein signaling 9-2 (RGS9-2), a member of the RGS family of Gα GTPase accelerating proteins, is expressed specifically in the striatum, which participates in antipsychotic-induced tardive dyskinesia and in levodopa-induced dyskinesia. We
Axelrod, Jeffrey D. +10 more
core
Voltage dependence of M2 muscarinic receptor antagonists and allosteric modulators
Muscarinic receptors are G protein-coupled receptors (GPCRs) that play a role in various physiological functions. Previous studies have shown that these receptors, along with other GPCRs, are voltage-sensitive; both their affinity toward agonists and their activation are regulated by membrane potential.
Shimrit, Hazan +2 more
openaire +2 more sources
Simulating Effects of Learning and Lesions with a Model of Intrinsic and Synaptically Gated Responses of Striatal Cholinergic Interneurons [PDF]
The giant cholinergic interneurons of the striatum are tonically active neurons (TANs) that respond with characteristic pauses to novel events and to appetitive and aversive conditioned stimuli.
Bullock, Daniel, Tan, Can Ozan
core +1 more source
Muscarinic acetylcholine receptor M2 (CHRM2; HM2) [PDF]
openaire +1 more source

