Molecular properties of muscarinic acetylcholine receptors
Muscarinic acetylcholine receptors, which comprise five subtypes (M1-M5 receptors), are expressed in both the CNS and PNS (particularly the target organs of parasympathetic neurons). M1-M5 receptors are integral membrane proteins with seven transmembrane
T. Haga
semanticscholar +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]
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
Regulation of Neuromodulator Receptor Efficacy - Implications for Whole-Neuron and Synaptic Plasticity [PDF]
Membrane receptors for neuromodulators (NM) are highly regulated in their distribution and efficacy - a phenomenon which influences the individual cell's response to central signals of NM release. Even though NM receptor regulation is implicated in the pharmacological action of many drugs, and is also known to be influenced by various environmental ...
arxiv +1 more source
Widespread decreases in cortical muscarinic receptors in a subset of people with schizophrenia.
These studies were undertaken to investigate the selectivity of cortical muscarinic receptor radioligand binding in muscarinic M(1) and M(4) receptor knockout mice and to determine whether a marked decrease in [(3)H]pirenzepine binding in Brodmann's area
A. Gibbons+6 more
semanticscholar +1 more source
Multitargeting nature of muscarinic orthosteric agonists and antagonists
Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor (GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ...
Jaromir Myslivecek
doaj +1 more source
Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogenous time-resolved FRET [PDF]
Flp-In T-REx 293 cells expressing a wild type human M muscarinic acetylcholine receptor construct constitutively and able to express a Receptor Activated Solely by Synthetic Ligand (RASSL) form of this receptor on demand maintained response to the ...
Alvarez-Curto, Elisa+3 more
core +2 more sources
Antidepressant-like Effects of Neuropeptide SF (NPSF) [PDF]
Neuropeptide SF (NPSF) is a member of RFamide neuropeptides that play diverse roles in central nervous system. Little is know about the effects of NPSF on brain functions. Antidepressant-like effect of NPSF was studied in modified mice FST. NPSF showed the antidepressant-like effects by decreasing the immobility time and increasing the climbing and ...
arxiv
A copper‐catalyzed decarboxylative alkynylation of tropanes is developed. This approach works under mild conditions and selectively produces a range of 3‐β‐alkynylated tropanes. Moreover, it provides a versatile and convergent platform for further functionalization of the triple bond.
Mayssa Zayene+6 more
wiley +1 more source
An in vivo biosensor for neurotransmitter release and in situ receptor activity. [PDF]
Tools from molecular biology, combined with in vivo optical imaging techniques, provide new mechanisms for noninvasively observing brain processes. Current approaches primarily probe cell-based variables, such as cytosolic calcium or membrane potential ...
Griesbeck, Oliver+6 more
core +2 more sources
Sympathetic nerve innervation promotes the progression of Epstein‐Barr virus‐positive diffuse large B‐cell lymphoma (EBV+ DLBCL) via β2‐adrenergic receptors. The discovery of enhanced nerve infiltration and β2AR expression reveals a novel mechanism and highlights the sympathetic–β2AR axis as a promising target for therapeutic intervention in EBV+ DLBCL.
Silan Huang+10 more
wiley +1 more source