The nicotinic receptor of cochlear hair cells: A possible pharmacotherapeutic target? [PDF]
Mechanosensory hair cells of the organ of Corti transmit information regarding sound to the central nervous system by way of peripheral afferent neurons.
Elgoyhen, Ana Belen+2 more
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SARS-CoV-2 infection was announced as a pandemic in March 2020. Since then, several scientists have focused on the low prevalence of smokers among hospitalized COVID-19 patients. These findings led to our hypothesis that the Nicotinic Cholinergic System (
Nikolaos Alexandris+9 more
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A photoisomerizable muscarinic antagonist. Studies of binding and of conductance relaxations in frog heart [PDF]
These experiments employ the photoisomerizable compound, 3,3'-bis- [alpha-(trimethylammonium)methyl]azobenzene (Bis-Q), to study the response to muscarinic agents in frog myocardium. In homogenates from the heart, trans-Bis-Q blocks the binding of [3H]-N-
Birdsall, Nigel J. M.+5 more
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Agonist activation of a nicotinic acetylcholine receptor [PDF]
How does an agonist activate a receptor? In this article I consider the activation process in muscle nicotinic acetylcholine receptors (AChRs), a prototype for understanding the energetics of binding and gating in other ligand-gated ion channels. Just as movements that generate gating currents activate voltage-gated ion channels, movements at binding ...
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Activation of muscle nicotinic acetylcholine receptor channels by nicotinic and muscarinic agonists [PDF]
The dose‐response parameters of recombinant mouse adult neuromuscular acetylcholine receptor channels (nAChR) activated by carbamylcholine, nicotine, muscarine and oxotremorine were measured. Rate constants for agonist association and dissociation, and channel opening and closing, were estimated from single‐channel kinetic analysis.
Gustav Akk, Anthony Auerbach
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Recently, we discovered a cholinergic mechanism that inhibits the adenosine triphosphate (ATP)-dependent release of interleukin-1β (IL-1β) by human monocytes via nicotinic acetylcholine receptors (nAChRs) composed of α7, α9 and/or α10 subunits ...
Anna Zakrzewicz+17 more
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Small molecule ligands for α9 * and α7 nicotinic receptors: A survey and an update, respectively
The α9- and α7-containing nicotinic acetylcholine receptors (nAChRs) mediate numerous physiological and pathological processes by complex mechanisms that are currently the subject of intensive study and debate.
Alessandro Giraudo+2 more
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An expanding range of targets for kynurenine metabolites of tryptophan [PDF]
The kynurenine pathway of tryptophan metabolism accounts for most of the tryptophan that is not committed to protein synthesis and includes compounds active in the nervous and immune systems.
Darlington, L. Gail+2 more
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Acute Administration of Desformylflustrabromine Relieves Chemically Induced Pain in CD-1 Mice
Neuronal nicotinic acetylcholine receptors are cell membrane-bound ion channels that are widely distributed in the central nervous system. The α4β2 subtype of neuronal nicotinic acetylcholine receptor plays an important role in modulating the ...
Loni A. Weggel, Anshul A. Pandya
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Caenorhabditis elegans muscle Cys-loop receptors as novel targets of terpenoids with potential anthelmintic activity [PDF]
The anthelmintic treatment of nematode infections remains the pillar of worm control in both human and veterinary medicine. Since control is threatened by the appearance of drug resistant nematodes, there is a need to develop novel compounds, among which
Bouzat, Cecilia Beatriz+2 more
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