Results 31 to 40 of about 32,846 (260)

A Cation-π Interaction in the Binding Site of the Glycine Receptor Is Mediated by a Phenylalanine Residue [PDF]

, 2008
Cys-loop receptor binding sites characteristically contain many aromatic amino acids. In nicotinic ACh and 5-HT3 receptors, a Trp residue forms a cation-{pi} interaction with the agonist, whereas in GABAA receptors, a Tyr performs this role.
Dougherty, Dennis A., Hanek, Ariele P., Lester, Henry A., Lummis, Sarah C. R., Lynch, Joseph W., Millen, Kat S., Pless, Stephan A.   +6 more
core   +2 more sources

TC299423, a Novel Agonist for Nicotinic Acetylcholine Receptors [PDF]

Frontiers in Pharmacology, 2017
(E)-5-(Pyrimidin-5-yl)-1,2,3,4,7,8-hexahydroazocine (TC299423) is a novel agonist for nicotinic acetylcholine receptors (nAChRs). We examined its efficacy, affinity, and potency for α6β2∗ (α6β2-containing), α4β2∗, and α3β4∗ nAChRs, using [125I]-epibatidine binding, whole-cell patch-clamp recordings, synaptosomal 86Rb+ efflux, [3H]-dopamine release, and
Teagan R. Wall, Brandon J. Henderson, George Voren, Charles R. Wageman, Purnima Deshpande, Bruce N. Cohen, Sharon R. Grady, Michael J. Marks, Michael J. Marks, Daniel Yohannes, Paul J. Kenny, Merouane Bencherif, Henry A. Lester   +12 more
openaire   +4 more sources

Canonical and Novel Non-Canonical Cholinergic Agonists Inhibit ATP-Induced Release of Monocytic Interleukin-1β via Different Combinations of Nicotinic Acetylcholine Receptor Subunits α7, α9 and α10

Frontiers in Cellular Neuroscience, 2017
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, Katrin Richter, Alisa Agné, Sigrid Wilker, Kathrin Siebers, Bijan Fink, Gabriela Krasteva-Christ, Gabriela Krasteva-Christ, Gabriela Krasteva-Christ, Mike Althaus, Mike Althaus, Winfried Padberg, Arik J. Hone, J. Michael McIntosh, J. Michael McIntosh, J. Michael McIntosh, Veronika Grau, Veronika Grau   +17 more
doaj   +1 more source

Agonist activation of a nicotinic acetylcholine receptor [PDF]

Neuropharmacology, 2015
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 ...
openaire   +2 more sources

Small molecule ligands for α9 * and α7 nicotinic receptors: A survey and an update, respectively

Pharmacological Research, 2023
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, Marco Pallavicini, Cristiano Bolchi   +2 more
doaj   +1 more source

Suppression of methamphetamine-seeking behavior by nicotinic agonists [PDF]

Proceedings of the National Academy of Sciences, 2006
To understand the mechanism of methamphetamine (MAP) craving from the viewpoint of nicotinic acetylcholinergic transmission, we examined the responsible site of the brain for anticraving effects produced by nicotinic agonists by using a MAP self-administration paradigm in rats.
Takato, Hiranita, Yoko, Nawata, Katsuya, Sakimura, Kusnandar, Anggadiredja, Tsuneyuki, Yamamoto   +4 more
openaire   +2 more sources

Acute Administration of Desformylflustrabromine Relieves Chemically Induced Pain in CD-1 Mice

Molecules, 2019
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
doaj   +1 more source

Dyskinesia and brain-derived neurotrophic factor levels after long-term levodopa and nicotinic receptor agonist treatments in female mice with near-total unilateral dopaminergic denervation

BMC Neuroscience, 2018
Background The treatment of Parkinson’s disease is often complicated by levodopa-induced dyskinesia (LID). Nicotinic acetylcholine receptor agonists can alleviate LID in animal models but may be less effective in conditions of severe dopaminergic ...
Sakari Leino, Samuel Kohtala, Tomi Rantamäki, Sini K. Koski, Saara Rannanpää, Outi Salminen   +5 more
doaj   +1 more source

Alpha9 nicotinic acetylcholine receptors and the treatment of pain [PDF]

, 2009
Chronic pain is a vexing worldwide problem that causes substantial disability and consumes significant medical resources. Although there are numerous analgesic medications, these work through a small set of molecular mechanisms.
Absalom, Nathan, Chebib, Mary, Elgoyhen, Ana Belen, McIntosh, J. Michael, Vincler, Michelle   +4 more
core   +1 more source

Developmental sex differences in nicotinic currents of prefrontal layer VI neurons in mice and rats.

PLoS ONE, 2010
BackgroundThere is a large sex difference in the prevalence of attention deficit disorder; yet, relatively little is known about sex differences in the development of prefrontal attention circuitry.
Nyresa C Alves, Craig D C Bailey, Raad Nashmi, Evelyn K Lambe   +3 more
doaj   +1 more source