Results 31 to 40 of about 10,698 (157)

Sleep-related hypermotor epilepsy associated mutations uncover important kinetic roles of α4β2- nicotinic acetylcholine receptor intracellular structures.

PLoS ONE, 2021
Sleep-related hypermotor epilepsy (SHE) is a group of seizure disorders prominently associated with mutations in nicotinic acetylcholine receptors (nAChR). The most prevalent central nervous system nAChR subtype contains α4 and β2 subunits, in two ratios.
Maegan M Weltzin, Andrew A George, Ronald J Lukas, Paul Whiteaker   +3 more
doaj   +1 more source

Degradation kinetics of α‐conotoxin TxID

FEBS Open Bio, 2019
α‐Conotoxin (CTx) TxID is a potent α3β4 nicotinic acetylcholine receptor (nAChR) antagonist that has been suggested as a potential drug candidate to treat addiction and small cell lung cancer.
Pan Xu, Yang Xiong, Yiqiao Liu, Shurun Yu, Dongting Zhangsun, Yong Wu, Sulan Luo   +6 more
doaj   +1 more source

TC299423, a Novel Agonist for Nicotinic Acetylcholine Receptors

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 ...
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
doaj   +1 more source

(-)-Pentylsedinine, a New Alkaloid from the Leaves of with Agonist Activity at Nicotinic Acetylcholine Receptor

Natural Product Communications, 2015
Lobelia tupa , also called devil's tobacco, is a native plant from the center-south of Chile which has been used by the native people of Chile as a hallucinogenic and anesthetic plant.
Cristian Paz, José Becerra, Mario Silva, Viviana Burgos, Matthias Heydenreich, Bernd Schmidt, Thu Tran, Irina Vetter   +7 more
doaj   +1 more source

High-throughput cell-based assays for identifying antagonists of multiple smoking-associated human nicotinic acetylcholine receptor subtypes

SLAS Discovery, 2022
There is substantial evidence that in addition to nicotine, other compounds found in tobacco smoke significantly influence smoking behavior. Further, recent years have seen an explosion in the availability of non-combusted products that deliver nicotine,
Michelle Kassner, J. Brek Eaton, Nanyun Tang, Joachim L. Petit, Nathalie Meurice, Hongwei Holly Yin, Paul Whiteaker   +6 more
doaj   +1 more source

Suggested conserved amino acid sequence for reversal of α3β4 nAChR inhibition by Aβ.

, 2013
Suggested conserved amino acid sequence for reversal of α3β4 nAChR inhibition by Aβ.
Cleber A. Trujillo (350391), Luciana B. Sathler (435560), Sergio T. Ferreira (310090), Luiz Juliano (56592), Arthur A. Nery (435559), Margaret H. Magdesian (347034), Henning Ulrich (184271), Maria A. Juliano (92351)   +7 more
core   +1 more source

AChBP-targeted alpha-conotoxin correlates distinct binding orientations with nAChR subtype selectivity [PDF]

, 2007
Neuronal nAChRs are a diverse family of pentameric ion channels with wide distribution throughout cells of the nervous and immune systems. However, the role of specific subtypes in normal and pathological states remains poorly understood due to the lack ...
Sixma, Titia K., Alewood, Paul F., Buettner, Regina, van Elk, R, Smit, A.B., Sixma, T., Dutertre, S., Nicke, A, van Elk, R., Smit, A., Nicke, Annette, Alewood, P. F., Sixma, T.K., Kendel, Y., Smit, AB, Lewis, R. J., Hopping, G., Kendel, Y, van Elk, René, Büttner, Regina, Elk, René van, Ulens, C, Ulens, Chris, Buttner, R, Kendel, Yvonne, Sixma, TK, Fish, Alexander, Lewis, R.J., Schroeder, Christina, Lewis, Richard,, Smit, August,, Buttner, R., Elk, R. van, Alewood, P.F., Lewis, Richard J., Fish, A, Sixma, Titia,, Schroeder, C., Alewood, Paul,, Fish, A., Alewood, P., Dutertre, Sébastien, Smit, August B., Ulens, C., Hopping, Gene, Nicke, A., Lewis, R.   +46 more
core   +1 more source

Molecular Regulation of Betulinic Acid on α3β4 Nicotinic Acetylcholine Receptors

Molecules, 2021
Betulinic acid (BA) is a major constituent of Zizyphus seeds that have been long used as therapeutic agents for sleep-related issues in Asia. BA is a pentacyclic triterpenoid. It also possesses various anti-cancer and anti-inflammatory effects.
Shinhui Lee, Woog Jung, Sanung Eom, Hye Duck Yeom, Heui-Dong Park, Junho H. Lee   +5 more
doaj   +1 more source

α-Conotoxin [S9A]TxID Potently Discriminates between α3β4 and α6/α3β4 Nicotinic Acetylcholine Receptors

, 2017
α3β4 nAChRs have been implicated in various pathophysiological conditions. However, the expression profile of α3β4 nAChRs and α6/α3β4 nAChRs overlap in a variety of tissues.
Wu, Yong, Sulan Luo, Zhangsun, Manqi, Manqi Zhangsun, Zhangsun, Dongting, Peta J. Harvey, Craik, David J., McIntosh, J. Michael, Luo, Sulan, Zhu, Xiaopeng, Harvey, Peta J., Quentin Kaas, Kaas, Quentin, Xiaopeng Zhu, David J. Craik, Dongting Zhangsun, Yong Wu, J. Michael McIntosh   +17 more
core   +1 more source

Structural mechanisms for α-conotoxin activity at the human α3β4 nicotinic acetylcholine receptor

, 2017
Nicotinic acetylcholine receptors (nAChR) are therapeutic targets for a range of human diseases. α-Conotoxins are naturally occurring peptide antagonists of nAChRs that have been used as pharmacological probes and investigated as drug leads for nAChR ...
Paul F. Alewood, Nikita Abraham, Andreas Brust, Lotten Ragnarsson, Michael Healy, Richard J. Lewis   +5 more
core   +2 more sources