Article
Biochemistry & Molecular Biology
Julia Bukanova, Elena Solntseva, Rodion Kondratenko, Eva Kudova
Summary: Epi is a positive modulator of GABA-induced chloride current (I-GABA) with an EC50 of 5.7 μM in Purkinje cells and 9.3 μM in hippocampal neurons. The potentiation of I-GABA by Epi is more pronounced at low GABA concentrations.
Article
Biochemistry & Molecular Biology
Dieter Janzen, Benedikt Slavik, Markus Zehe, Christoph Sotriffer, Helene M. Loos, Andrea Buettner, Carmen Villmann
Summary: This study analyzed the modulatory potential of 11 SQTs at GABA(A) receptors to characterize their potential neurotropic activity. The research found differences in receptor modulation by SQTs in HEK293 cells and neurons, with the presence of gamma(2) and delta subunits being important for SQT modulation. Additionally, the study provided insight into how nutritional digestion can affect the neurotropic potential of natural compounds.
JOURNAL OF NEUROCHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Julia V. Bukanova, Rodion V. Kondratenko, Elena I. Solntseva
Summary: This study investigates the interaction between positive allosteric modulators (PAMs) and competitive antagonists of GABA(A)Rs, demonstrating unblocking effects and revealing an allosteric relationship between these two types of compounds.
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
(2022)
Article
Clinical Neurology
Marwa Elamin, Fouad Lemtiri-Chlieh, Tiwanna M. Robinson, Eric S. Levine
Summary: This study investigates the sodium channel kinetics in Dup15q neurons, a neurodevelopmental disorder associated with autism and seizures. The Dup15q neurons showed increased sodium current density, depolarizing shift in steady-state inactivation, delayed onset of slow inactivation, and faster recovery from inactivation processes. These dysfunctional inactivation kinetics may contribute to the development of seizures in Dup15q patients and suggest the potential use of drugs that modulate inactivation kinetics for therapeutic approaches.
Article
Integrative & Complementary Medicine
Thao Nguyen Thi Phuong, Seon Hui Jang, Santosh Rijal, Woo Kwon Jung, Junghyun Kim, Soo Joung Park, Seong Kyu Han
Summary: The study examined how linalool acted on SG neurons of the Vc in mice, revealing that linalool exhibits GABA- and glycine-mimetic effects. This suggests that linalool can be a promising target molecule for orofacial pain management by activating inhibitory neurotransmission in the SG area of the Vc.
AMERICAN JOURNAL OF CHINESE MEDICINE
(2021)
Article
Biochemistry & Molecular Biology
Katarzyna Terejko, Michal A. Michalowski, Ilona Izykowska, Anna Dominik, Aleksandra Brzostowicz, Jerzy W. Mozrzymas
Summary: GABA type A receptors play a crucial role in mediating inhibition in the adult mammalian brain and have a complex gating mechanism involving openings/closings, preactivation, and desensitization. The ligand binding sites affect the receptor's gating mechanism, suggesting shared structural determinants for distinct conformational transitions.
ACS CHEMICAL NEUROSCIENCE
(2021)
Article
Medicine, Research & Experimental
J. V. Bukanova, E. I. Solntseva, R. V. Kondratenko, V. G. Skrebitsky
Summary: Ivermectin, a macrocyclic lactone used as an antiparasitic agent, is being researched for its potential in treating cancer and viral diseases. This study showed that neuronal glycine receptors are highly sensitive to Ivermectin.
BULLETIN OF EXPERIMENTAL BIOLOGY AND MEDICINE
(2021)
Article
Neurosciences
Fang-Qi Shu, Yun-Gang Lu, Hui-Ping Tang, Zeng-You Ye, Yi-Na Huang, Ming Wang, Zheng-Quan Tang, Lin Chen
Summary: The study found that resveratrol noncompetitively inhibits I-Gly in auditory neurons by decreasing the affinity of glycine to its receptor. These results suggest that the native glycine receptors but not GABA(A) receptors in central neurons are targets of resveratrol during clinical administrations.
BRAIN RESEARCH BULLETIN
(2021)
Article
Neurosciences
Virginia Bazzurro, Elena Gatta, Elena Angeli, Aroldo Cupello, Stefan Lange, Eva Jennische, Mauro Robello, Alberto Diaspro
Summary: The study explored the pharmacological action of the antisecretory factor (AF) on different GABA(A) receptor populations in cerebellar granule cells. It found that AF-16, a peptide derived from the AF protein, can enhance the electrophysiological response in different neuronal regions and suggests the involvement of specific GABA(A) receptor subtypes.
EUROPEAN JOURNAL OF NEUROSCIENCE
(2022)
Article
Neurosciences
Shih-Yin Ho, I-Chun Chen, Che-Wen Tsai, Kai-Chieh Chang, Chun-Jung Lin, Yijuang Chern, Horng-Huei Liou
Summary: The ENT1 inhibitor J7 has been found to have anticonvulsant effects in an animal model of Dravet syndrome, possibly by modulating the presynaptic A1R-mediated signaling in granule cells.
Article
Chemistry, Applied
Seon Hui Jang, Soo Joung Park, Kyoung-A Kim, Seong Kyu Han
Summary: The study found that resveratrol directly affects SG neurons of Vc, potentially inhibiting them through the activation of GABA(A) receptors and/or glycine receptors. This suggests that resveratrol could be a promising therapeutic for orofacial pain modulation.
NATURAL PRODUCT RESEARCH
(2022)
Article
Neurosciences
Sam A. Booker, Anna Sumera, Peter C. Kind, David J. A. Wyllie
Summary: The study found that the contribution of GluN2A subunits to glutamatergic synaptic currents varies among different subclasses of interneurons in the CA1 region of the hippocampus. GluN2A contributes to EPSC in parvalbumin-positive and somatostatin-positive interneurons, while its contribution is negligible in cholecystokinin (CCK)-positive interneurons. Furthermore, synaptic potentiation at glutamatergic synapses on CCK-positive interneurons does not require the activation of GluN2A-containing NMDARs but does rely on the activation of NMDARs containing GluN2B and GluN2D subunits.
Article
Biology
Crescent L. Combe, Carol M. Upchurch, Carmen C. Canavier, Sonia Gasparini
Summary: A combination of in vitro electrophysiology and modeling identified TRPM4 channels as major drivers of cholinergic modulation of firing rate in rat CA1 pyramidal neurons. Cholinergic agonist carbachol reverses the spike rate adaptation caused by Na-V channel inactivation, resulting in more spikes on the down-ramp compared to the up-ramp. Pharmacological experiments and modeling suggest that TRPM4 channels play a role in the cholinergic shift of firing center of mass through Ca2+-activated nonspecific cation current ICAN.
Article
Instruments & Instrumentation
Ian Delgadillo Bonequi, Abraham Stroschein, Lucas J. Koerner
Summary: This article describes a custom and open-source FPGA-based data acquisition system that is used for electrophysiology and closed-loop feedback experiments. The system combines FPGA acquisition and processing with high-speed analog and digital converters to enable real-time feedback. The digital approach simplifies experimental setup and repeatability by allowing for system identification and in situ tuning of filter bandwidths.
REVIEW OF SCIENTIFIC INSTRUMENTS
(2022)
Article
Biochemistry & Molecular Biology
David P. Richards, Rohit N. Patel, Ian R. Duce, Bhupinder P. S. Khambay, Michael A. Birkett, John A. Pickett, Ian R. Mellor
Summary: Ladybird beetles possess strong chemical defences, and recent studies have shown that their alkaloids can target receptors and act as antagonists. This study explored the actions of one particular alkaloid found in ladybirds on different types of receptors.