The mechanisms of potentiation and inhibition of GABA

Autor:	Alexey V, Rossokhin, Irina N, Sharonova, Anton, Dvorzhak, Julia V, Bukanova, Vladimir G, Skrebitsky
Rok vydání:	2019
Předmět:	Mefenamic Acid Purkinje Cells Binding Sites Anti-Inflammatory Agents Non-Steroidal Animals Niflumic Acid Drug Synergism Etomidate GABA-A Receptor Antagonists Receptors GABA-A Anesthetics Intravenous Cells Cultured Rats
Zdroj:	Neuropharmacology. 160
ISSN:	1873-7064
Popis:	Fenamates mefanamic and niflumic acids (MFA and NFA) induced dual potentiating and inhibitory effects on GABA currents recorded in isolated cerebellar Purkinje cells using the whole-cell patch-clamp and fast-application techniques. Regardless of the concentration, both drugs induced a pronounced prolongation of the current response. We demonstrated that the same concentration of drugs can produce both potentiating and inhibitory effects, depending on the GABA concentration, which indicates that both processes take place simultaneously and the net effect depends on the concentrations of both the agonist and fenamate. We found that the NFA-induced block is strongly voltage-dependent. The Woodhull analysis of the block suggests that NFA has two binding sites in the pore - shallow and deep. We built a homology model of the open GABA
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::178d059edc46e513105da4ff9bef1a50 https://pubmed.ncbi.nlm.nih.gov/31560908 Zobrazit plný text záznamu Full Text from ScienceDirect