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In continuation of our published review on general inhalational anesthetics, the current article presents a survey of intravenous agents for general anaesthesia. From chemical point of view these compounds belong to structurally diverse categories, such as barbiturates - thiopental (Sodium pentothal®, Trapanal®, Pentothal®), methohexital (Brevital®), and hexobarbital (Evipan®, Hexenal®, Citopan®, Tobinal®); non-barbiturate derivatives - ketamine (Ketalar® Ketaset®), esketamine (Ketanest®), and etomidate (Amidate®, Hypnomidate®), phenolic derivatives - propofol (Diprivan®); steroid derivatives - mixture of alfadolone and alfaxalone (Althesin® in human and Saffan® in veterinary anesthesia); and derivatives of phenylacetic acid - propanidid (Epontol®, Sombrevin®). Most of these compounds are chiral, with the exception of propofol and propanidid.
View Article and Find Full Text PDFMolecular Docking and Preclinical Study of Five-Membered S,S-Palladaheterocycle as Hepatoprotective Agent.
Adv Pharm Bull
October 2019
Bashkir State Medical University, 3 Lenin Str., 450008 Ufa, Russia.
In order to investigate mechanisms underlying the hepatoprotective action of S,Spalladaheterocycle, inhibition of cytochromes P450 has been modeled by molecular docking of four palladaheterocycle stereoisomers to the active sites of an enzymatic oxidase system. To obtain a deeper insight into biochemical aspects providing a basis for the therapeutic effects of five-membered palladacycles (as mixture of stereoisomers), a number of preclinical trials has been conducted 2D and 3D structures of palladaheterocycle stereoisomers were obtained via converting into SDF files by means of software MarvinSketch. Binding of palladaheterocycle at the active sites of cytochromes P450 2E1 and P450 2C9 has been studied by molecular docking using LeadIT 2.
View Article and Find Full Text PDFEffects of Hypericum montbretti extract on the central nervous system and involvement of GABA (A)/Benzodiazepine receptors in its pharmacological activity.
Phytother Res
November 2012
Department of Pharmacology, Faculty of Pharmacy, Anadolu University, 26470, Eskisehir, Turkey.
The present study was undertaken to investigate the putative activity of a methanol extract of Hypericum montbretti (Guttiferae) on the central nervous system. Rutin (1519 ppm) and quercitrin (784 ppm) were identified as the major phenolic compounds in the extract. When administered at 25, 50 and 100 mg/kg doses, the extract decreased the total number of head-dipping behaviours performed by mice during a hole-board test.
View Article and Find Full Text PDFThe effect of hexenal and nembutal on the tissue bushy receptors was studied the living isolated frog urinary bladder using methylene blue staining. These drugs were shown to induce the changes in the receptor pulse activity which included three phases: an initial sharp increase, an abrupt decline and a low protracted plateau. Reactions to hexenal and nembutal, while possessing some common features, had their own peculiarities.
View Article and Find Full Text PDFPropolis protects CYP 2E1 enzymatic activity and oxidative stress induced by carbon tetrachloride.
Mol Cell Biochem
August 2007
School of Studies in Zoology, Jiwaji University, Gwalior, 474011 MP, India.
Induction of CYP 2E1 by carbon tetrachloride (CCl(4)) is one of the central pathways by which CCl(4) generates oxidative stress in hepatocytes. Experimental liver injury was induced in rats by CCl(4) to determine toxicological actions on CYP 2E1 by microsomal drug metabolizing enzymes. In this report, ethanolic extract of propolis at a dose of 200 mg/kg (po) was used after 24 h of toxicant administration to validate its protective potential.
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