[Pharmacological studies on the new indene derivatives with beta-adrenergic blocking activity (author's transl)].
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Some derivatives of N'-(5-nitro-2-furoyl)-N2-(3-chloro-1H-indenyl-2-methylene)hydrazine (I) were synthesized and screened for in vitro antimicrobial activity. None was more active than the parent compound and the greater hydrophilic character was associated with loss of inhibitory activity against gram-negative bacteria.
Mixtures of organic solvents are used extensively in industry. The aim of this study was to develop a method for the determination of components of commercial multi-component solvent mixtures, and to perform qualitative and quantitative analyses of the mixtures. Farbasol, Solvesso and Shellsol mixtures were analysed by gas chromatography with a mass spectrometry detector (GC/MS). The composition of mixtures was determined using the mass spectrum computer analysis. Fractions of alkyl benzene, naphthalene and diphenyl derivatives were isolated. The proportions of the individual fractions in the mixtures differed. A predominant fraction was present in each mixture. Solvents (trimethylbenzene, tetramethylbenzene, ethyltoluene, diethylbenzene, isopropylotoulene) which significantly increase health risk due to their suspected neurotoxicity, were identified in each mixture.
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Intracellular recordings were made from bullfrog sympathetic ganglion cells to elucidate effects of 2-n-butyl-1-(4-methylpiperazinyl)-5,6-methylenedioxyindene.2 HCl (TN-871) on synaptic transmission. TN-871 at 30 nM augmented cholinergic nicotinic fast excitatory postsynaptic potentials (fast EPSPs), whereas the drug at 3 microM reversibly depressed them, without affecting acetylcholine-induced depolarizations. TN-871 did not affect active and passive electrical properties of the ganglion cells. The quantal analysis method was applied to the fast EPSPs in a 0.54 mM Ca2+/7.56 mM Mg2+ Ringer's solution. The mean quantal content was significantly increased by TN-871 at 30 nM but significantly decreased at 3 microM. TN-871 at 300 nM either increased or decreased the mean quantal content. The mean quantal size of the fast EPSPs was not changed by TN-871 at the concentrations examined. Fast EPSPs in a 0.99 mM Ca2+/4.86 mM Mg2+ Ringer's solution were not affected by nicardipine, but were inhibited in amplitude by omega-conotoxin in a concentration-dependent manner. It is likely that TN-871, in high concentrations, might block omega-conotoxin-sensitive N-type calcium channels in the presynaptic terminals. These results indicate that TN-871 modulates transmitter release from preganglionic nerve terminals without changing the postsynaptic sensitivity of the ganglion cells to ACh.