100962-76-3Relevant academic research and scientific papers
Cyclohexanol analogues are positive modulators of GABAA receptor currents and act as general anaesthetics in vivo
Hall, Adam C.,Griffith, Theanne N.,Tsikolia, Maia,Kotey, Francesca O.,Gill, Nikhila,Humbert, Danielle J.,Watt, Erin E.,Yermolina, Yuliya A.,Goel, Shikha,El-Ghendy, Bahaa,Hall, C. Dennis
experimental part, p. 175 - 181 (2012/05/04)
GABAA receptors meet all the pharmacological criteria required to be considered important general anaesthetic targets. In the following study, the modulatory effects of various commercially available and novel cyclohexanols were investigated on recombinant human γ-aminobutyric acid (GABA A, α1β2γ2s) receptors expressed in Xenopus oocytes, and compared to the modulatory effects on GABA currents observed with exposures to the intravenous anaesthetic agent, propofol. Submaximal EC20 GABA currents were typically enhanced by co-applications of 3-300 μM cyclohexanols. For instance, at 30 μM 2,6-diisopropylcyclohexanol (a novel compound) GABA responses were increased ～ 3-fold (although similar enhancements were achieved at 3 μM propofol). As regards rank order for modulation by the cyclohexanol analogues at 30 μM, the % enhancements for 2,6-dimethylcyclohexanol ～ 2,6-diethylcyclohexanol ～ 2,6-diisopropylcyclohexanol ～ 2,6-di-sec-butylcyclohexanol ?2,6-di-tert-butylcyclohexanol ～ 4-tert-butylcyclohexanol > cyclohexanol ～ cyclopentanol ～ 2-methylcyclohexanol. We further tested the potencies of the cyclohexanol analogues as general anaesthetics using a tadpole in vivo assay. Both 2,6-diisopropylcyclohexanol and 2,6- dimethylcyclohexanol were effective as anaesthetics with EC50s of 14.0 μM and 13.1 μM respectively, while other cyclohexanols with bulkier side chains were less potent. In conclusion, our data indicate that cyclohexanols are both positive modulators of GABAA receptors currents and anaesthetics. The positioning and size of the alkyl groups at the 2 and 6 positions on the cyclohexanol ring were critical determinants of activity.
Compounds for mass coloration of high temperature polymers
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Example A2, (2008/06/13)
The invention relates to novel soluble pigment precursors possessing not only higher thermal stability but also improved solubility characteristics and to a process for mass coloration of high temperature polymers that utilizes these novel soluble pigment precursors. The pigment precursors of the invention are essentially of the formula A(B)x??(I) where x is an integer from 1 to 8, A is the radical of a chromophore of the quinacridone, anthraquinone, perylene, indigo, quinophthalone, indanthrone, isoindolinone, isoindoline, dioxazine, azo, phthalocyanine or diketopyrrolopyrrole series, this radical being linked with xB groups via one or more heteroatoms, these heteroatoms being selected from the group consisting of N, O and S and forming part of the radical A, and B is hydrogen or a group of the formula although at least one B group is not hydrogen and when x is from 2 to 8 the B groups may be identical or different. E1, E2, R1, R2, R3, R4, R7, R11, R14and G1are as defined in the specification. Also claimed are some materials pigmented according to the invention.
