The hypnotic, anxiolytic, and antinociceptive profile of a novel 渭-opioid agonist was written by Montes, Guilherme Carneiro;Monteiro da Silva, Bianca Nascimento;Rezende, Bismarck;Sudo, Roberto Takashi;Ferreira, Vitor Francisco;de Carvalho da Silva, Fernando;Pinto, Angelo da Cunha;Vasconcellos da Silva, Barbara;Zapata-Sudo, Gisele. And the article was included in Molecules in 2017.Recommanded Product: 2-(But-3-yn-1-yloxy)tetrahydro-2H-pyran This article mentions the following:
5′-4-Alkyl/aryl-1H-1,2,3-triazole derivatives I (R = CH2OH, (CH2)5, Ph, etc.) were synthesized and a pharmacol. screening of these derivatives was performed to identify a possible effect on the Central Nervous System (CNS) and to explore the associated mechanisms of action. The mice received a peritoneal injection (100 渭mol/kg) of each of the triazole derivatives 10 min prior to the injection of pentobarbital and the mean hypnosis times were recorded. The mean hypnosis time increased for the mice treated with I (R = (CH2)5) which was prevented when mice were administered CTOP, a 渭-opioid antagonist. Locomotor and motor activities were not affected by I (R = (CH2)5). The anxiolytic effect of I (R = (CH2)5) was evaluated next in an elevated-plus maze apparatus Compound I (R = (CH2)5) and midazolam increased a percentage of entries and spent time in the open arms of the apparatus compared with the control group. Conversely, a decrease in the percentages of entries and time spent in the closed arms were observed Pretreatment with naloxone, a non-specific opioid antagonist, prior to administration of I (R = (CH2)5) exhibited a reverted anxiolytic effect. Compound I (R = (CH2)5) exhibited antinociceptive activity in the hot plate test, and reduced reactivity to formalin in the neurogenic and the inflammatory phases. These data suggest that I (R = (CH2)5) can activate 渭-opioid receptors to provoke antinociceptive and anti-inflammatory effects in mice. In the experiment, the researchers used many compounds, for example, 2-(But-3-yn-1-yloxy)tetrahydro-2H-pyran (cas: 40365-61-5Recommanded Product: 2-(But-3-yn-1-yloxy)tetrahydro-2H-pyran).
2-(But-3-yn-1-yloxy)tetrahydro-2H-pyran (cas: 40365-61-5) belongs to tetrahydropyran derivatives. Tetrahydropyran is an important raw material and intermediate used in Organic Synthesis, Pharmaceuticals, Agrochemicals and dyestuff. The reaction of tertiary 1,4- and 1,5-diols with cerium ammonium nitrate at room temperature gives tetrahydrofuran and tetrahydropyran derivatives in high yield and stereoselectivity. Various fragrant compounds have been synthesized using this method.Recommanded Product: 2-(But-3-yn-1-yloxy)tetrahydro-2H-pyran
Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics