Sedative Effects of Inhaled Benzylacetone and Structural Features Contributing to Its Activity

Abstract

Benzylacetone is released by heated agarwood, when inhaled it has a potent effect on reducing the locomotor activity of mice. This study investigated the relationships between the sedative activities of benzylacetone and its derivatives as well as the chemical structures of these compounds by comparing their activities in mice treated with a series of compounds. It was demonstrated that benzylacetone-like compounds had sedative activities and their intensities varied depending on the functional group in the carbon chain, the substituent in the benzene ring, and their combinations. A quantitative structure-activity relationship study was carried out using a series of 17 benzylacetone derivatives to determine the structural features with significant for the sedative activity.

Appetite-Enhancing Effects: The Influence of Concentrations of Benzylacetone and <i>trans</i>-Cinnamaldehyde and Their Inhalation Time, as Well as the Effect of Aroma, on Body Weight in Mice

“…9,12) Likewise, locomotor-reducing effects were seen in the mice administered 7.4×10 −6 mg/L benzylacetone in our study, but not in mice exposed to the same dose of transcinnamaldehyde (Figs. 6A, B).…”

“…This is because excitable activities such as jumping and rearing are observed when mice inhale higher doses of the compounds. 9) In 1-d test, benzylacetone and trans-cinnamaldehyde were vaporised in a plastic cage (13 L) using the same procedure followed for evaluation of weight gain. Mice were placed in the cages for 60 min, and subsequently moved to colony cages containing Igloo FastTracs running wheels with counters for mice (MK-713/CU01, Muromachi Kikai Co., Tokyo, Japan).…”

“…Statistical analyses were performed by Dunnett's test, two-way ANOVA and subsequent t-tests with Bonferroni testing for multiple comparisons 3,9) using GraphPad InStat (GraphPad Software Inc.) and R (R Development Core Team, R Foundation for Statistical Computing). A probability level of p<0.05 was considered statistically significant.…”

“…7) It is known that chronic administration of ghrelin leads to increased body weight in rats. 8) However, it is not yet known whether the appetite-enhancing effects are affected by concentration, 9) and/ or inhalation time, 10) and the results differ among inhalation tests. Because appetite may increase after inhalation of the active compounds, weight gain after chronic administration should be investigated.…”

Locomotor-Reducing Activity of Sesquiterpenes Related to <i>Zingiber zerumbet</i> Essential Oil and Hexahydrozerumbone Derivatives

“…4) Most of the effective compounds showed a two-phase effect and effects at lower doses were considered true activity because the mice displayed excited activities, such as jumping and rearing, at higher doses. 8) Statistical Analysis Results were expressed as the mean±standard error of the mean (S.E.M.). Statistical analyses were performed by Dunnett's test using GraphPad Instat (GraphPad Software, San Diego, CA, U.S.A.).…”