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provides coniferyl ferulate(CAS#:580-22-3) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
Background and Purpose
The aim of this study was to compare the abilities of cannabidiolic acid methyl ester (HU‐580) and cannabidiolic acid (CBDA) to enhance 5‐HT1A receptor activation in vitro and produce 5‐HT1A‐mediated reductions in nausea and anxiety in vivo.
We investigated the effects of HU‐580 and CBDA on (i) activation by 8‐hydroxy‐2‐(di‐n‐propylamino)tetralin of human 5‐HT1A receptors in CHO cell membranes, using [35S]‐GTPγS binding assays, (ii) gaping by rats in acute and anticipatory nausea models, and (iii) stress‐induced anxiety‐like behaviour, as indicated by exit time from the light compartment of a light-dark box of rats subjected 24 h earlier to six tone‐paired foot shocks.
HU‐580 and CBDA increased the Emax of 8‐hydroxy‐2‐(di‐n‐propylamino) tetralin in vitro at 0.01-10 and 0.1-10 nM, respectively, and reduced signs of (i) acute nausea at 0.1 and 1 μg·kg−1 i.p. and at 1 μg·kg−1 i.p., respectively, and (ii) anticipatory nausea at 0.01 and 0.1 μg·kg−1, and at 0.1 μg·kg−1 i.p. respectively. At 0.01 μg·kg−1, HU‐580, but not CBDA, increased the time foot‐shocked rats spent in the light compartment of a light-dark box. The anti‐nausea and anti‐anxiety effects of 0.01 or 0.1 μg·kg−1 HU‐580 were opposed by the 5‐HT1A antagonist, WAY100635 (0.1 mg·kg−1 i.p.).
Conclusions and Implications
HU‐580 is more potent than CBDA at enhancing 5‐HT1A receptor activation, and inhibiting signs of acute and anticipatory nausea, and anxiety. Consequently, HU‐580 is a potential medicine for treating some nausea and anxiety disorders and possibly other disorders ameliorated by enhancement of 5‐HT1A receptor activation.
Cannabidiolic acid methyl ester, a stable synthetic analogue of cannabidiolic acid, can produce 5‐HT1A receptor‐mediated suppression of nausea and anxiety in rats
Roger G Pertwee,corresponding author 1 Erin M Rock, 2 Kelsey Guenther, 2 Cheryl L Limebeer, 2 Lesley A Stevenson, 1 Christeene Haj, 3 Reem Smoum, 3 Linda A Parker, 2 and Raphael Mechoulam 3
The retinal photocycle dynamics of the fluorescent voltage sensor QuasAr1 (Archaerhodopsin 3 P60S-T80S-D95H-D106H-F161V mutant from Halorubrum sodomense) in pH 8 Tris buffer was studied. The samples were photoexcited to the first absorption band of the protonated retinal Schiff base (PRSB) Ret_580 (absorption maximum at λmax ≈ 580 nm), and the retinal Schiff base photoisomerization and protonation state changes were followed by absorption spectra recordings during light exposure and after light exposure. Ret_580 turned out to be composed of two protonated retinal Schiff base isomers, namely Ret_580I and Ret_580II. Photoexcitation of Ret_580I resulted in barrier-involved isomerization to Ret_540 (quantum yield ≈ 0.056) and subsequent retinal proton release leading to Ret_410 deprotonated retinal Schiff base (RSB). In the dark, Ret_410 partially recovered to Ret_580I and partially stabilized to irreversible Ret_400 due to apoprotein restructuring (Ret_410 lifetime ≈ 2 h). Photoexcitation of Ret_580II resulted in barrier-involved isomerization to Ret_640 (quantum yield ≈ 0.00135) and subsequent deprotonation to Ret_370 (RSB). In the dark, Ret_370 partially recovered to Ret_580II and partially stabilized to irreversible Ret_350 due to apoprotein restructuring (Ret_370 lifetime ≈ 10 h). Photocycle schemes and reaction coordinate diagrams for Ret_580I and Ret_580II were developed and photocyle parameters were determined.
QuasAr1, Archaerhodopsin 3, genetically encoded fluorescent voltage sensor, absorption spectroscopic characterization, fluorescence studies, photocycle dynamics, photoisomerization, deprotonation, reprotonation
Photocycle Dynamics of the Archaerhodopsin 3 Based Fluorescent Voltage Sensor QuasAr1
Alfons Penzkofer,1,* Arita Silapetere,2 and Peter Hegemann2
ESICM LIVES 2016: part three Milan, Italy. 1-5 October 2016
2016 Sep 29