- Natural-Product-Derived Transient Receptor Potential Melastatin 8 (TRPM8) Channel Modulators
-
A library of novel structural hybrids of menthol and cubebol was tested for each derivative's ability to interact with the transient receptor potential subfamily melastatin member 8 (TRPM8) channel. This structure-activity relationship study revealed three potent modulators of the TRPM8 ion channel: a novel agonist (4) with an EC50 value of 11 ± 1 μM, an antagonist (15) with an IC50 value of 2 ± 1 μM, and an allosteric modulator (21) that minimized channel desensitization toward menthol. Each of these novel exocyclic olefin analogues of menthol is readily accessible by synthesis and was tested using Ca2+ assays and electrophysiology.
- Legay, Christina M.,Gorobets, Evgueni,Iftinca, Mircea,Ramachandran, Rithwik,Altier, Christophe,Derksen, Darren J.
-
p. 2746 - 2749
(2016/06/15)
-
- Hydrogenation and conformational analysis of (1R,2R,6S)-3-methyl-6-(1- methylethenyl)cyclohex-3-ene-1,2-diol
-
Hydrogenation of (1R,2R,6S)-3-methyl-6-(1-methylethenyl)cyclohex-3-ene-1,2- diol was studied. Nickel chloride-sodium tetrahydridoborate system turned out to selectively reduce the double bond in the isopropenyl group. The results of conformational analysis of (1R,2R,6S)-3-methyl-6-(1-methylethenyl)cyclohex-3- ene-1,2-diol and its partly and completely hydrogenated derivatives were in a good agreement with the NMR data. Pleiades Publishing, Ltd., 2010.
- Ardashov,Genaev,Il'ina,Korchagina,Volcho,Salakhutdinov
-
experimental part
p. 1786 - 1789
(2011/04/17)
-
- Insight into acid-mediated asymmetric spirocyclization in the presence of a chiral diol
-
Asymmetric spirocyclization based on intramolecular conjugate addition using a combination of a Lewis acid and an optically active cyclohexane-1,2-diol has been studied in connection with 1) the effect of substituents on the cyclohexane-1,2-diol and 2) th
- Kiguchi,Tsurusaki,Yamada,Aso,Tanaka,Sakai,Suemune
-
p. 1536 - 1540
(2007/10/03)
-