- Identification of a Novel TRPM8 Agonist from Nutmeg: A Promising Cooling Compound
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The transient receptor potential melastatin 8 (TRPM8) ion channel is the primary receptor for innocuous cold stimuli (8′-7-ethoxy-4-hydroxy-3,3′,5′-trimethoxy-8-O-4′-neolignan (1) with an EC50 of 0.332 μM, which was isolated from a well-known spice, nutmeg (Myristica fragrans Houtt.). Structure activity relationships are also disclosed, showing that the 7-d-menthoxy derivative is the most potent agonist (EC50 = 11 nM). The combination of 1 and l-(-)-menthol has an additive effect, suggesting that neolignan compounds interact with TRPM8 at different sites from those of l-(-)-menthol.
- Shirai, Tomohiro,Kumihashi, Kentaro,Sakasai, Mitsuyoshi,Kusuoku, Hiroshi,Shibuya, Yusuke,Ohuchi, Atsushi
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p. 715 - 719
(2017/07/22)
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- Flavor composition
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PROBLEM TO BE SOLVED: To provide a flavoring composition comprising a novel compound useful for giving a cold sensation and a flavor giving method using the flavoring composition.SOLUTION: A compound represented by formula (I) is contained in an amount of
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- Cooling Agent and TRPM8 Activator
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Provided are a cooling agent having an excellent TRPM8 activating action, a TRPM8 activator, a method for imparting cooling sensation, and a novel compound useful for imparting cooling sensation. Disclosed is a cooling agent comprising, as an active ingre
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- PYRIDAZINONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT
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It is to provide a novel pyridazinone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1 represents H or C1-6 alkyl, each of R2 and R3 represents H, X, C1-6 alkoxy, Z represents O or S, and A represents AA or BB, wherein AA represents: and BB represents: wherein R4 represents H or C1-6 alkyl, and each of R5 and R6 represents C1-6 alkyl.
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Page/Page column 169
(2010/04/25)
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- PYRAZOLONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT
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It is to provide a novel pyrazolone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1,R2: C1-6 alkyl; R3,R4: H, X, C1-6 alkoxy; Z:O, S; A:AA, BB, wherein AA represents wherein BB represents wherein R5: H, C1-6 alkyl ; R6,R7: C1-6 alkyl.
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Page/Page column 120
(2010/04/25)
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