Potentiation of the Ionotropic GABA Receptor Response by Whiskey Fragrance

It is well-known that the target of most mood-defining compounds is an ionotropic γ-aminobutyric acid receptor (GABAA receptor). The potentiation of the response of these inhibitory neurotransmitter receptors induces anxiolytic, sedative, and anesthetic activity in the human brain. To study the effe...

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Bibliographic Details
Published in:Journal of agricultural and food chemistry 2002-11, Vol.50 (23), p.6828-6834
Main Authors: Hossain, Sheikh Julfikar, Aoshima, Hitoshi, Koda, Hirofumi, Kiso, Yoshinobu
Format: Article
Language:English
Subjects:
Alcoholic Beverages
Animals
Brain Chemistry
Cattle
Drug Synergism
Female
GABA Antagonists
Gene Expression
Lactones - pharmacology
Male
Odorants
Oocytes - metabolism
Pentylenetetrazole
Phenols - pharmacology
Phenylpropionates - pharmacology
Rats
Rats, Wistar
Receptors, GABA-A - drug effects
Receptors, GABA-A - genetics
Receptors, GABA-A - physiology
Seizures - chemically induced
Transfection
Xenopus
Xenopus laevis
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Summary:It is well-known that the target of most mood-defining compounds is an ionotropic γ-aminobutyric acid receptor (GABAA receptor). The potentiation of the response of these inhibitory neurotransmitter receptors induces anxiolytic, sedative, and anesthetic activity in the human brain. To study the effects of whiskey fragrance on the GABAA receptor-mediated response, GABAA receptors were expressed in Xenopus oocyte by injecting rat whole brain mRNA or cRNA prepared from the cloned cDNA for the α1 and β1 subunits of the bovine receptors. Most whiskey components such as phenol, ethoxy, and lactone derivatives potentiated the electrical responses of GABAA receptors, especially ethyl phenylpropanoate (EPP), which strongly potentiated the response. When this compound was applied to mice through respiration, the convulsions induced by pentetrazole were delayed, suggesting that EPP was absorbed by the brain, where it could potentiate the GABAA receptor responses. The extract of other alcoholic drinks such as wine, sake, brandy, and shochu also potentiated the responses to varying degrees. Although these fragrant components are present in alcoholic drinks at low concentrations (extremely small quantities compared with ethanol), they may also modulate the mood or consciousness of the human through the potentiation of the GABAA receptor response after absorption into the brain, because these hydrophobic fragrant compounds are easily absorbed into the brain through the blood−brain barrier and are several thousands times as potent as ethanol in the potentiation of the GABAA receptor-mediated response. Keywords: Ethyl phenylpropanoate; GABAA receptor; potentiation; whiskey fragrance; Xenopus oocyte
ISSN:0021-8561
1520-5118
DOI:10.1021/jf020448e