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Updated: Sep 26, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
[Possible involvement of GABAB receptors in action of antidepressants]
Yutaka Nakagawa1, Tsuyoshi Ishima
1Pharmaceutical Marketing Center, Kyowa Hakko Kogyo Co. Ltd., 1-6-1, Otemachi, Chiyoda-ku, Tokyo, 100-8185 Japan.
Abstract:
Antidepressants are divided into several groups such as monoamine oxidase inhibitors, serotonin reuptake inhibitors, noradrenaline reuptake inhibitors and alpha-adrenoceptor antagonists. Antidepressants show, however, a common clinical profile: their clinical actions occur after a chronic treatment. It is, therefore, suggested that antidepressants have a common pharmacological profile. We reviewed possible involvement of gamma-aminobutyric acid (GABA)B receptors in action of antidepressants. Our data in combination with previous ones from other laboratories suggest that antidepressants suppress the activity of presynaptic 5-hydroxytryptamine3 receptors on GABA neurons, resulting in the reduction of GABA release. It is likely that the decrease in GABA release attenuates GABAB receptor-mediated neurotransmission, thereby upregulating GABAB receptors.
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