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Neurochemical and Molecular Pharmacological Aspects of the GABAB Receptor

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Abstract

Metabotropic γ-aminobutyric acid (GABA)B receptors are known to modulate the synaptic release of various neurotransmitters in the nervous system. Activation of GABAB receptor induces the inhibition of adenylyl cyclase activity, while it does not stimulate the formation of inositol phosphates. Activation of a potassium conductance and suppression of a calcium conductance are also recognized, similarly to some of G protein-coupled receptors. Recent molecular cloning has revealed that GABAB receptor possesses a large extracellular domain including the binding site for GABA and seven transmembrane domains. Their molecular structures in the brain are unique and interesting because of heterodimerization consisting of two distinct genes: GABABR1 and GABABR2. Such assembled receptors can be classified as a novel type of the metabotropic receptor superfamily.

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  1. President office and Department of Pharmacology, Meiji College of Oriental Medicine, Hiyoshi-cho, Funai-gun, Kyoto, 629-0392, Japan

    Kinya Kuriyama

  2. Molecular Neuroscience Research Center, Shiga University of Medical Science, Seta-Tsukinowacho, Otsu, 520-2192, Japan

    Masaaki Hirouchi & Hiroshi Kimura

  3. Research Laboratories, Nippon Shinyaku Co., Ltd., 14 Nishi nosho-Monguchi-cho, Kisshoin, Minami-ku, Kyoto 601-8550, Japan

    Masaaki Hirouchi

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Kuriyama, K., Hirouchi, M. & Kimura, H. Neurochemical and Molecular Pharmacological Aspects of the GABAB Receptor. Neurochem Res 25, 1233–1239 (2000). https://doi.org/10.1023/A:1007640027977

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