Search Results - "Hikichi, Hirohiko"

Targeting of metabotropic glutamate receptors for the treatment of schizophrenia by Chaki, Shigeyuki, Hikichi, Hirohiko

“…The glutamatergic system is involved in a wide range of physiological processes in the brain, and its dysfunction plays an important role in the etiology and…”
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Stimulation of Metabotropic Glutamate (mGlu) 2 Receptor and Blockade of mGlu1 Receptor Improve Social Memory Impairment Elicited by MK-801 in Rats by Hikichi, Hirohiko, Kaku, Ayaka, Karasawa, Jun-ichi, Chaki, Shigeyuki

“…Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. Both the stimulation of the metabotropic glutamate (mGlu) 2/3…”
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Stimulation of postsynapse adrenergic α2A receptor improves attention/cognition performance in an animal model of attention deficit hyperactivity disorder by Kawaura, Kazuaki, Karasawa, Jun-ichi, Chaki, Shigeyuki, Hikichi, Hirohiko

“…•Clonidine improved attention deficit in the 5-trial inhibitory avoidance model.•Guanfacine improved attention deficit in the 5-trial inhibitory avoidance…”
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Discovery and in vitro and in vivo profiles of 4-fluoro- N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]- N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist by Satoh, Atsushi, Nagatomi, Yasushi, Hirata, Yukari, Ito, Satoru, Suzuki, Gentaroh, Kimura, Toshifumi, Maehara, Shunsuke, Hikichi, Hirohiko, Satow, Akio, Hata, Mikiko, Ohta, Hisashi, Kawamoto, Hiroshi

“…We identified 4-fluoro- N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]- N-methylbenzamide 27 as a potent mGluR1 antagonist. The compound possessed…”
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Antipsychotic profiles of TASP0443294, a novel and orally active positive allosteric modulator of metabotropic glutamate 2 receptor by Hikichi, Hirohiko, Hiyoshi, Tetsuaki, Marumo, Toshiyuki, Tomishima, Yasumitsu, Kaku, Ayaka, Iida, Izumi, Urabe, Hiroki, Tamita, Tomoko, Yasuhara, Akito, Karasawa, Jun-ichi, Chaki, Shigeyuki

“…Glutamatergic dysfunction has been implicated in psychiatric disorders such as schizophrenia. The stimulation of metabotropic glutamate (mGlu) 2 receptor has…”
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Preclinical metabolism and the disposition of vornorexant/TS‐142, a novel dual orexin 1/2 receptor antagonist for the treatment of insomnia by Konno, Yoshihiro, Kamigaso, Shunsuke, Toki, Hidetoh, Terasaka, Shuichi, Hikichi, Hirohiko, Endo, Hiromi, Yamaguchi, Jun‐Ichi, Mizuno‐Yasuhira, Akiko

“…We investigated the metabolism and disposition of vornorexant, a novel dual orexin receptor antagonist, in rats and dogs, and clarified in vitro metabolite…”
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Behavioral effects of N -desmethylclozapine on locomotor activity and sensorimotor gating function in mice—Possible involvement of muscarinic receptors by Maehara, Shunsuke, Hikichi, Hirohiko, Ohta, Hisashi

“…Abstract N -desmethylclozapine (NDMC), a major circulating metabolite of the atypical antipsychotic drug, clozapine, and has M1 muscarinic receptor partial…”
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Pharmacological effects of the metabotropic glutamate receptor 1 antagonist compared with those of the metabotropic glutamate receptor 5 antagonist and metabotropic glutamate receptor 2/3 agonist in rodents: detailed investigations with a selective allosteric metabotropic glutamate receptor 1 antagonist, FTIDC [4-[1-(2-fluoropyridine-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide] by Satow, Akio, Maehara, Shunsuke, Ise, Satoko, Hikichi, Hirohiko, Fukushima, Miyuki, Suzuki, Gentaroh, Kimura, Toshifumi, Tanak, Takeshi, Ito, Satoru, Kawamoto, Hiroshi, Ohta, Hisashi

“…The functional roles of metabotropic glutamate receptor (mGluR) 1 in integrative brain functions were investigated using a potent and selective mGluR1…”
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Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: A potential treatment for psychotic disorders by Ito, Satoru, Hirata, Yukari, Nagatomi, Yasushi, Satoh, Atsushi, Suzuki, Gentaroh, Kimura, Toshifumi, Satow, Akio, Maehara, Shunsuke, Hikichi, Hirohiko, Hata, Mikiko, Ohta, Hisashi, Kawamoto, Hiroshi

“…We describe here the discovery and biological profile of a series of isoindolinone derivatives as developed mGluR1 antagonists. Our combined strategy of rapid…”
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Unique antipsychotic activities of the selective metabotropic glutamate receptor 1 allosteric antagonist 2-cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one by Satow, Akio, Suzuki, Gentaroh, Maehara, Shunsuke, Hikichi, Hirohiko, Murai, Takeshi, Murai, Takashi, Kawagoe-Takaki, Hiroko, Hata, Mikiko, Ito, Satoru, Ozaki, Satoshi, Kawamoto, Hiroshi, Ohta, Hisashi

“…A newly discovered metabotropic glutamate receptor (mGluR) 1 allosteric antagonist,…”
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Characterization of metabolic phenotypes of mice lacking GPR61, an orphan G-protein coupled receptor by Nambu, Hirohide, Fukushima, Miyuki, Hikichi, Hirohiko, Inoue, Takao, Nagano, Norihiro, Tahara, Yoshio, Nambu, Tadahiro, Ito, Junko, Ogawa, Yoshihiro, Ozaki, Satoshi, Ohta, Hisashi

“…GPR61 is an orphan G protein-coupled receptor whose function remains unknown. The purpose of the present study is to elucidate the importance of GPR61 in…”
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Antipsychotic effects of N-desmethylclozapine on sensorimotor gating function in rats — Possible involvement of activation of M₁ muscarinic receptors by Maehara, Shunsuke, Satow, Akio, Hikichi, Hirohiko, Ohta, Hisashi

“…N-desmethylclozapine (NDMC), one of the major metabolites of clozapine, has been demonstrated to exhibit partial agonistic activity at M₁ muscarinic receptors…”
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Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl-3,6-dihydropyridine-1(2H)-carboxamide (FTIDC) by Suzuki, Gentaroh, Kimura, Toshifumi, Satow, Akio, Kaneko, Naoki, Fukuda, Junko, Hikichi, Hirohiko, Sakai, Naoko, Maehara, Shunsuke, Kawagoe-Takaki, Hiroko, Hata, Mikiko, Azuma, Tomoko, Ito, Satoru, Kawamoto, Hiroshi, Ohta, Hisashi

“…A highly potent and selective metabotropic glutamate receptor (mGluR) 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,…”
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Correlation of Receptor Occupancy of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Mouse Brain With In vivo Activity of Allosteric mGluR1 Antagonists by Suzuki, Gentaroh, Kawagoe-Takaki, Hiroko, Inoue, Takao, Kimura, Toshifumi, Hikichi, Hirohiko, Murai, Takashi, Satow, Akio, Hata, Mikiko, Maehara, Shunsuke, Ito, Satoru, Kawamoto, Hiroshi, Ozaki, Satoshi, Ohta, Hisashi

“…The aim of this study was to clarify the relationship between receptor occupancy and In vivo pharmacological activity of mGluR1 antagonists. The tritiated…”
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Face-washing behavior induced by the group I metabotropic glutamate receptor agonist (S)-3,5-DHPG in mice is mediated by mGlu1 receptor by HIKICHI, Hirohiko, IWAHORI, Yuki, MURAI, Takeshi, MAEHARA, Shunsuke, SATOW, Akio, OHTA, Hisashi

“…It is known for the non-selective group I metabotropic glutamate (mGlu) receptors agonist (S)-3,5-dihydroxyphenylglycine (S-3,5-DHPG) to cause convulsions,…”
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Safety and pharmacokinetic profiles of MGS0274 besylate (TS‐134), a novel metabotropic glutamate 2/3 receptor agonist prodrug, in healthy subjects by Watanabe, Mai, Marcy, Brian, Kinoshita, Kohnosuke, Fukasawa, Misako, Hikichi, Hirohiko, Chaki, Shigeyuki, Okuyama, Shigeru, Gevorkyan, Hakop, Yoshida, Shigeru

“…Aims The safety and pharmacokinetics of single and multiple doses of a novel mGlu2/3 receptor agonist prodrug, MGS0274 besylate (TS‐134), were investigated in…”
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A Novel Potent and Selective Histamine H 3 Receptor Antagonist Enerisant: In Vitro Profiles, In Vivo Receptor Occupancy, and Wake-Promoting and Procognitive Effects in Rodents by Hino, Noriko, Marumo, Toshiyuki, Kotani, Makiko, Shimazaki, Toshiharu, Kaku-Fukumoto, Ayaka, Hikichi, Hirohiko, Karasawa, Jun-Ichi, Tomishima, Yasumitsu, Komiyama, Hiroko, Tatsuda, Emi, Nozawa, Dai, Nakamura, Toshio, Chaki, Shigeyuki

“…Histamine H receptor antagonists/inverse agonists are known to enhance the activity of histaminergic neurons in the brain, thereby promoting arousal and…”
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Discovery of MGS0274, an ester prodrug of a metabotropic glutamate receptor 2/3 agonist with improved oral bioavailability by Urabe, Hiroki, Miyakoshi, Naoki, Ohtake, Norikazu, Nozoe, Akiko, Ochi, Motoki, Fukasawa, Misako, Kinoshita, Kohnosuke, Yamaguchi, Jun-ichi, Marumo, Toshiyuki, Hikichi, Hirohiko, Chaki, Shigeyuki, Hashihayata, Takashi

“…We previously reported that MGS0008 is a selective group II metabotropic glutamate receptor (mGlu2/3 receptor) agonist that is effective in animal models of…”
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Role of endogenous PACAP in catecholamine secretion from the rat adrenal gland by Fukushima, Y, Hikichi, H, Mizukami, K, Nagayama, T, Yoshida, M, Suzuki-Kusaba, M, Hisa, H, Kimura, T, Satoh, S

“…We elucidated the contribution of endogenous pituitary adenylate cyclase-activating polypeptide (PACAP) to neurally evoked catecholamine secretion from the…”
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Stimulation of the metabotropic glutamate (mGlu) 2 receptor attenuates the MK-801-induced increase in the immobility time in the forced swimming test in rats by Kawaura, Kazuaki, Karasawa, Jun-Ichi, Hikichi, Hirohiko

“…Negative symptoms of schizophrenia are poorly managed using the currently available antipsychotics. Previous studies indicate that agonists of the metabotropic…”
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