Shigeyuki Chaki

Summary

Affiliation: Taisho Pharmaceutical Co
Country: Japan

Publications

  1. doi request reprint mGlu2/3 and mGlu5 receptors: potential targets for novel antidepressants
    Shigeyuki Chaki
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Neuropharmacology 66:40-52. 2013
  2. ncbi request reprint [The potential of group II metabotropic glutamate receptor antagonists as a novel antidepressant]
    Shigeyuki Chaki
    Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, 331 9530 Japan
    Nihon Shinkei Seishin Yakurigaku Zasshi 32:219-26. 2012
  3. ncbi request reprint Targeting of metabotropic glutamate receptors for the treatment of schizophrenia
    Shigeyuki Chaki
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Curr Pharm Des 17:94-102. 2011
  4. doi request reprint Group II metabotropic glutamate receptor agonists as a potential drug for schizophrenia
    Shigeyuki Chaki
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Eur J Pharmacol 639:59-66. 2010
  5. ncbi request reprint MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama 331 9530, Japan
    Neuropharmacology 46:457-67. 2004
  6. ncbi request reprint ATC0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety
    Shigeyuki Chaki
    Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    CNS Drug Rev 11:341-52. 2005
  7. ncbi request reprint Anxiolytic- and antidepressant-like profile of a new CRF1 receptor antagonist, R278995/CRA0450
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama, Japan
    Eur J Pharmacol 485:145-58. 2004
  8. ncbi request reprint MCL0042: a nonpeptidic MC4 receptor antagonist and serotonin reuptake inhibitor with anxiolytic- and antidepressant-like activity
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama, Japan
    Pharmacol Biochem Behav 82:621-6. 2005
  9. ncbi request reprint Involvement of the melanocortin MC4 receptor in stress-related behavior in rodents
    Shigeyuki Chaki
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Eur J Pharmacol 474:95-101. 2003
  10. ncbi request reprint [Targeting metabotropic glutamate receptors to develop novel antipsychotics]
    Shigeyuki Chaki
    Molecular Function and Pharmacology Laboratories, Pharmaceutical Business Group, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama 331 8530, Japan
    Nihon Shinkei Seishin Yakurigaku Zasshi 30:207-13. 2010

Collaborators

Detail Information

Publications73

  1. doi request reprint mGlu2/3 and mGlu5 receptors: potential targets for novel antidepressants
    Shigeyuki Chaki
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Neuropharmacology 66:40-52. 2013
    ..This article is part of a Special Issue entitled 'Metabotropic Glutamate Receptors'...
  2. ncbi request reprint [The potential of group II metabotropic glutamate receptor antagonists as a novel antidepressant]
    Shigeyuki Chaki
    Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, 331 9530 Japan
    Nihon Shinkei Seishin Yakurigaku Zasshi 32:219-26. 2012
    ..In addition, the potential of other agents targeting glutamatergic transmission for novel antidepressants is being investigated...
  3. ncbi request reprint Targeting of metabotropic glutamate receptors for the treatment of schizophrenia
    Shigeyuki Chaki
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Curr Pharm Des 17:94-102. 2011
    ..This review describes the potential of both mGlu2/3 receptor agonists/potentiators and mGlu1 receptor antagonists for the treatment of schizophrenia...
  4. doi request reprint Group II metabotropic glutamate receptor agonists as a potential drug for schizophrenia
    Shigeyuki Chaki
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Eur J Pharmacol 639:59-66. 2010
    ..Possible neuronal circuits through which mGlu(2/3) receptor agonists exert their pharmacological effects have also been investigated...
  5. ncbi request reprint MGS0039: a potent and selective group II metabotropic glutamate receptor antagonist with antidepressant-like activity
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama 331 9530, Japan
    Neuropharmacology 46:457-67. 2004
    ..These results indicate that MGS0039 is a potent and selective antagonist of group II mGluR, and that group II mGluR antagonists, like MGS0039, have an antidepressant-like potential in experimental animal models...
  6. ncbi request reprint ATC0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety
    Shigeyuki Chaki
    Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    CNS Drug Rev 11:341-52. 2005
    ..In addition, ATC0175 was well tolerated in rat repeated toxicity study, and had no genotoxic liability. Therefore, ATC0175 has the potential to be effective in the treatment of patients with depression and/or anxiety disorders...
  7. ncbi request reprint Anxiolytic- and antidepressant-like profile of a new CRF1 receptor antagonist, R278995/CRA0450
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama, Japan
    Eur J Pharmacol 485:145-58. 2004
    ..These results indicate that R278995/CRA0450 is an orally active CRF(1) and sigma(1) receptor antagonist with potent anxiolytic-like and antidepressant-like activities...
  8. ncbi request reprint MCL0042: a nonpeptidic MC4 receptor antagonist and serotonin reuptake inhibitor with anxiolytic- and antidepressant-like activity
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama, Japan
    Pharmacol Biochem Behav 82:621-6. 2005
    ..Moreover, blockade of both the MC4 receptor and serotonin reuptake sites might represent a useful approach in the treatment of anxiety and depression...
  9. ncbi request reprint Involvement of the melanocortin MC4 receptor in stress-related behavior in rodents
    Shigeyuki Chaki
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Eur J Pharmacol 474:95-101. 2003
    ..Taken together our findings suggest that the melanocortin MC4 receptor might be related to stress-induced changes in behavior, and blockade of the melanocortin MC4 receptor may prevent stress-induced disorders such as anxiety...
  10. ncbi request reprint [Targeting metabotropic glutamate receptors to develop novel antipsychotics]
    Shigeyuki Chaki
    Molecular Function and Pharmacology Laboratories, Pharmaceutical Business Group, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama 331 8530, Japan
    Nihon Shinkei Seishin Yakurigaku Zasshi 30:207-13. 2010
    ..Therefore, mGlu2/3 receptor and mGlu5 receptor may provide exciting targets for the development of novel medications for schizophrenia...
  11. ncbi request reprint Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists
    Shigeyuki Chaki
    Taisho Pharmaceutical Co, Ltd, Saitama, Japan
    J Pharmacol Exp Ther 313:831-9. 2005
    ..These findings indicate that ATC0065 and ATC0175 are potent and orally active MCHR1 antagonists with anxiolytic and antidepressant activity in rodents...
  12. ncbi request reprint Melanocortin-4 receptor antagonists for the treatment of depression and anxiety disorders
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Yoshino cho, Kita ku, Saitama, Saitama, Japan
    Curr Top Med Chem 7:1145-51. 2007
    ..This review describes the involvement of the MC4 receptor in stress response and discusses the potential value of MC4 receptor antagonists for the treatment of stress-related disorders such as depression and anxiety...
  13. ncbi request reprint Non-monoamine-based approach for the treatment of depression and anxiety disorders
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Recent Pat CNS Drug Discov 1:1-27. 2006
    ..Here, we review recent patents and advances in research on these emerging molecular targets for the treatment of depression and anxiety, and discuss their advantages over currently used antidepressants and anxiolytics...
  14. ncbi request reprint Anxiolytic-like and antidepressant-like activities of MCL0129 (1-[(S)-2-(4-fluorophenyl)-2-(4-isopropylpiperadin-1-yl)ethyl]-4-[4-(2-methoxynaphthalen-1-yl)butyl]piperazine), a novel and potent nonpeptide antagonist of the melanocortin-4 receptor
    Shigeyuki Chaki
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Saitama, Japan
    J Pharmacol Exp Ther 304:818-26. 2003
    ..MC4 receptor antagonists may prove effective for treating subjects with stress-related disorders such as depression and/or anxiety...
  15. ncbi request reprint Group II metabotropic glutamate receptor-mediated regulation of dopamine release from slices of rat nucleus accumbens
    Shigeyuki Chaki
    Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Kita ku, Saitama, Japan
    Neurosci Lett 404:182-6. 2006
    ....
  16. ncbi request reprint Cocaine- and amphetamine-regulated transcript peptide produces anxiety-like behavior in rodents
    Shigeyuki Chaki
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Saitama 330 8530, Saitama, Japan
    Eur J Pharmacol 464:49-54. 2003
    ..As CART-(55-102) produced anxiety-like effects in rodents, this peptide may possibly be involved in anxiety and stress-related behavior...
  17. ncbi request reprint [Neuropeptide receptors: novel therapeutic targets for depression]
    Shigeyuki Chaki
    Nihon Yakurigaku Zasshi 127:196-200. 2006
  18. ncbi request reprint In vitro and in vivo pharmacological profile of 4-(4-fluorobenzylidene)-1-[2-[5-(4-fluorophenyl)-1H-pyrazol-4-yl] ethyl] piperidine (NRA0161)
    Yoshiko Suzuki
    Molecular Biology Laboratory, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Saitama shi, Saitama, 330 8530, Japan
    Life Sci 71:2603-15. 2002
    ..These findings suggest that NRA0161 may have atypical antipsychotic activities yet without producing extrapyramidal side effects...
  19. ncbi request reprint Neuropharmacological profiles of antagonists of group II metabotropic glutamate receptors
    Naoya Kawashima
    Research Strategy Group, Pharmaceutical Business Division, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Neurosci Lett 378:131-4. 2005
    ..These findings suggest that modulation of serotonergic neuron might be, at least in part, responsible for the antidepressant-like effects of group II mGluR antagonists...
  20. ncbi request reprint Prodrugs of 3-(3,4-dichlorobenzyloxy)-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (MGS0039): a potent and orally active group II mGluR antagonist with antidepressant-like potential
    Akito Yasuhara
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Saitama shi, Saitama 331 9530, Japan
    Bioorg Med Chem 14:4193-207. 2006
    ..In this paper, we report the synthesis, in vitro metabolic stabilities, and pharmacokinetic profiles of the prodrugs of 5, and the antidepressant-like effects of 7ao...
  21. ncbi request reprint AMPA receptor stimulation mediates the antidepressant-like effect of a group II metabotropic glutamate receptor antagonist
    Jun Ichi Karasawa
    Medicinal Pharmacology Laboratory, Taisho Pharmaceutical Co, Ltd, Kita ku, Saitama 331 9530, Japan
    Brain Res 1042:92-8. 2005
    ..Pretreatment with NBQX significantly attenuated the increase in serotonin release by MGS0039. These findings suggest that stimulation of postsynaptic AMPA receptors plays a role in mediating the pharmacological effects of MGS0039...
  22. doi request reprint AMPA receptor mediates mGlu 2/3 receptor antagonist-induced dopamine release in the rat nucleus accumbens shell
    Jun Ichi Karasawa
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, Kita ku, Saitama, Japan
    Neurochem Int 57:615-9. 2010
    ..These findings suggest that the activation of the postsynaptic AMPA receptor plays a role in mediating the regulation of dopamine release by the mGlu 2/3 receptor in the NAc shell...
  23. ncbi request reprint Effects of metabotropic glutamate 2/3 receptor antagonists in the stress-induced hyperthermia test in singly housed mice
    Michihiko Iijima
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, Saitama, Japan
    Psychopharmacology (Berl) 190:233-9. 2007
    ..Recently, modulation of the group II metabotropic glutamate (mGlu) 2/3 receptor has been proposed as a novel therapeutic approach for psychiatric disorders...
  24. ncbi request reprint In vitro and in vivo pharmacological profile of 5-[2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl]-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide (NRA0562), a novel and putative atypical antipsychotic
    Takeo Funakoshi
    CNS Diseases Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Saitama, Saitama 330 8530, Japan
    Life Sci 71:1371-84. 2002
    ....
  25. ncbi request reprint Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1
    Kosuke Kanuma
    Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Bioorg Med Chem Lett 15:3853-6. 2005
    ..4 nM) as well as good selectivity over the Y5 and the alpha2A receptors...
  26. ncbi request reprint Novel piperazines: potent melanocortin-4 receptor antagonists with anxiolytic-like activity
    Dai Nozawa
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Bioorg Med Chem 15:2375-85. 2007
    ..In this paper, we report the synthesis, structure-activity relationships, and oral activity of the novel mono-piperazines as MC4 receptor antagonists...
  27. ncbi request reprint Synthesis, in vitro pharmacology, and structure-activity relationships of 2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as mGluR2 antagonists
    Akito Yasuhara
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama shi, Saitama 331 9530, Japan
    Bioorg Med Chem 14:3405-20. 2006
    ..This paper reports on the synthesis, in vitro pharmacological profile, and structure-activity relationships (SARs) of 3-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid...
  28. doi request reprint Effect of an mGlu2/3 receptor antagonist on depressive behavior induced by withdrawal from chronic treatment with methamphetamine
    Michihiko Iijima
    Discovery Pharmacology І, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama, Japan
    Behav Brain Res 246:24-8. 2013
    ....
  29. doi request reprint Involvement of the mammalian target of rapamycin signaling in the antidepressant-like effect of group II metabotropic glutamate receptor antagonists
    Hiroyuki Koike
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Neuropharmacology 61:1419-23. 2011
    ..The present result suggests that the blockade of the mGlu2/3 receptor may activate mTOR signaling, and that the activation of mTOR signaling may contribute to the sustained antidepressant-like effects of mGlu2/3 receptor antagonists...
  30. doi request reprint Acute and sustained effects of a metabotropic glutamate 5 receptor antagonist in the novelty-suppressed feeding test
    Michihiko Iijima
    Discovery Pharmacology I, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Behav Brain Res 235:287-92. 2012
    ....
  31. ncbi request reprint Antipsychotic action of selective group II metabotropic glutamate receptor agonist MGS0008 and MGS0028 on conditioned avoidance responses in the rat
    Kazuaki Takamori
    Research Management Section, Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, 1 403, Yoshino cho, Saitama, Japan
    Life Sci 73:1721-8. 2003
    ..Since this effect is seen with a wide range of antipsychotics, such as haloperidol and clozapine [Life Sciences 71 (2002) 947], group II mGluR agonists deserve further attention for possible antipsychotic activity...
  32. ncbi request reprint An mGluR2/3 antagonist, MGS0039, exerts antidepressant and anxiolytic effects in behavioral models in rats
    Takao Yoshimizu
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Psychopharmacology (Berl) 186:587-93. 2006
    ..1.0]hexane-2,6-dicarboxylic acid (MGS0039) is a selective antagonist for group II metabotropic glutamate receptors (mGluR2/3), and that it exerted antidepressant effects in some animal behavioral tests...
  33. ncbi request reprint Identification of arginine analogues as antagonists and agonists for the melanocortin-4 receptor
    Dai Nozawa
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama, Japan
    Chem Pharm Bull (Tokyo) 55:1232-9. 2007
    ..The synthesis and structure-activity relationships of the arginine analogues as MC4 receptor ligands were described in this paper...
  34. ncbi request reprint Synthesis of diphenylmethyl analogues and their affinity for the melanocortin-4 receptor and the serotonin transporter
    Dai Nozawa
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama, Japan
    Chem Pharm Bull (Tokyo) 55:1044-50. 2007
    ..7 nM). Here, we describe the synthesis and biological evaluation of various diphenylmethyl analogues in relation to their actions on the MC4 receptor and the serotonin transporter...
  35. ncbi request reprint Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists
    Kosuke Kanuma
    Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Bioorg Med Chem 14:3307-19. 2006
    ....
  36. ncbi request reprint Design, synthesis, and structure-activity relationships of novel tetracyclic compounds as peripheral benzodiazepine receptor ligands
    Taketoshi Okubo
    Medicinal Chemistry Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama shi, Saitama 331 9530, Japan
    Bioorg Med Chem 12:3569-80. 2004
    ..44nM, 12f: IC(50)=0.37nM). In this paper, we present the design, synthesis, and structure-activity relationships (SARs) of novel tetracyclic compounds...
  37. ncbi request reprint In vitro and antinociceptive profile of HON0001, an orally active NMDA receptor NR2B subunit antagonist
    Sayoko Suetake-Koga
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama, Saitama 331 9530, Japan
    Pharmacol Biochem Behav 84:134-41. 2006
    ....
  38. ncbi request reprint D-Serine and a glycine transporter inhibitor improve MK-801-induced cognitive deficits in a novel object recognition test in rats
    Jun Ichi Karasawa
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama 331 9530, Japan
    Behav Brain Res 186:78-83. 2008
    ..The results also suggest that enhancing NMDA receptor function is an effective way for treating the cognitive deficits associated with schizophrenia...
  39. doi request reprint Role of BDNF/TrkB signaling in antidepressant-like effects of a group II metabotropic glutamate receptor antagonist in animal models of depression
    Hiroyuki Koike
    Discovery Pharmacology I, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Behav Brain Res 238:48-52. 2013
    ..These results suggest that BDNF/TrkB signaling may be involved in the sustained antidepressant-like effects of LY341495, as observed for ketamine treatment...
  40. doi request reprint Synthesis, in vitro pharmacology, and pharmacokinetic profiles of 2-[1-amino-1-carboxy-2-(9H-xanthen-9-yl)-ethyl]-1-fluorocyclopropanecarboxylic acid and its 6-heptyl ester, a potent mGluR2 antagonist
    Kazunari Sakagami
    Medicinal Chemistry Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama shi, Saitama 331 9530, Japan
    Bioorg Med Chem 16:4359-66. 2008
    ..49 nM) for mGluR2 as 1 but had a superior pharmacokinetic profile. Furthermore, a marked elevation of the plasma levels of (+)-16a was observed following the administration of a prodrug, (+)-17...
  41. doi request reprint D-Serine and a glycine transporter-1 inhibitor enhance social memory in rats
    Toshiharu Shimazaki
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama, 331 9530, Japan
    Psychopharmacology (Berl) 209:263-70. 2010
    ..Clinical evidence demonstrates that positive modulation of "glycine modulatory sites" on N-methyl-D: -aspartic acid (NMDA) receptors improve cognitive deficits as well as positive and negative symptoms in schizophrenic patients...
  42. ncbi request reprint Neuropharmacological profile of an atypical antipsychotic, NRA0562
    Shiho Hirota
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    CNS Drug Rev 9:375-88. 2003
    ..In vivo assays for extrapyramidal side effect liability showed that NRA0562 has a low rate of neurological side effects. Thus, NRA0562 may have unique antipsychotic activity with a lower propensity for extrapyramidal side effects...
  43. ncbi request reprint A metabotropic glutamate 2/3 receptor antagonist, MGS0039, increases extracellular dopamine levels in the nucleus accumbens shell
    Jun Ichi Karasawa
    Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Saitama 331 9530, Japan
    Neurosci Lett 393:127-30. 2006
    ....
  44. ncbi request reprint Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1
    Kosuke Kanuma
    Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Bioorg Med Chem Lett 15:2565-9. 2005
    ..The preliminary optimization resulted in the identification of compounds 20, 21, and 23...
  45. doi request reprint Involvement of AMPA receptor in both the rapid and sustained antidepressant-like effects of ketamine in animal models of depression
    Hiroyuki Koike
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Behav Brain Res 224:107-11. 2011
    ....
  46. ncbi request reprint Anxiolytic-like activity of MGS0039, a potent group II metabotropic glutamate receptor antagonist, in a marble-burying behavior test
    Toshiharu Shimazaki
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Eur J Pharmacol 501:121-5. 2004
    ..We also demonstrated that this effect was significantly attenuated by a group II mGlu receptor agonist. This data indicates that group II mGlu receptor antagonists may exert anti-obsessive-compulsive disorder effects in clinical use...
  47. ncbi request reprint Blockade of the metabotropic glutamate 2/3 receptors enhances social memory via the AMPA receptor in rats
    Toshiharu Shimazaki
    Medicinal Pharmacology Laboratory, Medical Research Laboratories, Taisho Pharmaceutical Co, Saitama, Saitama, Japan
    Eur J Pharmacol 575:94-7. 2007
    ..p.) in the social recognition test. These results suggest that the mGlu(2/3) receptor blockade increases social recognition memory, presumably through stimulation of the AMPA receptor...
  48. ncbi request reprint Synthesis, in vitro pharmacology, structure-activity relationships, and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives as potent and selective group II metabotropic glutamate receptor antagonists
    Atsuro Nakazato
    Medicinal Chemistry Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama shi, Saitama 331 9530, Japan
    J Med Chem 47:4570-87. 2004
    ..1.0]hexane-2,6-dicarboxylic acid derivatives 11 and 12, and pharmacokinetic profiles of several typical compounds...
  49. ncbi request reprint Stimulation of metabotropic glutamate (mGlu) 2 receptor and blockade of mGlu1 receptor improve social memory impairment elicited by MK-801 in rats
    Hirohiko Hikichi
    Discovery Pharmacology I, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, Japan
    J Pharmacol Sci 122:10-6. 2013
    ....
  50. doi request reprint Effects of agents targeting glutamatergic systems on marble-burying behavior
    Michihiko Iijima
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Neurosci Lett 471:63-5. 2010
    ..Furthermore, agents targeting glutamateric systems such as an AMPA receptor potentiator and an NR2B receptor antagonist, may be useful in treating OCD...
  51. ncbi request reprint Increase in secretion of glial cell line-derived neurotrophic factor from glial cell lines by inhibitors of vacuolar ATPase
    Mariko Nishiguchi
    Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Saitama, Saitama 330 8530, Japan
    Neurochem Int 42:493-8. 2003
    ..The V-type ATPase inhibitors may be beneficial to use for the treatment of diseases in which increase in GDNF could be effective...
  52. ncbi request reprint Monkey corticotropin-releasing factor1 receptor: Complementary DNA cloning and pharmacological characterization
    Yuichi Oshida
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita, Saitama, Saitama 331 9530, Japan
    Life Sci 74:1911-24. 2004
    ..Monkey CRF1 was expressed abundantly in the pituitary, cerebral cortex, hippocampus, amygdala and cerebellum. Thus the monkey CRF1 receptor and the human CRF1 receptor have similar molecular and pharmacological characteristics...
  53. ncbi request reprint Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor
    Dai Nozawa
    Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Bioorg Med Chem 15:1989-2005. 2007
    ..13nM. In this paper, we present the design, synthesis, and structure-activity relationships of the novel bis-piperazines as MC4 receptor antagonists...
  54. ncbi request reprint An arginine vasopressin V1b antagonist, SSR149415 elicits antidepressant-like effects in an olfactory bulbectomy model
    Michihiko Iijima
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Prog Neuropsychopharmacol Biol Psychiatry 31:622-7. 2007
    ..Furthermore, blockade of the V(1b) receptor or the CRF1 receptor may be useful in treating subjects suffering from chronic stressful conditions...
  55. ncbi request reprint Electrophysiological effects of melanocortin receptor ligands on neuronal activities of monoaminergic neurons in rats
    Naoya Kawashima
    Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Neurosci Lett 353:119-22. 2003
    ..The MC4 receptor mediating multiple regulation on the monoaminergic neuronal system may, in part, relate to stress responses (anxiety and/or depressive behavior)...
  56. ncbi request reprint Melanin-concentrating hormone MCH1 receptor antagonists: a potential new approach to the treatment of depression and anxiety disorders
    Toshiharu Shimazaki
    Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, Saitama, Japan
    CNS Drugs 20:801-11. 2006
    ....
  57. ncbi request reprint Design, synthesis and structure-affinity relationships of aryloxyanilide derivatives as novel peripheral benzodiazepine receptor ligands
    Taketoshi Okubo
    Medicinal Chemistry Laboratory, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama shi, Saitama 331 9530, Japan
    Bioorg Med Chem 12:423-38. 2004
    ..These novel derivatives would be useful for exploring the functions of PBR. In this paper, the design, synthesis and structure-affinity relationships of aryloxyanilide derivatives are described...
  58. ncbi request reprint Anxiolytic-like effect of a selective and non-peptidergic melanocortin 4 receptor antagonist, MCL0129, in a social interaction test
    Toshiharu Shimazaki
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Pharmacol Biochem Behav 80:395-400. 2005
    ..These results suggest that MC4 receptor is involved in social interaction, and that MCL0129, an MC4 receptor antagonist, has an anxiolytic-like effect in this model...
  59. ncbi request reprint Increased cell proliferation in the adult mouse hippocampus following chronic administration of group II metabotropic glutamate receptor antagonist, MGS0039
    Takao Yoshimizu
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Biochem Biophys Res Commun 315:493-6. 2004
    ..These findings raise the possibility that MGS0039 may exert antidepressant-like effects by modulating cell proliferation in the hippocampus...
  60. ncbi request reprint Separation-induced ultrasonic vocalization in rat pups: further pharmacological characterization
    Michihiko Iijima
    Psychiatric Diseases and Pain Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, Kita ku, Saitama, Japan
    Pharmacol Biochem Behav 82:652-7. 2005
    ..Moreover, the present data support the usefulness of SIV for evaluating the anxiolytic-like activity of mechanically diverse compounds...
  61. doi request reprint Effects of quercetin on the sleep-wake cycle in rats: involvement of gamma-aminobutyric acid receptor type A in regulation of rapid eye movement sleep
    Daiji Kambe
    Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Brain Res 1330:83-8. 2010
    ..c.v. injection of bicuculline. Therefore, the present results suggest that quercetin alters the sleep-wake cycle partly through activation of GABA(A) receptors...
  62. ncbi request reprint The pituitary mediates the anxiolytic-like effects of the vasopressin V1B receptor antagonist, SSR149415, in a social interaction test in rats
    Toshiharu Shimazaki
    Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Eur J Pharmacol 543:63-7. 2006
    ..These results suggest that the anxiolytic effects of the vasopressin V(1B) receptor antagonist in the social interaction test are mediated through blockade of the vasopressin V(1B) receptor in the pituitary...
  63. ncbi request reprint XIB4035, a novel nonpeptidyl small molecule agonist for GFRalpha-1
    Kimiko Tokugawa
    CNS Diseases Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Saitama, Saitama 330 8530, Japan
    Neurochem Int 42:81-6. 2003
    ..This is an interesting finding showing that a nonpeptidyl small molecule is capable of inducing activation of a receptor that normally bind a relatively large protein ligand such as GDNF...
  64. ncbi request reprint Antipsychotic profile of 5-[2-[4-(6-fluoro-1H-indole-3-yl)piperidin-1-yl]ethyl]-4-(4-fluorophenyl)thiazole-2-carboxylic acid amide (NRA0562) in rats
    Kazuaki Takamori
    CNS Diseases Research, Medicinal Pharmacology Laboratory, Medicinal Research Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403, Yoshino cho, Saitama, Saitama 330 8530, Japan
    Life Sci 71:947-52. 2002
    ..o.) potently impaired the conditioned avoidance response.These results suggest that antipsychotic profile of NRA0562 is consistent with profiles of clozapine or risperidone and may be considered an atypical antipsychotic agent...
  65. doi request reprint Pharmacological characterization of repeated corticosterone injection-induced depression model in rats
    Michihiko Iijima
    Discovery Pharmacology, Molecular Function and Pharmacology Laboratories, Taisho Pharmaceutical Co, Ltd, 1 403 Yoshino cho, Kita ku, Saitama, Saitama 331 9530, Japan
    Brain Res 1359:75-80. 2010
    ..Based on previous findings and the present results, this model could be used as an animal model of PMD and may be useful for evaluating the antidepressant-like potential of compounds targeting the HPA axis...
  66. ncbi request reprint Involvement of melanocortin-4 receptor in anxiety and depression
    Shigeyuki Chaki
    Medicinal Research Laboratories, Taisho Pharmaceutical Co Ltd, 1 403 Yoshino cho, Kita ku, Saitama 331 9530, Japan
    Peptides 26:1952-64. 2005
    ....
  67. pmc Metabotropic glutamate receptors: potential drug targets for psychiatric disorders
    Akito Yasuhara
    Medicinal Chemistry Laboratories, Taisho Pharmaceutical Co, Ltd
    Open Med Chem J 4:20-36. 2010
    ..This article reviews recent advances in development of each mGlu receptor ligands and their therapeutic potential...
  68. ncbi request reprint The role of the DRY motif of human MC4R for receptor activation
    Yoshiaki Yamano
    Department of Biochemistry and Biotechnology, Faculty of Agriculture, Tottori University, Tottori, Japan
    Biosci Biotechnol Biochem 68:1369-71. 2004
    ..While no MC4R ligand binding was detected in any of the mutants, one mutant, D146A, resulted in higher cAMP production in cells than the wild-type receptor without ligand stimulation...
  69. ncbi request reprint Regulation of CRF, POMC and MC4R gene expression after electrical foot shock stress in the rat amygdala and hypothalamus
    Yoshiaki Yamano
    Department of Biochemistry and Biotechnology, Faculty of Agriculture, Tottori University, Japan
    J Vet Med Sci 66:1323-7. 2004
    ..These results have provided the first evidence that exposure to stress increases expression of the MC4R system in the amygdala and hypothalamus...
  70. ncbi request reprint [MC4 receptor]
    Shigeyuki Chaki
    Nihon Yakurigaku Zasshi 128:53-5. 2006
  71. doi request reprint Mood disorders: regulation by metabotropic glutamate receptors
    Andrzej Pilc
    Institute of Pharmacology, Polish Academy of Sciences and Collegium Medicum, Jagiellonian University, Krakow, Poland
    Biochem Pharmacol 75:997-1006. 2008
    ....
  72. ncbi request reprint Polyamine transport, accumulation, and release in brain
    Takashi Masuko
    Graduate School of Pharmaceutical Sciences, Chiba University, Chiba, Japan
    J Neurochem 84:610-7. 2003
    ..Spermine was found to be accumulated in synaptic vesicles and was released from rat hippocampal slices by depolarization using a high concentration of KCl. Polyamines, in particular spermine, may function as neuromodulators in the brain...
  73. ncbi request reprint Phencyclidine-induced cognitive deficits in mice are improved by subsequent subchronic administration of the glycine transporter-1 inhibitor NFPS and D-serine
    Kenji Hashimoto
    Division of Clinical Neuroscience, Chiba University Center for Forensic Mental Health, 1 8 1 Inohana, Chiba, Japan
    Eur Neuropsychopharmacol 18:414-21. 2008
    ....