Výsledky vyhledávání - "Nobukazu Kakui"

Investigation of the Histamine H3 Receptor Binding Site. Design and Synthesis of Hybrid Agonists with a Lipophilic Side Chain

Autor: Kazuhiko Kato, Takashi Watanabe, Nobukazu Kakui, Makoto Ishikawa, Miki Yamauchi, Toshiaki Kudo, Fumikazu Yokoyama, Yasuo Sato

Publikováno v: Journal of Medicinal Chemistry. 53:6445-6456

As a part of our search for novel histamine H3 receptor agonists, we designed and synthesized hybrid compounds in which the lipophilic (4'-alkylphenylthio)ethyl moiety of a novel H3 receptor agonist, 4-(2-(4'-tert-butylphenylthio)ethyl)-1H-imidazole

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13249cfccf0328693e2405d196ea949f
https://doi.org/10.1021/jm100643t

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EF6265, a novel inhibitor of activated thrombin-activatable fibrinolysis inhibitor, protects against sepsis-induced organ dysfunction in rats*

Autor: Emiko Kato, Hidemi Ishii, Fumi Itoh, Nobukazu Kakui, Kokichi Suzuki, Yuko Muto, Shiro Sakakibara, Hiroyuki Iida

Publikováno v: Critical Care Medicine. 37:1744-1749

Although thrombin-activatable fibrinolysis inhibitor (TAFI) has been implicated as a negative regulator of fibrinolysis, its pathophysiological significance remains to be unveiled. We performed the pharmacologic study to assess the effect of EF6265,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a53c350e6a1e793198ae39fad3e8c1f1
https://doi.org/10.1097/ccm.0b013e31819ffc14

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A Newly Synthesized Poly(ADP-Ribose) Polymerase Inhibitor, DR2313 [2-Methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]: Pharmacological Profiles, Neuroprotective Effects, and Therapeutic Time Window in Cerebral Ischemia in Rats

Autor: Kunihiro Ohkuma, Toshifumi Hasegawa, Midori Ishikawa, Nobukazu Kakui, Hidemitsu Nakajima

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 312:472-481

We investigated the pharmacological profiles of DR2313 [2-methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]pyrimidine-4-one], a newly synthesized poly(ADP-ribose) polymerase (PARP) inhibitor, and its neuroprotective effects on ischemic injuries in vitro and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::186155220d6fa99710d53175ddb28958
https://doi.org/10.1124/jpet.104.075465

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Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice

Autor: Fumikazu Yokoyama, Kazuhiko Kato, Kunihiro Okuma, Makoto Ishikawa, Masayo Oyama, Yasuo Sato, Miki Yamauchi, Rie Shinei, Takako Nagayama, Nobukazu Kakui

Publikováno v: Journal of medicinal chemistry. 53(9)

The terminal nitrogen atom of histamine was modified with lipophilic substituents to investigate the structure-activity relationship of histamine type 3 receptor (H3R) agonists. The introduction of an alkylated benzene rings maintained or increased t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::01ccec4a166828d76ad97181b85ad6b9
https://pubmed.ncbi.nlm.nih.gov/20384344

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Synthesis and structure-activity relationships of N-aryl-piperidine derivatives as potent (partial) agonists for human histamine H3 receptor

Autor: Miki Yamauchi, Takeshi Furuuchi, Makoto Ishikawa, Nobukazu Kakui, Fumikazu Yokoyama, Yasuo Sato

Publikováno v: Bioorganicmedicinal chemistry. 18(14)

4-((1H-Imidazol-4-yl)methyl)-1-aryl-piperazine and piperidine derivatives were designed and synthesized as candidate human histamine type 3 agonists. The piperazine derivatives were found to have low (or no) affinity for human histamine H3 receptor,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2100e2292c2b7224017f4778a3aedcef
https://pubmed.ncbi.nlm.nih.gov/20541426

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Anxiolytic-like profile of mirtazapine in rat conditioned fear stress model: Functional significance of 5-hydroxytryptamine 1A receptor and alpha1-adrenergic receptor

Autor: Koichi Kitamura, Tsukasa Koyama, Fumikazu Yokoyama, Nobukazu Kakui, Miki Yamauchi, Takeshi Inoue, Taiichiro Imanishi

Publikováno v: Pharmacology, biochemistry, and behavior. 92(3)

Mirtazapine is an antidepressant with a unique mechanism of action and has been categorized as a Noradrenergic and Specific Serotonergic Antidepressant (NaSSA). Although numerous clinical trials suggested the usefulness of mirtazapine for not only ma

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3704e82d65c096f401d09981a6b2ee38
https://pubmed.ncbi.nlm.nih.gov/19167420

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Anxiolytic-like profiles of histamine H3 receptor agonists in animal models of anxiety: a comparative study with antidepressants and benzodiazepine anxiolytic

Autor: Makoto Ishikawa, Kunihiro Okuma, Takako Nagayama, Yasuo Sato, Miki Yamauchi, Nobukazu Kakui, Kaname Onozawa, Masayo Oyama, Fumikazu Yokoyama, Rie Shinei

Publikováno v: Psychopharmacology. 205(2)

Histamine H3 receptor functions as a presynaptic auto- and hetero-receptor on histaminergic and non-histaminergic neurons in the brain regulating the synaptic release of numerous neurotransmitters. Therefore, the ligands for this receptor have been p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d570d292981cd4c56019ffc8e4bdc09f
https://pubmed.ncbi.nlm.nih.gov/19357839

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Direct evidence that stimulation of neuropeptide Y Y5 receptor activates hypothalamo-pituitary-adrenal axis in conscious rats via both corticotropin-releasing factor- and arginine vasopressin-dependent pathway

Autor: Nobukazu Kakui, Koichi Kitamura

Publikováno v: Endocrinology. 148(6)

An abundance of data suggests a crucial role of neuropeptide Y (NPY) as an activator of the hypothamamo-pituitary-adrenal (HPA) axis. However, there is quite limited evidence regarding receptors that mediate this response. Here, we address the possib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6fffaf093fc9675eeefb90f1b40348d
https://pubmed.ncbi.nlm.nih.gov/17363455

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The selective serotonin reuptake inhibitor fluvoxamine suppresses post-feeding hyperactivity induced by food restriction in rats

Autor: Fumikazu Yokoyama, Nobukazu Kakui, Kaname Onozawa, Taiichiro Imanishi

Publikováno v: Pharmacology, biochemistry, and behavior. 87(1)

Previous studies demonstrated that rats allowed access to running wheel with food restriction schedules run excessively. This hyperactivity consisted of a pre-feeding activity (an increase in running activity before the feeding time, also termed food

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7cfa1e09d2d32fe3152f7f956621a37b
https://pubmed.ncbi.nlm.nih.gov/17493672

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Pharmacological characterization and feeding-suppressive property of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel, selective, and orally active antagonist for neuropeptide Y Y5 receptor

Autor: Makoto Suzuki, Takako Miyara, Masaharu Sugai, Kenji Asai, Yuji Tabata, Kozo Aoki, Jiro Tanaka, Fukuichi Ohsawa, Yuko Nakatani, Nobukazu Kakui, Hiroshi Kitaguchi, Naomi Masuda, Naoyuki Nishikawa

Publikováno v: The Journal of pharmacology and experimental therapeutics. 317(2)

We evaluated the pharmacological profiles of FMS586 [3-(5,6,7,8-tetrahydro-9-isopropyl-carbazol-3-yl)-1-methyl-1-(2-pyridin-4-yl-ethyl)-urea hydrochloride], a novel tetrahydrocarbazole derivative as a neuropeptide Y (NPY) Y5 receptor antagonist. This

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b37e4a5159b45af10d5b732876eae880
https://pubmed.ncbi.nlm.nih.gov/16436501

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