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  1. Article: [Preclinical pharmacological profiles and clinical outcome of the novel melatonin-receptor agonist ramelteon (Rozerem 8 mg).].

    Hirai, Keisuke / Kato, Koki / Nishikawa, Hisao / Yukuhiro, Nobuhito / Nishiyama, Keiji / Miyamoto, Masaomi

    Nihon yakurigaku zasshi. Folia pharmacologica Japonica

    2010  Volume 136, Issue 1, Page(s) 51–60

    MeSH term(s) Animals ; Chronic Disease ; Cyclic AMP/metabolism ; Drug Evaluation, Preclinical ; Humans ; Indenes/administration & dosage ; Indenes/adverse effects ; Indenes/pharmacology ; Randomized Controlled Trials as Topic ; Receptors, Melatonin/agonists ; Sleep Initiation and Maintenance Disorders/drug therapy ; Sleep Stages/drug effects ; Substance-Related Disorders ; Suprachiasmatic Nucleus/drug effects ; Suprachiasmatic Nucleus/physiology
    Chemical Substances Indenes ; Receptors, Melatonin ; ramelteon (901AS54I69) ; Cyclic AMP (E0399OZS9N)
    Language Japanese
    Publishing date 2010-07-08
    Publishing country Japan
    Document type Journal Article ; Review
    ZDB-ID 1097532-9
    ISSN 1347-8397 ; 0015-5691
    ISSN (online) 1347-8397
    ISSN 0015-5691
    DOI 10.1254/fpj.136.51
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 439: Show issues Location:
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  2. Article ; Online: 1,6-Dihydro-2H-indeno[5,4-b]furan derivatives: design, synthesis, and pharmacological characterization of a novel class of highly potent MT₂-selective agonists.

    Koike, Tatsuki / Hoashi, Yasutaka / Takai, Takafumi / Nakayama, Masaharu / Yukuhiro, Nobuhito / Ishikawa, Takashi / Hirai, Keisuke / Uchikawa, Osamu

    Journal of medicinal chemistry

    2011  Volume 54, Issue 9, Page(s) 3436–3444

    Abstract: A novel series of 1,6-dihydro-2H-indeno[5,4-b]furan derivatives were designed and synthesized as MT(2)-selective ligands. This scaffold was identified as a potent mimic of the 5-methoxy indole core of melatonin, and introduction of a cyclohexylmethyl ... ...

    Abstract A novel series of 1,6-dihydro-2H-indeno[5,4-b]furan derivatives were designed and synthesized as MT(2)-selective ligands. This scaffold was identified as a potent mimic of the 5-methoxy indole core of melatonin, and introduction of a cyclohexylmethyl group at the 7-position of this scaffold afforded an MT(2)-selective ligand 15 (K(i) = 0.012 nM) with high MT(1)/MT(2) selectivity (799). Compound 15 was identified as a potent full agonist for the MT(2) subtype and exhibited reentrainment effects to a new light/dark cycle in ICR mice at 3-30 mg/kg. This result demonstrated the involvement of the MT(2) receptors in chronobiotic activity.
    MeSH term(s) Acetamides/chemical synthesis ; Acetamides/chemistry ; Acetamides/pharmacology ; Animals ; Benzofurans/chemical synthesis ; Benzofurans/chemistry ; Benzofurans/pharmacology ; CHO Cells ; Circadian Rhythm ; Cricetinae ; Cricetulus ; Cyclic AMP/biosynthesis ; Darkness ; Humans ; Ligands ; Light ; Male ; Mice ; Mice, Inbred ICR ; Motor Activity/drug effects ; Radioligand Assay ; Receptor, Melatonin, MT1/agonists ; Receptor, Melatonin, MT2/agonists ; Structure-Activity Relationship
    Chemical Substances Acetamides ; Benzofurans ; Ligands ; N-(2-(7-(cyclohexylmethyl)-1,6-dihydro-2H-indeno(5,4-b)furan-8-yl)ethyl)acetamide ; Receptor, Melatonin, MT1 ; Receptor, Melatonin, MT2 ; Cyclic AMP (E0399OZS9N)
    Language English
    Publishing date 2011-05-12
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm200221q
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Effects of ramelteon (TAK-375) on nocturnal sleep in freely moving monkeys.

    Yukuhiro, Nobuhito / Kimura, Hiroyuki / Nishikawa, Hisao / Ohkawa, Shigenori / Yoshikubo, Shin-ichi / Miyamoto, Masaomi

    Brain research

    2004  Volume 1027, Issue 1-2, Page(s) 59–66

    Abstract: We investigated the effects of (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4]furan-8-yl)ethyl]propionamide (ramelteon, TAK-375), a novel MT1/MT2 receptor agonist, on nocturnal sleep in freely moving monkeys and compared these results with those of ... ...

    Abstract We investigated the effects of (S)-N-[2-(1,6,7,8-tetrahydro-2H-indeno-[5,4]furan-8-yl)ethyl]propionamide (ramelteon, TAK-375), a novel MT1/MT2 receptor agonist, on nocturnal sleep in freely moving monkeys and compared these results with those of melatonin and zolpidem. Treatment with ramelteon (0.03 and 0.3 mg/kg, p.o.) significantly shortened latency to sleep onset and significantly increased total duration of sleep. Treatment with melatonin (0.3, 1, and 3 mg/kg, p.o.) also decreased sleep latency, but the effect was weak; the only significant reduction was seen with the 0.3 mg/kg dose on latency to light sleep. Melatonin had no significant effects on the duration of sleep. Zolpidem had no significant effects on latency to sleep onset in this study at any dose (1, 3, 10, and 30 mg/kg, p.o.). The highest dose (30 mg/kg) of zolpidem had a tendency to increase slow wave sleep; however, it also induced apparent sedation and myorelaxation. Treatment with ramelteon and melatonin had no evident effect on the general behavior of the monkeys. Spectral analysis (fast Fourier transform, FFT) of both ramelteon and melatonin revealed sleep patterns that were indistinguishable from those of naturally occurring sleep. The EEG power spectra of zolpidem were qualitatively different from that of naturally occurring physiological sleep. Results of the present study support the investigation of ramelteon as a sleep-promoting agent in humans.
    MeSH term(s) Amides/pharmacology ; Animals ; Dose-Response Relationship, Drug ; Electroencephalography/drug effects ; Female ; Hypnotics and Sedatives/pharmacology ; Indenes/pharmacology ; Macaca fascicularis ; Melatonin/pharmacology ; Polysomnography/drug effects ; Pyridines/pharmacology ; Reaction Time/drug effects ; Receptors, Melatonin/agonists ; Sleep/drug effects ; Time Factors ; Wakefulness/drug effects
    Chemical Substances Amides ; Hypnotics and Sedatives ; Indenes ; Pyridines ; Receptors, Melatonin ; zolpidem (7K383OQI23) ; ramelteon (901AS54I69) ; Melatonin (JL5DK93RCL) ; propionamide (QK07G0HP47)
    Language English
    Publishing date 2004-11-19
    Publishing country Netherlands
    Document type Comparative Study ; Journal Article
    ZDB-ID 1200-2
    ISSN 1872-6240 ; 0006-8993
    ISSN (online) 1872-6240
    ISSN 0006-8993
    DOI 10.1016/j.brainres.2004.08.035
    Database MEDical Literature Analysis and Retrieval System OnLINE

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