Výsledky vyhledávání

Discovery of δ Opioid Receptor Full Inverse Agonists and Their Effects on Restraint Stress-Induced Cognitive Impairment in Mice

Autor: Toru Nemoto, Kennosuke Itoh, Hideaki Fujii, Takashi Iwai, Chiharu Iwamatsu, Mitsuo Tanabe, Eika Higashi, Shigeto Hirayama, Minami Nakamura

Publikováno v: ACS Chemical Neuroscience. 10:2237-2242

The cyclopropylmethyl group in classical δ opioid receptor (DOR) antagonist NTI, BNTX, and NTB was replaced with various electron-withdrawing groups to develop DOR inverse agonists. N-Benzyl NTB derivative SYK-657 was a potent DOR full inverse agoni

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5d1b2a0ab7cd3f13b954e5f668b295e
https://doi.org/10.1021/acschemneuro.9b00067

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Dyadic dynamics of HIV risk among transgender women and their primary male sexual partners: the role of sexual agreement types and motivations

Autor: Don Operario, Toru Nemoto, Sari L. Reisner, Kristi E. Gamarel, Lynae A. Darbes, Colleen C. Hoff, Deepalika Chakravarty

Publikováno v: AIDS Care. 28:104-111

Transgender women—individuals assigned a male sex at birth who identify as women, female, or on the male-to-female (MTF) trans feminine spectrum—are at high-risk of HIV worldwide. Prior research has suggested that transgender women more frequentl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb293e86343caff959a6417ba0ee4abc
https://doi.org/10.1080/09540121.2015.1069788

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Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists

Autor: Shigeto Hirayama, Yusuke Iihara, Takashi Iwai, Hideaki Fujii, Toru Nemoto, Hiroshi Nagase, Eika Higashi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:2927-2930

We synthesized derivatives of the δ opioid receptor (DOR) antagonists naltrindole (NTI) and compound 1 that were modified with small alkyl or fluorinated ethyl substituents on the 17-nitrogen. Although the derivatives showed decreased binding affini

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69a09d107b212b94e6f056d303666e99
https://doi.org/10.1016/j.bmcl.2015.05.038

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Synthesis and Pharmacology of a Novel κ Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton

Autor: Toru Nemoto, Naohisa Wada, Takashi Iwai, Shigeto Hirayama, Hiroshi Nagase, Hideaki Fujii

Publikováno v: ACS Medicinal Chemistry Letters. 5:868-872

We designed and synthesized the 1,3,5-trioxazatriquinane derivatives with m-hydroxyphenyl groups. These compounds include the phenethylamine structure within them, which is a common structure observed in morphinan derivatives like morphine. Among the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cd012ef4f14f21c79a7df9f4ffa326b8
https://doi.org/10.1021/ml5000542

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Design and synthesis of quinolinopropellane derivatives with selective δ opioid receptor agonism

Autor: Ryo Nakajima, Toru Nemoto, Naoshi Yamamoto, Hiroshi Nagase, Shigeto Hirayama, Hideaki Fujii, Takashi Iwai, Shuichi Hirono, Hiroaki Gouda

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24(13):2851-2854

Indolopropellane 2 was reported to show almost no binding affinity to the δ opioid receptor (DOR) in spite of the fact that 2 has both the propellane fundamental skeleton (message part) with binding ability to the opioid receptors and a possible DOR

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6db1a242e9878ad281180f9acf4381e6

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Novel Delta Opioid Receptor Agonists with Oxazatricyclodecane Structure

Autor: Takashi Iwai, Hiroshi Nagase, Mitsuhiko Yamada, Akiyoshi Saitoh, Hideaki Fujii, Kohei Hayashida, Shigeto Hirayama, Toru Nemoto, Akinobu Yokoyama, Eriko Nakata, Yasuhito Uezono, Yuka Sudo

Publikováno v: ACS Medicinal Chemistry Letters. 5:368-372

We synthesized compounds 4a,c-f,h,i containing the oxazatricyclodecane structure from a novel rearrangement reaction product 2a. All the prepared compounds 4a,c-f,h,i exhibited full agonistic activities for the δ opioid receptor (DOR). Among them, t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29bbe0a89d75cf00ba507c7f72336c6f
https://doi.org/10.1021/ml400491k

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Synthesis and evaluation of novel opioid ligands with a C-homomorphinan skeleton

Autor: Kyoko Ishikawa, Hideaki Fujii, Toru Nemoto, Kenichiro Nagai, Kennosuke Itoh, Shigeto Hirayama, Yusuke Mochizuki

Publikováno v: Bioorganicmedicinal chemistry. 24(10)

As the reports about C-homomorphinans with the seven-membered C-ring are much fewer than those of morphinan derivatives with a six-membered C-ring, we attempted to synthesize C-homomorphinan derivatives and to evaluate their opioid activities. C-Homo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c84caade615f85effeec5f106ed92c1c
https://pubmed.ncbi.nlm.nih.gov/27079125

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Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 3: Synthesis of decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position and their pharmacologies

Autor: Shigeto Hirayama, Hideaki Fujii, Hiroshi Nagase, Satomi Imaide, Shuichi Hirono, Hiroaki Gouda, Toru Nemoto

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:7711-7714

To clarify the essential structures of an opioid κ receptor selective agonist, nalfurafine, for binding to the κ receptor, we designed and synthesized the decahydro(iminoethano)phenanthrene derivatives with an oxygen functionality at the 3-position

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef697b2e0387a8143aa0586c0314d7f1
https://doi.org/10.1016/j.bmcl.2012.09.101

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Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: Part 3, novel propellane derivatives with pentacyclic skeletons

Autor: Hiroshi Nagase, Toru Nemoto, Shigeto Hirayama, Ryo Nakajima, Naoshi Yamamoto, Shuichi Hirono, Hiroaki Gouda, Hideaki Fujii, Junko Akiyama

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:7697-7701

Previously reported propellane derivative KNT-42 preferred the κ receptor and functioned as a message part in the message-address concept, but its affinity for the κ receptor was not high. To improve affinity, we synthesized five pentacyclic propel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6e566c414cf9a6170614b5df96592b29
https://doi.org/10.1016/j.bmcl.2012.09.102

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Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: Synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies

Autor: Shigeto Hirayama, Hideaki Fujii, Satomi Imaide, Toru Nemoto, Hiroshi Nagase

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:5071-5074

To clarify the essential structures of an opioid κ receptor selective agonist, nalfurafine, for binding to the κ receptor, we designed and synthesized some nalfurafine derivatives and the decahydro(iminoethano)phenanthrene derivatives with a cycloh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::782e2714e2231970d707127f6f688a33
https://doi.org/10.1016/j.bmcl.2012.05.122

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