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Hiroshi Nagase

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Yoshikazu Watanabe; Toru Nemoto; Hideaki Fujii; Shigeto Hirayama; Takashi Iwai; Shota Kitazawa; Hiroshi Nagase
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton having a 7-amide side chain and their pharmacologies.
Toru Nemoto; Miyuki Tomatsu; Naohisa Wada; Naoshi Yamamoto; Hideaki Fujii; Yukimasa Harada; Shigeto Hirayama; Marina Ishihara; Takashi Iwai; Hiroshi Nagase
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
Naohisa Wada; Toru Nemoto; Hideaki Fujii; Shigeto Hirayama; Takashi Iwai; Koji Koyano; Hiroshi Nagase
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 3: synthesis of novel triplet drugs with the bis(epoxymethano) or bis(dimethylepoxymethano) structure (double-capped triplet).

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All Publications

2013: Yoshikazu Watanabe; Toru Nemoto; Hideaki Fujii; Shigeto Hirayama; Takashi Iwai; Shota Kitazawa; Hiroshi Nagase
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton having a 7-amide side chain and their pharmacologies.
Bioorganic & medicinal chemistry 2013;21(11):3032-50.
2013: Toru Nemoto; Miyuki Tomatsu; Naohisa Wada; Naoshi Yamamoto; Hideaki Fujii; Yukimasa Harada; Shigeto Hirayama; Marina Ishihara; Takashi Iwai; Hiroshi Nagase
The effect of 17-N substituents on the activity of the opioid κ receptor in nalfurafine derivatives.
Bioorganic & medicinal chemistry letters 2013;23(1):268-72.
2012: Naohisa Wada; Toru Nemoto; Hideaki Fujii; Shigeto Hirayama; Takashi Iwai; Koji Koyano; Hiroshi Nagase
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 3: synthesis of novel triplet drugs with the bis(epoxymethano) or bis(dimethylepoxymethano) structure (double-capped triplet).
Bioorganic & medicinal chemistry letters 2012;22(24):7551-4.
2012: Hideaki Fujii; Hiroaki Gouda; Shigeto Hirayama; Shuichi Hirono; Ryo Nakajima; Toru Nemoto; Naoshi Yamamoto; Junko Akiyama; Hiroshi Nagase
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: part 3, novel propellane derivatives with pentacyclic skeletons.
Bioorganic & medicinal chemistry letters 2012;22(24):7697-701.
2012: Hideaki Fujii; Hiroaki Gouda; Shigeto Hirayama; Shuichi Hirono; Satomi Imaide; Toru Nemoto; Hiroshi Nagase
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.
Bioorganic & medicinal chemistry letters 2012;22(24):7711-4.
2012: Yoshihiro Ida; Ayaka Matsubara; Hideaki Fujii; Shigeto Hirayama; Toru Nemoto; Manabu Saito; Hiroshi Nagase
Synthesis of quinolinomorphinan derivatives as highly selective δ opioid receptor ligands.
Bioorganic & medicinal chemistry 2012;20(19):5810-31.
2012: Yoshinori Miyata; Hideaki Fujii; Seiki Kobayashi; Tsutomu Takeuchi; Yuka Uenohara; Hiroshi Nagase
Investigation of 7-benzylidenenaltrexone derivatives as resistance reverser for chloroquine-resistant Plasmodium chabaudi.
Bioorganic & medicinal chemistry letters 2012;22(16):5174-6.
2012: Hiroshi Nagase; Toru Nemoto; Shigeto Hirayama; Satomi Imaide; Hideaki Fujii
Essential structure of opioid κ receptor agonist nalfurafine for binding to the κ receptor 2: synthesis of decahydro(iminoethano)phenanthrene derivatives and their pharmacologies.
Bioorganic & medicinal chemistry letters 2012;22(15):5071-4.
2012: Hiroshi Nagase; Ryo Nakajima; Toru Nemoto; Junko Akiyama; Hiroaki Gouda; Shigeto Hirayama; Shuichi Hirono; Hideaki Fujii
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology. Part 2: Propellane derivatives with an amide side chain.
Bioorganic & medicinal chemistry letters 2012;22(8):2775-9.
2012: Yoshikazu Watanabe; Toru Nemoto; Hideaki Fujii; Shigeto Hirayama; Shota Kitazawa; Hiroshi Nagase
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
Bioorganic & medicinal chemistry letters 2012;22(8):2689-92.
2012: Yoshihiro Ida; Masayuki Imai; Toshiyuki Kanemasa; Akira Kato; Hideaki Fujii; Shigeto Hirayama; Takashi Nakamura; Toru Nemoto; Yumiko Osa; Hiroshi Nagase
Synthesis of quinolinomorphinan-4-ol derivatives as δ opioid receptor agonists.
Bioorganic & medicinal chemistry 2012;20(2):949-61.
2011: Hiroshi Nagase; Mayumi Nakajima; Kaoru Nakao; Toru Nemoto; Naohisa Wada; Akio Watanabe; Shigeto Hirayama; Koji Koyano; Hidenori Mochizuki; Hideaki Fujii
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. Part 2: Synthesis of novel triplet drugs with the epoxymethano structure (capped homotriplet).
Bioorganic & medicinal chemistry letters 2011;21(20):6198-202.
2011: Yoshinori Miyata; Hideaki Fujii; Seiki Kobayashi; Yumiko Osa; Tsutomu Takeuchi; Hiroshi Nagase
Opioid δ₁ receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi.
Bioorganic & medicinal chemistry letters 2011;21(16):4710-2.
2011: Naoshi Yamamoto; Ryo Nakajima; Toru Nemoto; Hideaki Fujii; Ko Hasebe; Naoki Izumimoto; Hidenori Mochizuki; Shinobu Momen; Hiroshi Nagase
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacology: part 1.
Bioorganic & medicinal chemistry letters 2011;21(13):4104-7.
2011: Hiroshi Nagase; Mayumi Nakajima; Toru Nemoto; Akio Watanabe; Ko Hasebe; Hidenori Mochizuki; Hideaki Fujii
Synthesis of novel triplet drugs with 1,3,5-trioxazatriquinane skeletons and their pharmacologies. 1: Synthesis of triplet drugs with morphinan skeletons.
Bioorganic & medicinal chemistry letters 2011;21(13):4023-6.
2011: Naoshi Yamamoto; Hideaki Fujii; Satomi Imaide; Shigeto Hirayama; Toru Nemoto; Junji Inokoshi; Hiroshi Tomoda; Hiroshi Nagase
Synthesis of (-)-homogalanthamine from naltrexone.
The Journal of organic chemistry 2011;76(7):2257-60.
2011: Toru Nemoto; Naoshi Yamamoto; Akio Watanabe; Hideaki Fujii; Ko Hasebe; Mayumi Nakajima; Hidenori Mochizuki; Hiroshi Nagase
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
Bioorganic & medicinal chemistry 2011;19(3):1205-21.
2011: Hiroshi Nagase; Hideaki Fujii
Opioids in preclinical and clinical trials.
Topics in current chemistry 2011;299():29-62.
2011: Hiroshi Nagase
Chemistry of opioids. Preface.
Topics in current chemistry 2011;299():ix-xi.
2011: Hiroshi Nagase; Hideaki Fujii
Synthesis of novel basic skeletons derived from naltrexone.
Topics in current chemistry 2011;299():187-237.
2010: Hiroshi Nagase; Toru Nemoto; Ayaka Matsubara; Manabu Saito; Naoshi Yamamoto; Yumiko Osa; Shigeto Hirayama; Mayumi Nakajima; Kaoru Nakao; Hidenori Mochizuki; Hideaki Fujii
Design and synthesis of KNT-127, a δ-opioid receptor agonist effective by systemic administration.
Bioorganic & medicinal chemistry letters 2010;20(21):6302-5.
2010: Hideaki Fujii; Yoshihiro Ida; Shinichi Hanamura; Yumiko Osa; Toru Nemoto; Mayumi Nakajima; Ko Hasebe; Kaoru Nakao; Hidenori Mochizuki; Hiroshi Nagase
Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists.
Bioorganic & medicinal chemistry letters 2010;20(17):5035-8.
2010: Hiroshi Nagase; Satomi Imaide; Miyuki Tomatsu; Toru Nemoto; Mayumi Nakajima; Kaoru Nakao; Hidenori Mochizuki; Hideaki Fujii
Investigation of Beckett-Casy model 2: synthesis of novel 15-16 nornaltrexone derivatives and their pharmacology.
Bioorganic & medicinal chemistry letters 2010;20(12):3726-9.
2010: Noriyuki Yamaotsu; Hideaki Fujii; Hiroshi Nagase; Shuichi Hirono
Identification of the three-dimensional pharmacophore of kappa-opioid receptor agonists.
Bioorganic & medicinal chemistry 2010;18(12):4446-52.
2010: Hiroshi Nagase; Satomi Imaide; Miyuki Tomatsu; Shigeto Hirayama; Toru Nemoto; Noriko Sato; Mayumi Nakajima; Kaoru Nakao; Hidenori Mochizuki; Hiroaki Gouda; Shuichi Hirono; Hideaki Fujii
Investigation of Beckett-Casy model 3: synthesis of novel naltrexone derivatives with contracted and expanded D-rings and their pharmacology.
Bioorganic & medicinal chemistry letters 2010;20(12):3801-4.
2010: Hideaki Fujii; Satomi Imaide; Akio Watanabe; Kenji Yoza; Mayumi Nakajima; Kaoru Nakao; Hidenori Mochizuki; Noriko Sato; Toru Nemoto; Hiroshi Nagase
A double decarboxylation reaction of an oxazolidinone and carboxylic Acid: its application to the synthesis of a new opioid lead compound.
The Journal of organic chemistry 2010;75(3):995-8.
2010: Satomi Imaide; Hideaki Fujii; Akio Watanabe; Toru Nemoto; Mayumi Nakajima; Kaoru Nakao; Hidenori Mochizuki; Hiroshi Nagase
Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
Bioorganic & medicinal chemistry letters 2010;20(3):1055-8.
2010: Hiroshi Nagase; Akio Watanabe; Toru Nemoto; Noriyuki Yamaotsu; Kohei Hayashida; Mayumi Nakajima; Ko Hasebe; Kaoru Nakao; Hidenori Mochizuki; Shuichi Hirono; Hideaki Fujii
Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology.
Bioorganic & medicinal chemistry letters 2010;20(1):121-4.
2009: Akio Watanabe; Hideaki Fujii; Mayumi Nakajima; Ko Hasebe; Hidenori Mochizuki; Hiroshi Nagase
Synthesis of a new opioid ligand having the oxabicyclo[3.2.1]octane skeleton using a new rearrangement reaction.
Bioorganic & medicinal chemistry letters 2009;19(9):2416-9.
2009: Hiroshi Nagase; Akio Watanabe; Masaya Harada; Mayumi Nakajima; Ko Hasebe; Hidenori Mochizuki; Kenji Yoza; Hideaki Fujii
Novel synthesis of a 1,3,5-trioxazatriquinane skeleton using a nitrogen clamp.
Organic letters 2009;11(3):539-42.
2008: Hiroshi Nagase; Naoshi Yamamoto; Toru Nemoto; Kenji Yoza; Kenshu Kamiya; Shuichi Hirono; Shinobu Momen; Naoki Izumimoto; Ko Hasebe; Hidenori Mochizuki; Hideaki Fujii
Synthesis of a stable iminium salt and propellane derivatives.
The Journal of organic chemistry 2008;73(20):8093-6.
2008: Koji Kawai; Jun Hayakawa; Toru Miyamoto; Yoshifumi Imamura; Shinichi Yamane; Hisanori Wakita; Hideaki Fujii; Kuniaki Kawamura; H Matsuura; Naoki Izumimoto; Ryosuke Kobayashi; Takashi Endo; Hiroshi Nagase
Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.
Bioorganic & medicinal chemistry 2008;16(20):9188-201.
2008: Satoshi Sakami; Koji Kawai; Masayuki Maeda; Takumi Aoki; Hideaki Fujii; Hiroshi Ohno; Tsuyoshi Ito; Akiyoshi Saitoh; Kaoru Nakao; Naoki Izumimoto; H Matsuura; Takashi Endo; Shinya Ueno; Kazuto Natsume; Hiroshi Nagase
Design and synthesis of a metabolically stable and potent antitussive agent, a novel delta opioid receptor antagonist, TRK-851.
Bioorganic & medicinal chemistry 2008;16(17):7956-67.
2008: Satoshi Sakami; Masayuki Maeda; Koji Kawai; Takumi Aoki; Kuniaki Kawamura; Hideaki Fujii; Ko Hasebe; Mayumi Nakajima; Takashi Endo; Shinya Ueno; Tsuyoshi Ito; Junzo Kamei; Hiroshi Nagase
Structure-antitussive activity relationships of naltrindole derivatives. Identification of novel and potent antitussive agents.
Journal of medicinal chemistry 2008;51(15):4404-11.
2006: Hideaki Fujii; Hiroshi Nagase
Rational drug design of selective epsilon opioid receptor agonist TAN-821 and antagonist TAN-1014.
Current medicinal chemistry 2006;13(10):1109-18.
2004: Yoshio Wakasa; Atsushi Fujiwara; Hideo Umeuchi; Takashi Endoh; Kiyoshi Okano; Toshiaki Tanaka; Hiroshi Nagase
Inhibitory effects of TRK-820 on systemic skin scratching induced by morphine in rhesus monkeys.
Life sciences 2004;75(24):2947-57.
2004: Ko Hasebe; Koji Kawai; Tomohiko Suzuki; Kuniaki Kawamura; Toshiaki Tanaka; Minoru Narita; Hiroshi Nagase; Tsutomu Suzuki
Possible pharmacotherapy of the opioid kappa receptor agonist for drug dependence.
Annals of the New York Academy of Sciences 2004;1025():404-13.
2004: Hideaki Fujii; Minoru Narita; Hirokazu Mizoguchi; Junichi Hirokawa; Koji Kawai; Toshiaki Tanaka; Leon F Tseng; Hiroshi Nagase
Rational drug design and synthesis of a selective opioid receptor antagonist on the basis of the accessory site concept.
Bioorganic & medicinal chemistry letters 2004;14(16):4241-3.
2004: Hideaki Fujii; Minoru Narita; Hirokazu Mizoguchi; Miho Murachi; Toshiaki Tanaka; Koji Kawai; Leon F Tseng; Hiroshi Nagase
Drug design and synthesis of epsilon opioid receptor agonist: 17-(cyclopropylmethyl)-4,5alpha-epoxy-3,6beta-dihydroxy-6,14-endoethenomorphinan-7alpha-(N-methyl-N-phenethyl)carboxamide (TAN-821) inducing antinociception mediated by putative epsilon opioid receptor.
Bioorganic & medicinal chemistry 2004;12(15):4133-45.
2004: Hideaki Fujii; Noriyuki Hirano; Hiromi Uchiro; Kuniaki Kawamura; Hiroshi Nagase
The first example of the stereoselective synthesis of 7 beta-carbamoyl-4,5alpha-epoxymorphinan via a novel and reactive gamma-lactone.
Chemical & pharmaceutical bulletin 2004;52(6):747-50.
2004: Kuniaki Kawamura; Hiromasa Horikiri; Jun Hayakawa; Chie Seki; Ken-ichi Yoshizawa; Hideo Umeuchi; Hiroshi Nagase
Syntheses of potential metabolites of a potent kappa-opioid receptor agonist, TRK-820.
Chemical & pharmaceutical bulletin 2004;52(6):670-4.
2004: Hiromasa Horikiri; Noriyuki Hirano; Yoichiro Tanaka; Junji Oishi; Hitoshi Hatakeyama; Kuniaki Kawamura; Hiroshi Nagase
Syntheses of 10-oxo, 10 alpha-hydroxy, and 10 beta-hydroxy derivatives of a potent kappa-opioid receptor agonist, TRK-820.
Chemical & pharmaceutical bulletin 2004;52(6):664-9.
2004: Tomohiko Suzuki; Naoki Izumimoto; Yuko Takezawa; Morihiro Fujimura; Yuko Togashi; Hiroshi Nagase; Toshiaki Tanaka; Takashi Endoh
Effect of repeated administration of TRK-820, a kappa-opioid receptor agonist, on tolerance to its antinociceptive and sedative actions.
Brain research 2004;995(2):167-75.
2003: Hideo Umeuchi; Yuko Togashi; Toshiyuki Honda; Kaoru Nakao; Kiyoshi Okano; Toshiaki Tanaka; Hiroshi Nagase
Involvement of central mu-opioid system in the scratching behavior in mice, and the suppression of it by the activation of kappa-opioid system.
European journal of pharmacology 2003;477(1):29-35.
2002: Yuko Togashi; Hideo Umeuchi; Kiyoshi Okano; Naoki Ando; Yoshitaka Yoshizawa; Toshiyuki Honda; Kuniaki Kawamura; Takashi Endoh; Jun Utsumi; Junzo Kamei; Toshiaki Tanaka; Hiroshi Nagase
Antipruritic activity of the kappa-opioid receptor agonist, TRK-820.
European journal of pharmacology 2002;435(2-3):259-64.
2001: Hiroshi Nagase; Y Yajima; Hideaki Fujii; K Kawamura; M Narita; J Kamei; Tomohiko Suzuki
The pharmacological profile of delta opioid receptor ligands, (+) and (-) TAN-67 on pain modulation.
Life sciences 2001;68(19-20):2227-31.
2001: Takashi Endoh; A Tajima; Naoki Izumimoto; Tomohiko Suzuki; A Saitoh; T Suzuki; M Narita; J Kamei; L F Tseng; H Mizoguchi; Hiroshi Nagase
TRK-820, a selective kappa-opioid agonist, produces potent antinociception in cynomolgus monkeys.
Japanese journal of pharmacology 2001;85(3):282-90.
2001: Hideaki Fujii; Koji Kawai; K Kawamura; A Mizusuna; Y Onoda; M Murachi; Toshiaki Tanaka; Takashi Endoh; Hiroshi Nagase
Synthesis of optically active TAN-67, a highly selective delta opioid receptor agonist, and investigation of its pharmacological properties.
Drug design and discovery 2001;17(4):325-30.
2000: Takashi Endoh; A Tajima; Tomohiko Suzuki; J Kamei; M Narita; L Tseng; Hiroshi Nagase
Characterization of the antinociceptive effects of TRK-820 in the rat.
European journal of pharmacology 2000;387(2):133-40.
1999: Takashi Endoh; H Matsuura; A Tajima; Naoki Izumimoto; C Tajima; Tomohiko Suzuki; A Saitoh; T Suzuki; M Narita; L Tseng; Hiroshi Nagase
Potent antinociceptive effects of TRK-820, a novel kappa-opioid receptor agonist.
Life sciences 1999;65(16):1685-94.
1998: Hiroshi Nagase; K Kawai; J Hayakawa; H Wakita; A Mizusuna; H Matsuura; C Tajima; Y Takezawa; Takashi Endoh
Rational drug design and synthesis of a highly selective nonpeptide delta-opioid agonist, (4aS*,12aR*)-4a-(3-hydroxyphenyl)-2-methyl- 1,2,3,4,4a,5,12,12a-octahydropyrido[3,4-b]acridine (TAN-67).
Chemical & pharmaceutical bulletin 1998;46(11):1695-702.
1998: Hiroshi Nagase; J Hayakawa; K Kawamura; K Kawai; Y Takezawa; H Matsuura; C Tajima; T Endo
Discovery of a structurally novel opioid kappa-agonist derived from 4,5-epoxymorphinan.
Chemical & pharmaceutical bulletin 1998;46(2):366-9.
1992: Takashi Endoh; H Matsuura; C Tanaka; Hiroshi Nagase
Nor-binaltorphimine: a potent and selective kappa-opioid receptor antagonist with long-lasting activity in vivo.
Archives internationales de pharmacodynamie et de thérapie 1992;316():30-42.