Pharmacologic effects of naldemedine, a peripherally acting μ‐opioid receptor antagonist, in in vitro and in vivo models of opioid‐induced constipation

Toshiyuki Kanemasa; Katsumi Koike; Tohko Arai; Hiroko Ono; Narumi Horita; Hiroki Chiba; Atsushi Nakamura; Yasuhide Morioka; Tsuyoshi Kihara; Minoru Hasegawa

doi:10.1111/nmo.13563

Pharmacologic effects of naldemedine, a peripherally acting μ‐opioid receptor antagonist, in in vitro and in vivo models of opioid‐induced constipation

Neurogastroenterology & Motility ◽

10.1111/nmo.13563 ◽

2019 ◽

Vol 31 (5) ◽

pp. e13563 ◽

Cited By ~ 8

Author(s):

Toshiyuki Kanemasa ◽

Katsumi Koike ◽

Tohko Arai ◽

Hiroko Ono ◽

Narumi Horita ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

In Vivo Models ◽

Opioid Receptor Antagonist ◽

Μ Opioid Receptor

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An In Vitro and In Vivo study of BNAP: A Novel Peripherally Selective μ‐opioid Receptor Antagonist

The FASEB Journal ◽

10.1096/fasebj.29.1_supplement.929.2 ◽

2015 ◽

Vol 29 (S1) ◽

Author(s):

D Williams ◽

Y Yuan ◽

D Stevens ◽

Y Zhang ◽

W Dewey ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

In Vivo Study ◽

Opioid Receptor Antagonist ◽

Μ Opioid Receptor

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Analogues of (3R)-7-Hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic). Synthesis and in Vitro and in Vivo Opioid Receptor Antagonist Activity

Journal of Medicinal Chemistry ◽

10.1021/jm1004978 ◽

2010 ◽

Vol 53 (14) ◽

pp. 5290-5301 ◽

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Author(s):

Scott P. Runyon ◽

Lawrence E. Brieaddy ◽

S. Wayne Mascarella ◽

James B. Thomas ◽

Hernán A. Navarro ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Antagonist Activity ◽

Opioid Receptor Antagonist

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In vivo effects of μ-opioid receptor agonist/δ-opioid receptor antagonist peptidomimetics following acute and repeated administration

British Journal of Pharmacology ◽

10.1111/bph.14148 ◽

2018 ◽

Vol 175 (11) ◽

pp. 2013-2027 ◽

Cited By ~ 20

Author(s):

Jessica P Anand ◽

Kelsey E Kochan ◽

Anthony F Nastase ◽

Deanna Montgomery ◽

Nicholas W Griggs ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Receptor Agonist ◽

Repeated Administration ◽

Opioid Receptor Antagonist ◽

Opioid Receptor Agonist ◽

Μ Opioid Receptor ◽

Δ Opioid Receptor ◽

In Vivo Effects

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Effects of Naldemedine, a Peripherally Acting μ-Opioid Receptor Antagonist, on Inhibition of Large Intestinal Transit Induced by Morphine in Rodent Models

Gastroenterology ◽

10.1016/s0016-5085(17)31879-6 ◽

2017 ◽

Vol 152 (5) ◽

pp. S508

Author(s):

Toshiyuki Kanemasa ◽

Hiroko Ono ◽

Atsushi Nakamura ◽

Yasuhidse Morioka ◽

Minoru Hasegawa

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Intestinal Transit ◽

Rodent Models ◽

Opioid Receptor Antagonist ◽

Μ Opioid Receptor

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Asymmetric Synthesis and in Vitro and in Vivo Activity of Tetrahydroquinolines Featuring a Diverse Set of Polar Substitutions at the 6 Position as Mixed-Efficacy μ Opioid Receptor/δ Opioid Receptor Ligands

ACS Chemical Neuroscience ◽

10.1021/acschemneuro.5b00100 ◽

2015 ◽

Vol 6 (8) ◽

pp. 1428-1435 ◽

Cited By ~ 22

Author(s):

Aaron M. Bender ◽

Nicholas W. Griggs ◽

Jessica P. Anand ◽

John R. Traynor ◽

Emily M. Jutkiewicz ◽

...

Keyword(s):

Asymmetric Synthesis ◽

Opioid Receptor ◽

Receptor Ligands ◽

Opioid Receptor Ligands ◽

Μ Opioid Receptor ◽

Mixed Efficacy ◽

Δ Opioid Receptor

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Synthesis and Structure–Activity Relationships of 5′-Aryl-14-alkoxypyridomorphinans: Identification of a μ Opioid Receptor Agonist/δ Opioid Receptor Antagonist Ligand with Systemic Antinociceptive Activity and Diminished Opioid Side Effects

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.0c00503 ◽

2020 ◽

Vol 63 (14) ◽

pp. 7663-7694 ◽

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Author(s):

Rakesh H. Vekariya ◽

Wei Lei ◽

Abhisek Ray ◽

Surendra K. Saini ◽

Sixue Zhang ◽

...

Keyword(s):

Side Effects ◽

Receptor Antagonist ◽

Opioid Receptor ◽

Receptor Agonist ◽

Antinociceptive Activity ◽

Opioid Receptor Antagonist ◽

Structure Activity ◽

Opioid Receptor Agonist ◽

Μ Opioid Receptor ◽

Δ Opioid Receptor

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Pharmacological Profile of Naldemedine, a Peripheral Acting μ-Opioid Receptor Antagonist: Comparison With Naloxone and Naloxegol

The American Journal of Gastroenterology ◽

10.14309/00000434-201810001-00173 ◽

2018 ◽

Vol 113 (Supplement) ◽

pp. S96-S97

Author(s):

Toshiyuki Kanemasa ◽

Katsumi Koike ◽

Kenji Takase ◽

Tohko Arai ◽

Atsushi Nakamura ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Pharmacological Profile ◽

Opioid Receptor Antagonist ◽

Μ Opioid Receptor

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Effects of the δ-opioid receptor antagonist naltrindole on opioid induced in vivo release of corticosterone

European Journal of Pharmacology ◽

10.1016/0014-2999(90)93878-t ◽

1990 ◽

Vol 183 (6) ◽

pp. 2321-2322

Author(s):

I. Kitchen ◽

A. Kennedy

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Opioid Receptor Antagonist ◽

In Vivo Release ◽

Δ Opioid Receptor

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Reversal and Prevention of the Respiratory-Depressant Effects of Heroin by the Novel μ-Opioid Receptor Antagonist Methocinnamox in Rhesus Monkeys

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.118.253286 ◽

2018 ◽

Vol 368 (2) ◽

pp. 229-236 ◽

Cited By ~ 10

Author(s):

Lisa R. Gerak ◽

David R. Maguire ◽

James H. Woods ◽

Stephen M. Husbands ◽

Alex Disney ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Rhesus Monkeys ◽

The Novel ◽

Opioid Receptor Antagonist ◽

Μ Opioid Receptor ◽

Respiratory Depressant

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Pharmacological Profile of Naldemedine, a Peripherally Acting μ-Opioid Receptor Antagonist: Comparison with Naloxone and Naloxegol

Journal of Pharmacology and Experimental Therapeutics ◽

10.1124/jpet.119.264515 ◽

2020 ◽

Vol 373 (3) ◽

pp. 438-444 ◽

Cited By ~ 2

Author(s):

Toshiyuki Kanemasa ◽

Katsumi Koike ◽

Kenji Takase ◽

Tohko Arai ◽

Atsushi Nakamura ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Pharmacological Profile ◽

Opioid Receptor Antagonist ◽

Μ Opioid Receptor

Download Full-text