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

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 ◽

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 ◽

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 ◽

Cited By ~ 2

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 ◽

Structure Activity ◽

Opioid Receptor Agonist ◽

Μ Opioid Receptor ◽

Δ Opioid Receptor

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 ◽

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 ◽

Μ Opioid Receptor ◽

Respiratory Depressant

Discovery of Axelopran (TD-1211): A Peripherally Restricted μ-Opioid Receptor Antagonist

ACS Medicinal Chemistry Letters ◽

10.1021/acsmedchemlett.9b00406 ◽

2019 ◽

Vol 10 (12) ◽

pp. 1641-1647

Author(s):

Daniel D. Long ◽

Scott R. Armstrong ◽

David T. Beattie ◽

Christina B. Campbell ◽

Timothy J. Church ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Intracerebroventricular administration of CYX-6, a potent μ-opioid receptor agonist, a δ- and κ-opioid receptor antagonist and a biased ligand at μ, δ & κ-opioid receptors, evokes antinociception with minimal constipation and respiratory depression in rats in contrast to morphine

European Journal of Pharmacology ◽

10.1016/j.ejphar.2020.172918 ◽

2020 ◽

Vol 871 ◽

pp. 172918 ◽

Cited By ~ 1

Author(s):

Mohammad Zafar Imam ◽

Andy Kuo ◽

Sussan Ghassabian ◽

Yunxin Cai ◽

Yajuan Qin ◽

...

Keyword(s):

Receptor Antagonist ◽

Respiratory Depression ◽

Opioid Receptor ◽

Opioid Receptors ◽

Receptor Agonist ◽

Intracerebroventricular Administration ◽

Opioid Receptor Agonist ◽

The μ-opioid receptor subtype is required for the anorectic effect of an opioid receptor antagonist

European Journal of Pharmacology ◽

10.1016/j.ejphar.2006.06.069 ◽

2006 ◽

Vol 545 (2-3) ◽

pp. 147-152 ◽

Cited By ~ 14

Author(s):

Jiaping Zhang ◽

Andrea Frassetto ◽

Ruey-Ruey C. Huang ◽

Julie Z. Lao ◽

Alexander Pasternak ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Receptor Subtype ◽

Anorectic Effect ◽

[d-1-Nal4]endomorphin-2 is a potent μ-opioid receptor antagonist in the aequorin luminescence-based calcium assay

Life Sciences ◽

10.1016/j.lfs.2006.03.016 ◽

2006 ◽

Vol 79 (11) ◽

pp. 1094-1099 ◽

Cited By ~ 2

Author(s):

Jakub Fichna ◽

Mariola Piestrzeniewicz ◽

Katarzyna Gach ◽

Jeroen Poels ◽

Emmanuel Burgeon ◽

...

Keyword(s):

Receptor Antagonist ◽

Opioid Receptor ◽

Inhibition of nociceptive responses of dorsal horn neurones in the cat spinal cord by ohmefentanyl, a preferring μ opioid receptor antagonist

Neuroscience Letters ◽

10.1016/0304-3940(90)90331-3 ◽

1990 ◽

Vol 112 (1) ◽

pp. 109-113

Author(s):

Z.-Q. Zhao ◽

H.-Q. Yang ◽

K.-M. Zhang

Keyword(s):

Spinal Cord ◽

Receptor Antagonist ◽

Dorsal Horn ◽

Opioid Receptor ◽

Nociceptive Responses ◽

Μ Opioid Receptor ◽

Dorsal Horn Neurones