Design, synthesis, and biological evaluation of C6-difluoromethylenated epoxymorphinan Mu opioid receptor antagonists-Reference-Cited by-同舟云学术

Design, synthesis, and biological evaluation of C6-difluoromethylenated epoxymorphinan Mu opioid receptor antagonists

Published:2022 Issue: Volume: Page:
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Kassick Andrew J.¹²,Treat Anny³,Tomycz Nestor²,Feasel Michael G.⁴,Kolber Benedict J.³,Averick Saadyah¹²^ORCID

Affiliation:

1. Neuroscience Disruptive Research Lab, Allegheny Health Network Research Institute, Allegheny General Hospital, Pittsburgh, PA 15212, USA

2. Neuroscience Institute, Allegheny Health Network, Allegheny General Hospital, Pittsburgh, PA 15212, USA

3. Department of Neuroscience and Center for Advanced Pain Studies, University of Texas at Dallas, Richardson, TX 75080, USA

4. Research and Technology Division, DEVCOM Chemical Biological Center, Aberdeen Proving Ground, MD 21010-5424, USA

Abstract

C6-difluoromethylenated epoxymorphinans were found to maintain in vitro potency against fentanyl and displayed effective in vivo blockade of fentanyl-induced anti-nociception in mice relative to the clinical opioid reversal agent naloxone.

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/MD/D1MD00285F

Reference35 articles.

1. A Tribute to Dr. Paul A. J. Janssen: Entrepreneur Extraordinaire, Innovative Scientist, and Significant Contributor to Anesthesiology

2. The Fentanyl Story

3. Pharmacokinetic-Pharmacodynamic Relationships for Opioids in Balanced Anaesthesia

4. Prescription opioids, abuse and public health in Canada: is fentanyl the new centre of the opioid crisis?

5. An epidemic of the use, misuse and overdose of opioids and deaths due to overdose, in the United States and Canada

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