G-Protein biased opioid agonists: 3-hydroxy-N-phenethyl-5-phenylmorphans with three-carbon chain substituents at C9-Reference-Cited by-同舟云学术

G-Protein biased opioid agonists: 3-hydroxy-N-phenethyl-5-phenylmorphans with three-carbon chain substituents at C9

Published:2020 Issue:8 Volume:11 Page:896-904
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Gutman Eugene S.¹²³⁴⁵,Bow Eric¹²³⁴⁵,Li Fuying¹²³⁴⁵,Sulima Agnieszka¹²³⁴⁵,Kaska Sophia⁶⁷⁸⁹¹⁰,Crowley Rachel¹¹¹²¹³¹⁴¹⁰,Prisinzano Thomas E.⁶⁷⁸⁹¹⁰^ORCID,Lee Yong-Sok¹⁵¹⁶¹⁷¹⁸¹⁰,Hassan Sergio A.¹⁵¹⁶¹⁷¹⁸¹⁰^ORCID,Imler Gregory H.¹⁹²⁰²¹¹⁰,Deschamps Jeffrey R.¹⁹²⁰²¹¹⁰,Jacobson Arthur E.¹²³⁴⁵^ORCID,Rice Kenner C.¹²³⁴⁵

Affiliation:

1. Drug Design and Synthesis Section

2. Molecular Targets and Medications Discovery Branch

3. Intramural Research Program

4. National Institute on Drug Abuse

5. National Institute on Alcohol Abuse and Alcoholism

6. Department of Pharmaceutical Sciences

7. College of Pharmacy

8. University of Kentucky

9. Lexington

10. USA

11. Department of Medicinal Chemistry

12. School of Pharmacy

13. University of Kansas

14. Lawrence

15. Center for Molecular Modeling, Center for Information Technology

16. National Institutes of Health

17. Department of Health and Human Services

18. Bethesda

19. Center for Biomolecular Science and Engineering

20. Naval Research Laboratory

21. Washington DC

Abstract

Three C9 substituted N-phenethyl-5-phenylmorphans were found to be extremely G-protein biased potent mu opioid receptor partial agonists that did not recruit beta-arrestin at all in both the PathHunter assay and in the Tango assay.

Funder

National Institute on Alcohol Abuse and Alcoholism

National Institute on Drug Abuse

Center for Information Technology

National Institute of General Medical Sciences

National Institutes of Health

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/2020/MD/D0MD00104J