Literature DB >> 22444677

Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.

Masahide Odan1, Natsuki Ishizuka, Yoshiharu Hiramatsu, Masanao Inagaki, Hiroshi Hashizume, Yasuhiko Fujii, Susumu Mitsumori, Yasuhide Morioka, Masahiko Soga, Masashi Deguchi, Kiyoshi Yasui, Akinori Arimura.   

Abstract

The discovery of novel CB2 ligands based on the 3-carbamoyl-2-pyridone derivatives by adjusting the size of side chain at 1-, 5- and 6-position is reported. The structure-activity relationship around this template lead to the identification of S-777469 as a selective CB2 receptor agonist, which exhibited the significant inhibition of scratching induced by Compound 48/80 at 1.0 mg/kg po and 10 mg/kg po (55% and 61%, respectively).
Copyright © 2012 Elsevier Ltd. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2012        PMID: 22444677     DOI: 10.1016/j.bmcl.2012.02.072

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  11 in total

1.  A synergistic interaction of 17-β-estradiol with specific cannabinoid receptor type 2 antagonist/inverse agonist on proliferation activity in primary human osteoblasts.

Authors:  Marko Hojnik; Luka Dobovišek; Željko Knez; Polonca Ferk
Journal:  Biomed Rep       Date:  2015-05-26

Review 2.  New approaches and challenges to targeting the endocannabinoid system.

Authors:  Vincenzo Di Marzo
Journal:  Nat Rev Drug Discov       Date:  2018-08-17       Impact factor: 84.694

3.  Quantification of small molecule drugs in biological tissue sections by imaging mass spectrometry using surrogate tissue-based calibration standards.

Authors:  Nozomi Takai; Yukari Tanaka; Hideo Saji
Journal:  Mass Spectrom (Tokyo)       Date:  2014-02-01

Review 4.  Targeting the endocannabinoid system with cannabinoid receptor agonists: pharmacological strategies and therapeutic possibilities.

Authors:  Roger G Pertwee
Journal:  Philos Trans R Soc Lond B Biol Sci       Date:  2012-12-05       Impact factor: 6.237

5.  The Structure-Function Relationships of Classical Cannabinoids: CB1/CB2 Modulation.

Authors:  Eric W Bow; John M Rimoldi
Journal:  Perspect Medicin Chem       Date:  2016-06-28

6.  Cannabinoid Receptor 2 Signalling Bias Elicited by 2,4,6-Trisubstituted 1,3,5-Triazines.

Authors:  Caitlin R M Oyagawa; Sara M de la Harpe; Yurii Saroz; Michelle Glass; Andrea J Vernall; Natasha Lillia Grimsey
Journal:  Front Pharmacol       Date:  2018-11-20       Impact factor: 5.810

7.  Erratum: Cannabinoid Receptor 2 Signalling Bias Elicited by 2,4,6-Trisubstituted 1,3,5-Triazines.

Authors: 
Journal:  Front Pharmacol       Date:  2019-04-05       Impact factor: 5.810

8.  CB2R Deficiency Exacerbates Imiquimod-Induced Psoriasiform Dermatitis and Itch Through the Neuro-Immune Pathway.

Authors:  Li Li; Xin Liu; Wenqiang Ge; Chao Chen; Yuqiong Huang; Zilin Jin; Muouyang Zhan; Xiaoru Duan; Xinxin Liu; Yi Kong; Jian Jiang; Xuemei Li; Xin Zeng; Fei Li; Shibin Xu; Man Li; Hongxiang Chen
Journal:  Front Pharmacol       Date:  2022-01-31       Impact factor: 5.810

Review 9.  Impact of Cannabinoid Compounds on Skin Cancer.

Authors:  Robert Ramer; Franziska Wendt; Felix Wittig; Mirijam Schäfer; Lars Boeckmann; Steffen Emmert; Burkhard Hinz
Journal:  Cancers (Basel)       Date:  2022-03-31       Impact factor: 6.639

Review 10.  Role of the Endocannabinoid System in the Adipose Tissue with Focus on Energy Metabolism.

Authors:  Volatiana Rakotoarivelo; Jyoti Sihag; Nicolas Flamand
Journal:  Cells       Date:  2021-05-21       Impact factor: 6.600

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.