Literature DB >> 7901416

N-substituted dibenzoxazepines as analgesic PGE2 antagonists.

E A Hallinan1, T J Hagen, R K Husa, S Tsymbalov, S N Rao, J P vanHoeck, M F Rafferty, A Stapelfeld, M A Savage, M Reichman.   

Abstract

8-Chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid, 2-acetylhydrazide (1, SC-19220) has been previously reported by us and others to be a PGE2 antagonist selective for the EP1 receptor subtype with antinociceptive activities. Analogs of SC-19220, in which the acetyl moiety has been replaced with pyridylpropionyl groups and their homologs, have been synthesized as illustrated by compounds 13 and 29. These and other members of this series have been shown to be efficacious analgesics and PGE2 antagonists of the EP1 subtype. This report discusses the structure activity relationships within this series.

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Year:  1993        PMID: 7901416     DOI: 10.1021/jm00074a010

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  13 in total

1.  A possible role of lipoxygenase in the activation of vanilloid receptors by anandamide in the guinea-pig bronchus.

Authors:  S J Craib; H C Ellington; R G Pertwee; R A Ross
Journal:  Br J Pharmacol       Date:  2001-09       Impact factor: 8.739

2.  Characterization of prostanoid receptors mediating actions of the isoprostanes, 8-iso-PGE(2) and 8-iso-PGF(2alpha), in some isolated smooth muscle preparations.

Authors:  W Sametz; S Hennerbichler; S Glaser; R Wintersteiger; H Juan
Journal:  Br J Pharmacol       Date:  2000-08       Impact factor: 8.739

3.  Differential peristaltic motor effects of prostanoid (DP, EP, IP, TP) and leukotriene receptor agonists in the guinea-pig isolated small intestine.

Authors:  Anaid Shahbazian; Akos Heinemann; Bernhard A Peskar; Peter Holzer
Journal:  Br J Pharmacol       Date:  2002-12       Impact factor: 8.739

4.  Inhibition of the Prostaglandin EP-1 Receptor in Periosteum Progenitor Cells Enhances Osteoblast Differentiation and Fracture Repair.

Authors:  Marina Feigenson; Jennifer H Jonason; Jie Shen; Alayna E Loiselle; Hani A Awad; Regis J O'Keefe
Journal:  Ann Biomed Eng       Date:  2019-04-12       Impact factor: 3.934

5.  Antihypertensive effects of selective prostaglandin E2 receptor subtype 1 targeting.

Authors:  Youfei Guan; Yahua Zhang; Jing Wu; Zhonghua Qi; Guangrui Yang; Dou Dou; Yuansheng Gao; Lihong Chen; Xiaoyan Zhang; Linda S Davis; Mingfeng Wei; Xuefeng Fan; Monica Carmosino; Chuanming Hao; John D Imig; Richard M Breyer; Matthew D Breyer
Journal:  J Clin Invest       Date:  2007-09       Impact factor: 14.808

Review 6.  Prostanoid receptor antagonists: development strategies and therapeutic applications.

Authors:  R L Jones; M A Giembycz; D F Woodward
Journal:  Br J Pharmacol       Date:  2009-07-15       Impact factor: 8.739

7.  Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere.

Authors:  Jason D Downey; Sam A Saleh; Thomas M Bridges; Ryan D Morrison; J Scott Daniels; Craig W Lindsley; Richard M Breyer
Journal:  Bioorg Med Chem Lett       Date:  2012-11-24       Impact factor: 2.823

8.  Involvement of EP1 and EP2 receptors in the regulation of the Na,K-ATPase by prostaglandins in MDCK cells.

Authors:  Keikantse Matlhagela; Mary Taub
Journal:  Prostaglandins Other Lipid Mediat       Date:  2006-01-27       Impact factor: 3.072

9.  Reactive astrocyte COX2-PGE2 production inhibits oligodendrocyte maturation in neonatal white matter injury.

Authors:  Lawrence R Shiow; Geraldine Favrais; Lucas Schirmer; Anne-Laure Schang; Sara Cipriani; Christian Andres; Jaclyn N Wright; Hiroko Nobuta; Bobbi Fleiss; Pierre Gressens; David H Rowitch
Journal:  Glia       Date:  2017-08-30       Impact factor: 7.452

10.  N-Cyclo-hexyl-5H,7H-13,15-dimethyl-9-nitro-5-oxophenanthrido[4,4a,5-bc][1,4]benzoxazepine-7-carboxamide.

Authors:  Jia-Lu Luo; Jin-Long Wu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-07-25
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