ArticleEuropean journal of medicinal chemistry2014
Development of second generation EP2 antagonists with high selectivity.
Article in European journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 36 citations in OpenAlex.
- Development of highly potent EP2 antagonists as novel anti-inflammatory neuroprotectants.Bioorganic & medicinal chemistry · 2026Article
- Preclinical development of an EP2 antagonist for post-seizure cognitive deficits.Neuropharmacology · 2023Article
- Second-Generation Prostaglandin Receptor EP2 Antagonist, TG8-260, with High Potency, Selectivity, Oral Bioavailability, and Anti-Inflammatory Properties.ACS pharmacology & translational science · 2022Article
- EP2 Antagonists (2011-2021): A Decade's Journey from Discovery to Therapeutics.Journal of medicinal chemistry · 2021Review
- A Novel Second-Generation EP2 Receptor Antagonist Reduces Neuroinflammation and Gliosis After Status Epilepticus in Rats.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2021Article
- PGE2 receptors in detrusor muscle: Drugging the undruggable for urgency.Biochemical pharmacology · 2021Review
- Targeting prostaglandin receptor EP2 for adjunctive treatment of status epilepticus.Pharmacology & therapeutics · 2020Review
- Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist for Use in Central Nervous System Disease Models.Journal of medicinal chemistry · 2020Article
- G protein-coupled receptors in acquired epilepsy: Druggability and translatability.Progress in neurobiology · 2019Review
- Small-molecule inhibition of prostaglandin E receptor 2 impairs cyclooxygenase-associated malignant glioma growth.British journal of pharmacology · 2019Article
- Suppressing pro-inflammatory prostaglandin signaling attenuates excitotoxicity-associated neuronal inflammation and injury.Neuropharmacology · 2019Article
- Peripherally Restricted, Highly Potent, Selective, Aqueous-Soluble EP2 Antagonist with Anti-Inflammatory Properties.Molecular pharmaceutics · 2018Article
- Cyclooxygenase-2 contributes to oxidopamine-mediated neuronal inflammation and injury via the prostaglandin E2 receptor EP2 subtype.Scientific reports · 2017Article
- Prostaglandin dehydrogenase is a target for successful induction of cervical ripening.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- Neuroinflammatory targets and treatments for epilepsy validated in experimental models.Epilepsia · 2017Review
- Inhibition of the prostaglandin E2 receptor EP2 prevents status epilepticus-induced deficits in the novel object recognition task in rats.Neuropharmacology · 2016Article
- Mapping PTGERs to the Ovulatory Follicle: Regional Responses to the Ovulatory PGE2 Signal.Biology of reproduction · 2016Review
- Anti-Inflammatory Small Molecules To Treat Seizures and Epilepsy: From Bench to Bedside.Trends in pharmacological sciences · 2016Review
- Defining the therapeutic time window for suppressing the inflammatory prostaglandin E2 signaling after status epilepticus.Expert review of neurotherapeutics · 2016Review
- Evaluation of WO 2012/177618 A1 and US-2014/0179750 A1: novel small molecule antagonists of prostaglandin-E2 receptor EP2.Expert opinion on therapeutic patents · 2015Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
EP2 receptor has emerged as an important biological target for therapeutic intervention. In particular, it has been shown to exacerbate disease progression of a variety of CNS and peripheral diseases. Deletion of the EP2 receptor in mouse models recapitulates several features of the COX-2 inhibition, thus presenting a new avenue for anti-inflammatory therapy which could bypass some of the adverse side effects observed by the COX-2 inhibition therapy. We have recently reported a cinnamic amide class of EP2 antagonists with high potency, but these compounds exhibited a moderate selectivity against prostanoid receptor DP1. Moreover they possess acrylamide moiety in the structure, which may result in liver toxicity over longer period of use in a chronic disease model. Thus, we now developed a second generation compounds that devoid of the acrylamide functionality and possess high potency and improved (>1000-fold) selectivity to EP2 over other prostanoid receptors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.