Neuroprotection Actions of EP1 Receptor Drugs

Prostaglandin E2 is the primary product of arachidonic metabolism and is synthesized via the prostaglandin and cycloxygenase pathways. The hormone-like chemical has been shown to affect the central nervous system and can modulate synaptic transmission and neurotransmitter release, the sleep/wake cycle, fever, pain and the immune system. PGE2 can bind to four known G protein-coupled receptors, named EP1, 2, 3 and 4 that are distinguished based on their specific signal-transduction pathways. Recently, researchers at JHU synthesized and tested novel compounds that antagonize the EP1 receptor to demonstrate for the first time that EP1 inhibition has neuroprotective effects against acute and long term brain damage. These results were supported by in vivo studies of EP1 double knockout mice with ischemic reperfusion injury. In addition, a related study has demonstrated that stimulating another EP receptor with an agonist can increase brain damage in mice due to excitotoxicity or ischemic re-perfusion injury. These results suggest that blocking these receptors either before or after an ischemic event may reduce neurological-associated injury. Description (Set) Proposed Use (Set) The development and/or manufacturing of an antagonist to EP receptors may aid preventative or therapeutic actions against neurological dysregulation in situations where blood flow is impaired in either acute or chronic neurological conditions. Any potential alternative to the proscribed COX-2 medication could provide the next generation of therapy to an aging population in a market worth approximately $30 billion per annum. Patent (Set) WO 2006/135545 A2

Inventor(s): Dore, Sylvain

Type of Offer: Licensing



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