TG6-10-1 is a potent and selective antagonist of prostaglandin E2 receptor subtype EP2 with Kb of 17.8 nM.
TG6-10-1 displays >300-fold selectivity over EP3, EP4, and IP receptors, 100-fold selectivity over EP1, 25-fold selectivity over FP and TP, and 10-fold selectivity over DP1 receptors.
TG6-10-1 completely recapitulates the effects of conditional ablation of COX-2 from principal forebrain neurons, accelerates recovery from weight loss, reduces brain inflammation, prevention of blood-brain barrier opening, and neuroprotection in the hippocampus, without modifying seizures acutely in the mouse pilocarpine model of SE.
