TG4-155 is a brain penetrant prostaglandin EP2 specific antagonist. TG4-155 has a 4730X selectivity over EP4 (2.4 nM vs 11.4 mM in binding assays), and a 7 fold selectivity over DP1 receptors. TG4-155 crosses the blood brain barrier, and has no antagonistic effects on EP4 signaling, and displays neuroprotective effects in a pilocarpine-induced status epilepticus (SE) seizure model. TG4-155 does not interfere with G-protein function or phosphodiesterase activity, and does not inhibit COX-1 or COX-2.
British journal of pharmacology, 176(11), 1680-1699 (2019-02-15)
An up-regulation of COX-2 in malignant gliomas causes excessive synthesis of PGE2 , which is thought to facilitate brain tumour growth and invasion. However, which downstream PGE2 receptor subtype (i.e., EP1 -EP4 ) directly contributes to COX activity-promoted glioma growth
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