Uses
L-798106 is a potent and selective prostanoid receptor EP3-selective antagonists. L-798106 has been used in multiple studies to tease out EP3 agonist activity, both in vitro and in vivo. L-798106 successfully blocks the actions of sulprostone, an EP3-selective agonist. L-798106 was useful in showing that the vascular contraction effect of PGE2 is due to its prostanoid EP3 agonist activity.
Uses
L-798106, a selective prostanoid receptor EP3 antagonist, is used in prostanoid receptor signaling studies that regulate COX-2 levels and the central excitatory effects of PGE(2) on PVN neurons.
Definition
ChEBI: L-798106 is an N-sulfonylcarboxamide resulting from the formal condensation of the carboxy group of o-naphthalen-2-ylcinnamic acid with the sulfonamide group of 5-bromo-2-methoxybenzenesulfonamide. It is a selective antagonist for the prostanoid receptor EP3, a prostaglandin receptor for prostaglandin E2 (PGE2). It has a role as a prostaglandin receptor antagonist. It is a N-sulfonylcarboxamide, a member of bromobenzenes and an aromatic ether.
Biochem/physiol Actions
L-798106 was among the first prostanoid receptor EP3-selective antagonists. It has been used in multiple studies to tease out EP3 agonist activity, both in vitro and in vivo. It successfully blocks the actions of sulprostone, an EP3-selective agonist, and it helped show that the vascular contraction effect of PGE2 is due to its prostanoid EP3 agonist activity.
in vivo
L-798106 (oral gavage; 50 and 100 μg/kg; once daily; 8 w) suppresses systemic insulin resistance and AT inflammation in db/db mice[3].
| Animal Model: | Male db/db mice[3] |
| Dosage: | 50 and 100 μg/kg |
| Administration: | Oral gavage; 50 and 100 μg/kg; once daily; 8 weeks |
| Result: | Suppressed the increased fasting blood glucose levels in the db/db mice.
Suppressed increased proinflammatory gene expressions in the adipocytes isolated from the epididymal AT of the db/db mice. |
IC 50
EP3: 0.3 nM (IC50); EP4: 916 nM (IC50); EP1: >5000 nM (IC50); EP2: >5000 nM (IC50)
