Target Validation Information
TTD ID	T85467
Target Name	Prostaglandin E2 receptor EP3 (PTGER3)
Type of Target	Clinical trial
Drug Potency against Target	DG041	Drug Info	IC50 = 5 nM
	3-(2-((E)-3-phenylprop-1-enyl)phenyl)acrylic acid	Drug Info	Ki = 100 nM	[2]
	3-(2-(4-methoxycinnamyl)phenyl)acrylic acid	Drug Info	Ki = 68 nM	[2]
	3-(2-(naphthalen-2-ylmethyl)phenyl)acrylic acid	Drug Info	Ki = 400 nM	[2]
	3-(2-cinnamylphenyl)acrylic acid	Drug Info	Ki = 100 nM	[2]
	FR-181157	Drug Info	Ki = 6800 nM	[1]
	LAROPIPRANT	Drug Info	Ki = 892 nM	[3]
Action against Disease Model	DG041	Drug Info	The bladder rhythmic contraction model and a bladder pain model measuring the visceromotor reflex (VMR) to urinary bladder distension (UBD) have been used to evaluate DG-041 in female rats. DG-041 (10 mg/kg), a peripherally restricted EP3 receptor antagonist, significantly reduced the frequency of bladder rhythmic contraction and inhibited the VMR response to bladder distension. DG-041 selectively attenuated responses of mechanosensitive afferent nerves to UBD, with strong suppression on the slow-conducting, high-threshold afferent fibers, with equivalent activity in thethree strains. We conclude that sensitization of afferent nerve activity was not one of the mechanisms of bladder hypersensitivity in SHR. EP3 receptors are involved in the regulation of bladder micturition and bladder nociception at the peripheral level.	[4]
References
REF 1	Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4. Bioorg Med Chem Lett. 2005 Jul 1;15(13):3284-7.
REF 2	Comparison between two classes of selective EP(3) antagonists and their biological activities. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5639-42.
REF 3	Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806.
REF 4	An excitatory role for peripheral EP3 receptors in bladder afferent function. Am J Physiol Renal Physiol. 2008 Aug;295(2):F585-94.

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