ONO-8130

Research use only, not for human use.

ONO-8130 is an orally available antagonist of EP1 receptor.

ONO-8130 is an orally available antagonist of EP1 receptor.

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ONO-8130 (0.3-30 mg/kg; Oral preadministration, once) strongly prevents both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent manner.ONO-8130 (30 mg/kg; Orally, once) reverses the established cystitis-related bladder pain.ONO-8130 (30 mg/kg; Orally, once) strongly inhibits phosphorylation of ERK in MDH, DCM, and SPN of the L6 spinal cord caused by intravesical administration of PGE2. Animal Model:Female ddY mice (18-22 g, 4-5 weeks old)Dosage:0.3, 3, 10, and 30 mg/kg Administration: Orally, once Result:Strongly prevented both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent manner, but had slight effect on the increased bladder weight and vascular permeability.Animal Model:Female ddY mice (18-22 g, 4-5 weeks old, established bladder pain caused by IP cyclophosphamide)Dosage:10, 30 mg/kgAdministration:Orally, once (administered 2.75 hours after i.p. cyclophosphamide) Result:Markedly attenuated the bladder pain-like nociceptive behavior and referred hyperalgesia in the acute phase (3.5-4 h after cyclophosphamide).Animal Model:Female ddY mice (18-22 g, 4-5 weeks old, established bladder pain caused by IP cyclophosphamide)Dosage:30 mg/kgAdministration:Orally, once (administered 4.75 hours after i.p. cyclophosphamide)Result:Significantly suppressed the bladder pain-like nociceptive behavior and tended to reduce the referred hyperalgesia in the persistent phase, 5.5-6 hours after cyclophosphamide.Animal Model:Female ddY mice (18-22 g, 4-5 weeks old, intravesical administration of PGE2 at 5 nmol/mouse)Dosage:30 mg/kg Administration:Orally, once Result:Strongly inhibited phosphorylation of ERK in MDH, DCM, and SPN of the L6 spinal cord caused by intravesical administration of PGE2 at 5 nmol/mouse, exerted complete blockade in DCM, while its inhibitory effects in MDH and SPN were partial.

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GPCR/G Protein

Prostaglandin Receptor

EP1

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459841-96-4

500.63

C25H28N2O5S2

>98% (HPLC)

DMSO:10 mM

CC1=CSC(=N1)S(=O)(=O)N(CC(C)C)C2=C(C=C3CCCC3=C2)OCC4=CC=C(C=C4)C(=O)O

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(-20℃)

With Ice Pack

≥ 2 years