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编 号:F362315
分子式:C25H28N2O5S2
分子量:500.63
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ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research.

体内研究:
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/kg
Administration: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/kg
Administration: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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