ONO-8130 是一种口服有效和选择性的前列腺素 EP1 受体 (
EP1 receptor) 拮抗剂。ONO-8130 可阻断 L6 脊髓中
ERK的磷酸化。ONO-8130 可减轻环磷酰胺致膀胱炎小鼠的膀胱疼痛。ONO-8130 可用于间质性膀胱炎的研究。
| 生物活性 |
ONO-8130 is an orally active and selective prostanoidEP1 receptorantagonist. ONO-8130 blocks phosphorylation ofERKin the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research[1].
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体内研究
(In Vivo) |
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[1].
ONO-8130 (30 mg/kg; Orally, once) reverses the established cystitis-related bladder pain[1].
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[1].
| Animal Model: |
Female ddY mice (18-22 g, 4-5 weeks old)[1] |
| 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)[1] |
| 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)[1] |
| 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)[1] |
| 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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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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