ONO-8130 是前列腺素 EP1 受体选择性拮抗剂,口服有活力,能够阻断 L6 脊髓中ERK的磷酸化。它可缓解环磷酰胺致膀胱炎小鼠的膀胱疼痛,可用于研究间质性膀胱炎。
产品描述
ONO-8130 is an orally available antagonist of EP1 receptor.
体内活性
Oral preadministration of ONO-8130 at 0.3-30 mg/kg 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.?Oral ONO-8130 at 30 mg/kg also reversed the established cystitis-related bladder pain.?Intravesical administration of prostaglandin E2 caused prompt phosphorylation of ERK in the L6 spinal cord, an effect blocked by ONO-8130.?The prostaglandin E2/EP1 system participates in processing of cystitis-related bladder pain, and that EP1 antagonists including ONO-8130 are useful for treatment of bladder pain, particularly in interstitial cystitis.?Prostaglandin E2 contributes to cystitis-related bladder pain via EP1 receptors in mice, indicating possible therapeutic usefulness of selective EP1 antagonists[1].
Cas No.
459841-96-4
分子式
C25H28N2O5S2
分子量
500.63
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years