Dabuzalgron 是一种口服活性选择性 α-1A 肾上腺素受体激动剂，用于治疗尿失禁。它通过维持线粒体功能来预防多柔比星引起的心脏毒性。

Dabuzalgron is an orally active selective alpha-1A adrenergic receptor agonist used to treat urinary incontinence. Dabuzaron prevents cardiotoxicity caused by doxorubicin by maintaining mitochondrial function.

Dabuzaron treatment increased ERK phosphorylation in a dose-dependent manner with an EC50 of 4.8 μM. ERK1 / 2 activation helps Dabuzaron's cardioprotection. Dabuzaron (10 μM; 4 hours) protects NRVM from cell death caused by doxorubicin (DOX). Dabuzaren (10 μM; 4 hours) activation of α1A-AR alleviates the harmful effects of DOX on mitochondrial membrane potential and eliminates the activation of important elements of the apoptotic response to mitochondrial damage.

Dabuzaron (10μg / kg; oral tube; twice daily; 7 consecutive days; C57B16J wild-type or α1A-AR gene knockout mice) treatment can prevent DOX cardiotoxicity by activating α1A-AR. Dabuzaron prevents mitochondrial function-related transcript reduction, up-regulates PGC1α, retains ATP content, and reduces oxidative stress in DOX-treated mouse hearts.

219311-44-1

C12H16ClN3O3S

317.79

达布扎琼;Ro 115-1240

DMSO:25 mg/mL(78.67 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years