Centhaquin is a compound that produces
hypotension and
bradycardia in higher doses and
resuscitation in lower doses. It is water insoluble, and is unsuitable for intravenous use. We prepared the
citrate salt of
centhaquin and evaluated its cardiovascular efficacy vs.
centhaquin.
Centhaquin citrate was prepared and characterized; its purity was determined by HPLC. Mean arterial pressure (MAP), heart rate (HR), pulse pressure (PP), cardiac output (CO), stroke volume (SV) and
stroke work (SW) following
intravenous administration of
centhaquin and the
citrate (0.05, 0.15 and 0.45 mg.kg(-1)) were determined in anaesthetized male Sprague-Dawley rats.
Centhaquin citrate was 99.8% pure and water soluble.
Centhaquin (0.05, 0.15 and 0.45 mg.kg(-1)) produced a maximal decrease in MAP of 15.6, 25.2 and 28.1%, respectively; while
centhaquin citrate produced a greater (p<0.001) decrease of 35.7, 47.1 and 54.3%, respectively. The decrease in PP and HR produced by the
citrate was greater than
centhaquin (p<0.001). At 0.45 mg.kg(-1)
centhaquin produced a maximal decrease of 20.9% (p<0.01) in CO, while
centhaquin citrate produced a decrease of 42.1% (p<0.001). Reduction in SV (p<0.01) and SW (p<0.001) produced by
centhaquin citrate were greater than
centhaquin.
Centhaquin citrate has greater cardiovascular activity compared to
centhaquin.