Abstract
There is scarce information about the effects of danazol and its derivatives at cardiovascular level. In addition, to date the cellular site and mechanism of action of danazol at the cardiovascular level is very confusing. In order to clarify those phenomena in this study, a danazol derivative was synthesized with the objective of evaluating its activity on perfusion pressure and coronary resistance and comparing this phenomenon with the effect exerted by danazol. The Langendorff technique was used to measure changes on perfusion pressure and coronary resistance in an isolated rat heart model in the absence or presence of danazol and its derivative. Additionally, to characterize the molecular mechanism involved in the inotropic activity induced by danazol derivative was evaluated by measuring left ventricular pressure in the absence or presence of following compounds; flutamide, prazosin, metoprolol, indomethacin and nifedipine. The results showed that danazol derivative significantly increased the perfusion pressure and coronary resistance in comparison with the control conditions and danazol. Additionally, other data indicate that the danazol derivative increases left ventricular pressure in a dose-dependent manner; nevertheless, this phenomenon was significantly inhibited by flutamide. These data suggest that danazol derivative induces positive inotropic activity through of the activation androgen receptor.
Highlights
Several reports which indicate that congestive heart failure (CHF) is a main cause of death in patients with heart disease [1,2]
In order to clarify those phenomena in this study, a danazol derivative was synthesized with the objective of evaluating its activity on perfusion pressure and coronary resistance and comparing this phenomenon with the effect exerted by danazol
We considered validating the effect induced by some steroids on perfusion pressure via prostanglandins [36] and to evaluate the possibility that the activities exerted by the danazol derivative involve stimulation and secretion of prostaglandins
Summary
Several reports which indicate that congestive heart failure (CHF) is a main cause of death in patients with heart disease [1,2]. For the treatment of CHF has been several drugs such as the digitalis glycosides, the use of these agents is limited by their narrow therapeutic window and their propensity to cause life-threatening arrhythmias [3,4]. There are studies that show the synthesis of a steroid derivative (F90927) which exerts a positive inotropic activity in cardiac muscle via activation of the L-type Ca2+. Recently other type of steroid derivative (Furosemide-Pregnenolone) was synthesized which showed apositive inotropic activity on cardiac muscle via activation of the L-type Ca2+ channel [8]
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