Changes Induced by Estradiol-Ethylenediamine Derivative on Perfusion Pressure and Coronary Resistance in Isolated Rat Heart: L-Type Calcium Channel

Abstract

Aim. The present study was designed to investigate the effects of estradiol-ethylenediamine derivative on perfusion pressure and coronary resistance in rats. An additional aim was to identify the molecular mechanisms involved.Methods. The Langendorff model was used to measure perfusion pressure and coronary resistance changes in isolated rat heart after estradiol-ethylenediamine derivative alone and following compounds; tamoxifen (estrogen receptor antagonist), prazosin (alpha1 adrenoreceptor antagonist), metoprolol (selective beta1 receptor blocker), indomethacin (prostanglandin synthesis inhibitor) and nifedipine (L-type calcium-channel inhibitor).Results. The results show that estradiol-ethylenediamine derivative [10 -9 mmol] significantly increased perfusion pressure (p = 0.005) and coronary resistance (p = 0.006) in isolated rat heart. Additionally, the effect of estradiolethylenediamine on perfusion pressure [10 -9 to 10 -4 mmol] was only blocked in the presence of the L-type calciumchannel (nifedipine).Conclusions. These data suggest that the effect of estradiol-ethylenediamine on perfusion pressure and vascular coronary involves activation of the L-type calcium channel through a non-genomic molecular mechanism.

Preparation of two steroid derivatives and its theoretical interaction with a 17β‐hydroxysteroid dehydrogenase type 1

“…The 1 H NMR spectra for 2 ( Figure 1) showed several signals at 0.90 ppm for methyl bound to steroid nucleus; at 1.20-2.60, 6.54 and 6.90 ppm for steroid moiety: at 3.72 ppm for methylene bound to both amino group and ring A of steroid nucleus; at 6.80 and 7.56-8.70 ppm for phenyl groups; at 3.04, 3.80 ppm for methylene groups bound to both amino groups; at 7.58 ppm for both amino and hydroxyl groups. 13…”

“…The estradiol-ethylenediamine derivative was prepared using a previous method reported [13]. In addition, all the reagents used in this study were purchased from Sigma-Aldrich Sigma-Aldrich Co., Ltd.…”

“…Infrared spectra (IR) were determined using KBr pellets on a Perkin Elmer Lambda 40 spectrometer. 1 H and 13 C NMR (nuclear magnetic resonance) spectra were recorded on a Varian VXR300/5 FT NMR spectrometer at 300 and 75.4 MHz (megahertz) in CDCl 3 (deuterated chloroform) using TMS (tetramethylsilane) as an internal standard. EIMS (electron impact mass spectroscopy) spectra were determined using a Finnigan Trace Gas Chromatography Polaris Q-Spectrometer.…”

GPER modulates tone and coronary vascular reactivity in male and female rats

“…The mechanisms responsible for the increased CPP levels observed in female rats compared with male rats of the same age have not been fully elucidated. However, Figueroa-Valverde and coworkers (Figueroa-Valverde et al 2011) demonstrated that oestradiol infusion significantly increased the perfusion pressure and coronary resistance of isolated hearts in rats due to an increase in calcium levels via activation of L-type calcium channels through nongenomic molecular mechanisms. In fact, our results show that after castration, the CPP was significantly reduced in the female group.…”

New Amino-steroid-anthracenone with Biological Activity Against Ischemia-reperfusion Injury in a Wistar Rat Model

“…It is important that the study population involved in each group was n = 9. *Krebs-Henseleit system was composed of the following substances in mmol concentrations per liter; 117.8 NaCl; 6 KCl; 1.75 CaCl 2 ; 1.2 NaH 2 PO 4 ; 1.2 MgSO 4 ; 24.2 NaHCO 3 ; 5 glucose, and 5 sodium pyruvate [27]. The solution was then bubbled with a mixture of O 2 /CO 2 (95:5/5%) and the mixture was regulated to a pH of 7.4 (37°C).…”