International Journal of Pharmacy and Pharmacology

ISSN 2326-7267

International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (4), pp. 001-010, April, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals

Full Length Research Paper

Inotropic Activity Assessment of a Newly Synthesized Estradiol Derivative Using Isolated Rat Heart Preparations

Figueroa-Valverde L.1*, Díaz-Cedillo F.2, López-Ramos M.1, García-Cervera E1 and Pool-Gómez E.1

1Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, Universidad Autonóma de Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México. 2Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional. Prol. Carpio y Plan de Ayala s/n Col. Santo Tomas, México, D.F. C.P. 11340.

Accepted 8 January, 2025

Several studies indicate that some steroid derivatives have inotropic activity; nevertheless, there is scarce information about the effects of the estradiol derivatives at cardiovascular level. Therefore, in this study, estradiol derivative was synthetized with the objective of evaluating its inotropic activity. In this first stage, the Langendorff technique was used to measure perfusion pressure and coronary resistance changes in isolated rat heart in absence or presence of estradiol derivative. In second stage, the inotropic activity of estradiol derivative was evaluated by measuring left ventricular pressure in absence or presence of following compounds; tamoxifen, prazosin, metoprolol, indomethacin and nifedipine. The results showed that the estradiol derivative significantly increase the perfusion pressure and coronary resistance in isolated heart. Additionally, other data indicate that estradiol derivative increase left ventricular pressure in a dose-dependent manner [10-9 to 10 -4 mmol]; nevertheless, this phenomenon was significantly inhibited by nifedipine at a dose of 1 × 10-6 mmol. In conclusion, these data suggest that the estradiol derivative induces positive inotropic activity through of activation the L-type calcium channel.

Key words: Estradiol derivative, Langendorff, inotropic activity.