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Drug Res (Stuttg) 2023; 73(05): 263-270
DOI: 10.1055/a-1995-6351
Original Article

Evaluation of Biological Activity Exerted by Dibenzo[b,e]Thiophene-11(6H)-One on Left Ventricular Pressure Using an Isolated Rat Heart Model

Lauro Figueroa-Valverde
1   Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche, Campeche, Camp., México
,
Marcela Rosas-Nexticapa
2   Facultad de Nutrición, Universidad Veracruzana, Médicos y Odontologos, Unidad del Bosque Xalapa Veracruz, México
,
Magdalena Alvarez-Ramirez
2   Facultad de Nutrición, Universidad Veracruzana, Médicos y Odontologos, Unidad del Bosque Xalapa Veracruz, México
,
Maria López-Ramos
1   Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche, Campeche, Camp., México
,
Francisco Díaz-Cedillo
3   Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional. Santo Tomas, México
,
Maria Virginia Mateu-Armad
2   Facultad de Nutrición, Universidad Veracruzana, Médicos y Odontologos, Unidad del Bosque Xalapa Veracruz, México
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Abstract

Background Some studies show that some Dibenzo derivatives can produce changes in the cardiovascular system; however, its molecular mechanism is not very clear.

Objective The objective of this investigation was to evaluate the inotropic activity of ten Dibenzo derivatives (compounds 1 to 10) on either perfusion pressure or left ventricular pressure.

Methods Biological activity produced by the Dibenzo derivatives on either perfusion pressure or coronary resistance was evaluated using an isolated rat heart. In addition, the molecular mechanism of biological activity produced by compound 4 (Dibenzo[b,e]thiophene-11(6H)-one) on left ventricular pressure was determined using both Bay-k8644 and nifedipine as pharmacological tools in an isolated rat heart model.

Results The results showed that Dibenzo[b,e]thiophene-11(6H)-one increases perfusion pressure and coronary resistance at a dose of 0.001 nM. Besides, other data display that Dibenzo[b,e]thiophene-11(6H)-one increases left ventricular pressure in a dose-dependent manner (0.001 to 100 nM) and this effect was similar to biological activity produced by Bay-k8644 drug on left ventricular pressure. However, the effect exerted by Dibenzo[b,e]thiophene-11(6H)-one was inhibited in the presence of nifedipine at a dose of 1 nM.

Conclusions All these data suggest that Dibenzo[b,e]thiophene-11(6H)-one increase left ventricular pressure through calcium channel activation. In this way, Dibenzo[b,e]thiophene-11(6H)-one could be a good candidate as positive inotropic agent to heart failure.

Key words

Dibenzo - derivative - calcium - channel


Publication History

Received: 17 November 2022

Accepted: 06 December 2022

Article published online:
01 March 2023

© 2023. Thieme. All rights reserved.

Georg Thieme Verlag
Rüdigerstraße 14, 70469 Stuttgart, Germany

 

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