title: [Inotropic activity induced by carbamazepine-alkyne derivative in an isolated heart model and perfused to constant flow].
abstract: Inotropic activity induced by carbamazepine-alkyne derivative in an isolated heart model and perfused to constant flow Introduction. Few data exist with respect to the effects of carbamazepine and its derivatives at cardiovascular level; furthermore, the molecular mechanisms and cellular site of action are still unclear. Objective. The effects induced by carbamazepine-alquine derivative on perfusion pressure, vascular resistance and left ventricular pressure were evaluated. Materials and methods. The effects of carbamazepine and carbamazepine-alquine on the perfusion pressure, vascular resistance and left ventricular pressure were examined in isolated rat hearts (Langendorff model). Results. Four results were obtained: (1) The carbamazepine-alquine derivative 10-9 mM increased the perfusion pressure and vascular resistance in comparison with the carbamazepine 10-9 mM; (2) the effect of carbamazepine-alquine derivative 10-9-10-4 mM on left ventricular pressure not was inhibited by metoprolol or prazosin at a dose of 10-6 mM; (3) nifedipine 10-6 mM blocked the effects exerted by the carbamazepine-alquine derivative 10-9-10--4 mM on left ventricular pressure, and (4) the carbamazepine-alquine derivative at dose of 10-9 mM increased the concentration of intracellular calcium over a time period of 3-18 min; nevertheless, in presence of nifedipine 10-6 mM this effect was inhibited significantly (p=0.005). Conclusions. The activity exerted by carbamazepine-alquine derivative on perfusion pressure, vascular resistance and left ventricular pressure involved activation of calcium channel type-L, brought indirectly changes in the intracellular calcium levels and subsequently induced a positive inotropic effect.
authors.affiliation: Laboratorio de Investigación en Ciencias Biológicas y Fármaco-Química, Facultad de Ciencias Químico- Biológicas, Universidad Autónoma de Campeche, Campeche, México. lauro_1999@yahoo.com
authors.forename: Lauro
authors.initials: L
authors.lastname: Figueroa-Valverde
authors.forename: Francisco
authors.initials: F
authors.lastname: Díaz-Cedillo
authors.forename: María
authors.initials: M
authors.lastname: López-Ramos
authors.forename: Elodia
authors.initials: E
authors.lastname: García-Cervera
authors.forename: Karen
authors.initials: K
authors.lastname: Quijano-Ascencio
mesh_terms: D000480:Alkynes / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002118:Calcium / Q000378:metabolism; D020746:Calcium Channels, L-Type / Q000378:metabolism; D002220:Carbamazepine / Q000737:chemistry* / Q000494:pharmacology*; D006321:Heart / Q000187:drug effects* / Q000502:physiology*; D015394:Molecular Structure; D009200:Myocardial Contraction / Q000187:drug effects*; D010477:Perfusion; D051381:Rats; D017208:Rats, Wistar; D013268:Stimulation, Chemical; D014655:Vascular Resistance / Q000187:drug effects; D017725:Ventricular Pressure / Q000187:drug effects
chemical_list: D000480:Alkynes; D020746:Calcium Channels, L-Type; D002220:Carbamazepine; D002118:Calcium