Sousa-Brito, Hellida Larissa; Arruda-Barbosa, Loeste; Vasconcelos-Silva, Alfredo Augusto; Gonzaga-Costa, Karoline; Duarte, Gloria Pinto; Borges, Rosivaldo Santos; Magalhaes, Pedro Jorge Caldas; Lahlou, Saad published the artcile< Vasorelaxant effect of trans-4-chloro-β-nitrostyrene, a synthetic nitroderivative, in rat thoracic aorta>, Product Details of C8H6ClNO2, the main research area is trans chloro nitrostyrene vasorelaxant thoracic aorta structure activity relationship; IP3 receptors; calcium influx; endothelium-independent vasorelaxation; ryanodine-sensitive Ca2+ channels; trans-4-chloro-β-nitrostyrene.
Previously, we showed that 1-nitro-2-phenylethene, a nitrostyrene derivative of 1-nitro-2-phenylethane, induced vasorelaxant effects in rat aorta preparations Here, we studied mechanisms underlying the vasorelaxant effects of its structural analog, trans-4-chloro-β-nitrostyrene (T4CN), in rat aortic rings. Increasing concentrations of T4CN (0.54-544.69μM) fully and similarly relaxed contractions induced by phenylephrine (PHE, 1μM) or KCl (60 mM) in endothelium-intact aortic rings with IC50 values of 66.74 [59.66-89.04] and 79.41 [39.92-158.01] μM, resp. In both electromech. and pharmacomech. couplings, the vasorelaxant effects of T4CN remained unaltered by endothelium removal, as evidenced by the IC50 values (108.35 [56.49-207.78] and 65.92 [39.72-109.40] μM, resp.). Pretreatment of endothelium-intact preparations with L-NAME, ODQ, glibenclamide, or TEA did not change the vasorelaxant effect of T4CN. Under Ca2+-free conditions, T4CN significantly reduced the phasic contractions induced by caffeine or PHE, as well as the contractions due to exogenous CaCl2 in aortic preparations stimulated with PHE (in the presence of verapamil). These results suggest that in rat aortic rings, T4CN induced vasorelaxation independently from the activation of soluble guanylate cyclase/cGMP pathway, an effect that may be related to the electrophilicity of the substituted chloro-nitrostyrene. This vasorelaxation seems to involve inhibition of both calcium influx from the extracellular milieu and calcium mobilization from intracellular stores mediated by IP3 receptors and by ryanodine-sensitive Ca2+ channels.
Fundamental & Clinical Pharmacology published new progress about Arterial endothelium, thoracic aorta endothelium. 5153-70-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClNO2, Product Details of C8H6ClNO2.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics