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In this paper, an analogue of hirsutine (compound  1 ) has been synthesized and evaluated as an anti-hypertension agent, which exhibits extraordinary effects on the contractile response of thoracic aorta rings from male SD rats in vitro (IC 50  = 1.129×10 -9 ±0.5025) and the abilities of reducing the systolic blood pressure (SBP) and heart rate (HR) of SHR in vivo. The mechanism investigation reveals that the vasodilatation induced by compound  1  is mediated by both endothelium-dependent and -independent manners. The relaxation in endothelium-intact aortic rings induced by compound  1  can be inhibited by L-NAME (1×10 -6  mol•L -1 ) and ODQ (1×10 -6  mol•L -1 ). Moreover, compound  1  can also block Ca 2+  influx through L-type Ca 2+  channels and inhibit intracellular Ca 2+  release while no effect on K +  channel has been observed. All these data demonstrated that the NO/cyclic GMP pathway can be involved in endothelium-dependent manner induced by compound  1 . Meanwhile the mechanism on the vasodilatation of compound  1  probably also related to blockade of Ca 2+  influx through L-type Ca 2+  channels and inhibition of intracellular Ca 2+  release may have no relationship with K +  channels.

The Novel Analogue of Hirsutine as an Anti-Hypertension and Vasodilatary Agent Both In Vitro and In Vivo