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Vasorelaxant effect of 3,4-dihydro-2-(4-morpholinylmethy)-1(2H)-naphthalenone on the vascular smooth muscle of rabbits

Xue Li, Yuan-Yuan Wei, Shou-Ting Fu*, Lan Zhu, Bing Wang   

  1. 1. School of the Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, China
    2. Cardiovascular Medicine, Shenyang 245 Hospital, Shenyang 110000, China
  • Received:2009-03-03 Revised:2009-05-10 Online:2009-06-15 Published:2009-06-15
  • Contact: Shou-Ting Fu*

Abstract:

The purpose of this study was to examine the relaxation effect of CY on the vascular smooth muscle (VSM) from rabbits. Experiments were carried out on isolated thoracic aorta of rabbits. CY (3×10–3 mM – 3 mM) could relax the VSM preparations pre-contracted by adrenaline (AD), noradrenaline (NE), high-K+ solution or BaCl2 with respective EC50 values of (0.31±0.11) mM, 0.19±0.03 mM, 0.20±0.04 mM and 0.25±0.04 mM. Moreover, CY (10–2 mM, 0.1 mM and 1 mM) inhibited norepinephrine (NE), CaCl2 and KCl-induced vasoconstriction in a concentration dependent manner. The phasic contraction produced by NE was concentration dependently attenuated with CY (10–2 mM, 0.1 mM and 1 mM) in calcium-free medium, similar to that caused by verapamil. The present findings suggest that CY relaxed thoracic aortic rings by blocking voltage-dependent Ca2+ channels. The inhibition of intracellular Ca2+ release may be one of the main vasorelaxant mechanisms of CY.

Key words: 3,4-Dihydro-2-(4-morpholinylmethy)-1(2H)-naphthalenone, 3,4-Dihydro-2-(4-morpholinylmethy)-1(2H)-naphthalenone, Vascular smooth muscle, Vascular smooth muscle, Ca2+ channels, Ca2+ channels, Rabbit, Rabbit

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