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Anti-diarrheal and spasmolytic activities study of 3,4-Dihydro-2-(4-Morpholinylmethy)-1(2H)-Naph-thalenone(CY)

【摘要】:正Objective To investigate the spasmolytic and anti-diarrheal activities of 3,4-dihydro-2-(4-mor- pholinylmethy)-l(2H)-naphthalenone (CY),which was first synthesized by Welch,Willard M et al.in 1977.Methods The spasmolytic effects of CY were tested on isolated rabbit small intestine at the concentra- tion of 0.01 to 3 mM;the diarrheal-index was evaluated on diarrhea mice to study the anti-diarrheal activi- ties of CY.Results CY (0.1-1 mM) inhibited spontaneous motility of rabbit small intestine and at the con- centration of 0.01 to 3 mM CY inhibited the contractile response of rabbit small intestine and colon induced by acetylcholine (10~(-2) mg·mL~(-1)),high K~+(60 mM) and BaCl_2 (1 mg·mL~(-1)).When tested against calci- um channel blocked in rabbit small intestine and colon,CY caused a rightward shift in the Ca~(2+) dose-re- sponse curves,similar to that produced by verapamil,a well-known calcium antagonist.CY could inhibit the diarrhea induced by castor oil,MgSO_4 and liquid paraffin and LD_(50) of CY is 277.2 mg·kg~(-1).Conclusions CY may produce its spasmolytic and anti-diarrheal effects as a calcium antagonist.

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