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

Objective To investigate the spasmolytic and anti-diarrheal activities of 3,4-dihydro-2-(4-morpholinylmethy)-1(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 concentration of 0.01 to 3 mM;the diarrheal-index was evaluated on diarrhea mice to study the anti-diarrheal activities of CY.Results CY(0.1-1 mM)inhibited spontaneous motility of rabbit small intestine and at the concentration 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 BaCl2(1 mg·mL-1).When tested against calcium channel blocked in rabbit small intestine and colon,CY caused a rightward shift in the Ca2+ dose-response curves,similar to that produced by verapamil,a well-known calcium antagonist.CY could inhibit the diarrhea induced by castor oil,MgSO4 and liquid paraffin and LD50 of CY is 277.2 mg·kg-1.Conclusions CY may produce its spasmolytic and anti-diarrheal effects as a calcium antagonist.