Cardiac Ca^<2+> Channel-Blocking Effects of the Cyproheptadine Derivative AH-1058 in Isolated Guinea Pig Cardiomyocytes

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The Ca2+ channel-blocking efficacy of the cyproheptadine derivative AH-1058 (4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-[(E)-3-(3-methoxy-2-nitro)phenyl-2-propenyl]piperidine hydrochloride) was quantitatively assessed using isolated guinea pig cardiomyocytes. AH-1058 (0.001 – 10 μM) and its mother compound cyproheptadine (1 – 100 μM) reduced the Ca2+ currents elicited from the holding potential of −80 or −40 mV. The IC50 values for cyproheptadine at holding potentials of −80 and −40 mV were 42.44 and 7.75 μM, respectively, whereas those for AH-1058 were 4.91 and 0.32 μM, respectively, whose potency was equivalent to those of the typical Ca2+ channel blocker verapamil. These results suggest that the introduction of the cinnamil structure to cyproheptadine can generate a potent L-type Ca2+ channel-blocking compound as potent as verapamil.
社団法人日本薬理学会の論文
2003-02-01