Abstract
Benzylisoquinoline compounds antagonised the ability of calmodulin (CaM) to stimulate the activity of calmodulin-dependent cyclic nucleotide phosphodiesterase (CaM-PDE). This ‘anti-CaM’ activity was related to the hydrophobicity of the non-polar terminal region of the antagonist molecule. Antagonistic potency increased with the increase of hydrophobicity; the anti-CaM activity did not change when the polar terminus was a tertiary amine or quarternary amine. The anti-CaM potency was greater for bisbenzylisoquinoline compounds than for monobenzylisoquinoline compounds. Among the bidbenzylisoquinoline compounds anti-CaM pathway was: D 3 > D 2 berbamine > daurisoline > dauriune. Compound D 3, which exhibited an IC 50 value of 2.8 μM, was one of the most potent calmodulin antagonists, among benzylisoquinoline compounds, so far reported.
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