Key result
Protopine acts as a promiscuous inhibitor of cation channel currents including I(Ca,L), I(K), I(K1), and I(Na) in guinea-pig ventricular myocytes, reducing I(Ca,L) amplitude by up to 54.2%.
Population
Single isolated ventricular myocytes from guinea-pig
Comparison
Extracellular application of Protopine at… vs Control (absence of Protopine)
Design
Preclinical
Authors
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Protopine’s multi-channel effects in guinea-pig myocytes warrant mechanistic caution; leaves open translation to human anti-arrhythmic use.
Protopine exerts its anti-arrhythmic and negative inotropic effects through promiscuous inhibition of multiple cation channels (I(Ca,L), I(K), I(K1), I(Na)) rather than selective calcium channel blockade.
Song et al. (2000) studied this question. Protopine vs. Control was evaluated on L-type Ca(2+) current (I(Ca,L)) amplitude and other cation channel currents. Protopine acts as a promiscuous inhibitor of cation channel currents including I(Ca,L), I(K), I(K1), and I(Na) in guinea-pig ventricular myocytes, reducing I(Ca,L) amplitude by up to 54.2%.
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