| Compound inhibition testing of native, human L-type calcium current (ICa,L) under near-physiological temperature and ionic conditions. |
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Parameters Evaluated:
- ICa,L pharmacological response
- use-dependence
Method:
- manual patch clamp (voltage clamp mode)
- 2-4 concentrations
- n≥2 cells/concentration
- control: nifedipine
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| Figure 1: Effect of nifedipine on ICa,L current. The peak current obtained at 0 mV was reduced compared with control after application of 3, 10, 30 and 100 nM nifedipine (top panel). The mean percent block of ICa,L current (bottom panel) after application of each concentration of nifedipine (circles) ± S.E.M. (vertical bars) was fit to a simple binding equation (solid line). The calculated IC50 was 25 nM. The number of observations is shown in parentheses. Current traces were recorded by depolarizing test pulses to 0 mV for 300 ms repeated at 5 s intervals from a holding potential of –40 mV. Peak current elicited during the test pulse was used to measure concentration-response relationship. |
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