- Zheng, W. et al. (1991) Mol. Pharmacol. 40, 734.
- Alomone Labs FPL 64176 increases L-type CaV channels currents expressed in Xenopus oocytes.A. Time course of CaV1.2 (co expressed with α2δ1 and β1 auxiliary subunits) tail peak current amplitude, elicited by 100 ms voltage step from holding potential of -100 mV to -10 mV, delivered every 10 seconds. Application of 0.1 and 1 µM FPL 64176 (#F-160) increases the CaV1.2 current (indicated by the horizontal bar). B. Representative current traces before and during application of 0.1 and 1 µM FPL 64176 (as indicated).
FPL 64176 acts as a non-dihydropyridine L-type calcium channel activator with high efficacy properties. It's a benzoylpyrrole compound that has the ability to increase macroscopic inward current through L-type calcium channels. It extends the opening of single calcium channels during depolarization and slows channel closing upon repolarization without affecting currents through other calcium channels1-3.
FPL 64176 is being used as a tool for studying the physiological roles and disorders of L-type channels, identification of L-type currents within the mix of channel subtypes and for increasing the contractility of smooth and cardiac muscle2.
The use of FPL 64176 has revealed an inactivation and adaptation process for ryanodine receptors and the presence of cardiac sparklets3,4.
L-type voltage-gated calcium channels are one of the three major classes (CaV1-CaV3) of voltage-gated calcium channels. They are expressed in many excitable tissues and play as important transducers in the plasma membrane, altering membrane depolarization to intracellular signaling. Many physiological functions, including brain, endocrine, and sensory functions and muscle contraction rely on proper L-type channel activity5.