prenylamine

Clinical trial activity

0 trials · 0 clinical orgs · 0 marketing orgs

Mechanism of action

• Sodium channel protein type V alpha subunitBLOCKER

  SCN5A blocker

  Prenylamine is a potent sodium channel (NaCh) blocker during voltage clamp conditions in vitro and a long-acting local anesthetic (LA) when injected into rats for blockage of sciatic nerve in vivo. It interacts with calmodulin and inhibits, dose dependently, myosin light chain kinase (Ca2+-dependent protein kinase) and actomyosin( Ca2+-dependent ATPase) A nonselective inhibitor for slow Ca2+ channels, tends to prolong the cycle length to decrease the diastolic depolarization, the rate of rise of action potential, the amplitude of action potential. Prenylamine also affected several classic apoptosis-related proteins, including Bax, Bcl-2, and cytochrome c, and increased caspase-3 activity.

  Binding of prenylamine to the sodium channels (NaChs) is highly voltage-dependent: The resting affinity (IC50 at -150 mV) for prenylamine in neuronal NaChs is 27.7 +- 1.3 uM, whereas the inactivated affinity (IC50 at -60 mV) is 0.75 +-0.02 uM¿ a 37-fold difference.

  • Sodium channel protein type 5 subunit alpha (SCN5A) ↗
• CalmodulinINHIBITOR

  CALM1 inhibitor

  Prenylamine is a potent sodium channel (NaCh) blocker during voltage clamp conditions in vitro and a long-acting local anesthetic (LA) when injected into rats for blockage of sciatic nerve in vivo. It interacts with calmodulin and inhibits, dose dependently, myosin light chain kinase (Ca2+-dependent protein kinase) and actomyosin( Ca2+-dependent ATPase) A nonselective inhibitor for slow Ca2+ channels, tends to prolong the cycle length to decrease the diastolic depolarization, the rate of rise of action potential, the amplitude of action potential. Prenylamine also affected several classic apoptosis-related proteins, including Bax, Bcl-2, and cytochrome c, and increased caspase-3 activity.

  Binding of prenylamine to the sodium channels (NaChs) is highly voltage-dependent: The resting affinity (IC50 at -150 mV) for prenylamine in neuronal NaChs is 27.7 +- 1.3 uM, whereas the inactivated affinity (IC50 at -60 mV) is 0.75 +-0.02 uM¿ a 37-fold difference.

  • Calmodulin-1 (CALM1) ↗