Inhibition of N-Type Calcium Channels by Fluorophenoxyanilide Derivatives
نویسندگان
چکیده
A set of fluorophenoxyanilides, designed to be simplified analogues of previously reported ω-conotoxin GVIA mimetics, were prepared and tested for N-type calcium channel inhibition in a SH-SY5Y neuroblastoma FLIPR assay. N-type or Cav2.2 channel is a validated target for the treatment of refractory chronic pain. Despite being significantly less complex than the originally designed mimetics, up to a seven-fold improvement in activity was observed.
منابع مشابه
Effects of L-type Calcium Channel Antagonists Verapamil and Diltiazem on fKv1.4ΔN Currents in Xenopus oocytes
The goal of this study was to determine the effects of the L-type calcium channel blockers verapamil and diltiazem on the currents of voltage-gated potassium channel (fKv1.4ΔN), an N-terminal-deleted mutant of the ferret Kv1.4 potassium channel. Measurements were made using a two electrode voltage clamp technique with channels expressed stably in Xenopus oocytes. The fKv1.4ΔN currents displayed...
متن کاملEffects of L-type Calcium Channel Antagonists Verapamil and Diltiazem on fKv1.4ΔN Currents in Xenopus oocytes
The goal of this study was to determine the effects of the L-type calcium channel blockers verapamil and diltiazem on the currents of voltage-gated potassium channel (fKv1.4ΔN), an N-terminal-deleted mutant of the ferret Kv1.4 potassium channel. Measurements were made using a two electrode voltage clamp technique with channels expressed stably in Xenopus oocytes. The fKv1.4ΔN currents displayed...
متن کاملInhibition of CatSper and Hv1 Channels and NOX5 Enzyme Affect Progesterone-Induced Increase of Intracellular Calcium Concentration and ROS Generation in Human Sperm
Background: Normal sperm function depends on appropriate intracellular calcium (Cai2+) and reactive oxygen species (ROS) levels. Calcium activates NADPH oxidase-5 (NOX5) that leads to ROS generation. The calcium channel of sperm (CatSper) is activated by progesterone and intracellular alkalization. Herein, the interactive role of CatSper, Hv1 channels, and NOX5 enzyme on Cai2+ and ROS generatio...
متن کاملInteraction between cannabinoid receptors and inhibition of L-type calcium channel on passive avoidance learning and memory in male rats
Introduction: There is currently a debate over the interaction between Ca2+ channels and cannabinoid system on learning and memory processing. In this study, we examined the effect of acute injection of cannabinoid agonist (Win- 55212-2) (Win) or antagonist (AM251), following chronic injection of verapamil, as a L-type Ca2+ channels blocker, on passive avoidance (PA) test in male Wistar rats...
متن کاملThe effects of eight weeks resistance training on α -1A protein of pre-synaptic P-Q-type calcium channels in FHL and soleus muscles of rats
The purpose of this study was to investigate the effects of 8 weeks resistance training (RT) on α -1A protein of pre-synaptic P-Q-type Calcium Channels in FHL and soleus muscles of rats. 16 male wistar rats provided from razi institute, randomly divided to 2 groups (Control-Sham; n=8 and Resistance Training; n= 8). Training group conducted 8 weeks (5 session/week) resistance program on spe...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره 13 شماره
صفحات -
تاریخ انتشار 2015