ZD7288 是一种选择性超极化激活的环核苷酸门控通道阻滞剂，可抑制海马突触可塑性。

ZD7288, a selective hyperpolarization-activated cyclic nucleotide-gated channel blocker, inhibits hippocampal synaptic plasticity.

ZD7288 attenuated glutamate-induced rises in [Ca(2+)]i in a concentration-dependent manner and reversed 8-Br-cAMP-mediated facilitation of these glutamate-induced [Ca(2+)]i rises.?ZD7288 inhibits hippocampal synaptic plasticity both glutamate release and resultant [Ca(2+)]i increases in rat hippocampal neurons[1].

Cultured hippocampal neurons were incubated with 1 μM Fura-2 acetoxy-methylol ester for 30 minutes at 37°C, washed three times with artificial cerebrospinal fluid (containing 140 mM NaCl, 5 mM KCl, 2 mM CaCl2, 1 mM MgCl2, 10 mM glucose and 10 mM hydroxyethyl piperazine ethanesulfonic acid, pH 7.3), and then incubated at room temperature in the dark for 30 minutes.?Fura-2 fluorescence was observed by a Ratio Vision digital fluorescence microscopy system.?Fluorescence signals were evoked by 340 and 380 nm excitation wavelengths and collected at 510 nm by TILLvisION 4.0 software.?The 340:380 nm fluorescence ratio was used to represent [Ca2+]i.?Peak calcium change was represented as the percentage increase from baseline.?Neurons were incubated in ZD7288 (25, 50 or 100 μM) or 8-Br-cAMP (5 or 50 μM) for 15 minutes prior to stimulation with 50 μM glutamate.?All experiments were repeated in triplicate, using different batches of cells across 4–5 dishes[1].

133059-99-1

C15H21ClN4

292.81

N-乙基-1,6-二氢-1,2-二甲基-6-(甲基亚氨基)-N-苯基-4-嘧啶胺盐酸盐;ICI D7288

H2O:50 mg/mL (170.76 mM)
DMSO:50 mg/mL (170.76 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years