Kv7 piperidinylmethyl pyrimidine amide as a potassium channel openerThe present invention, pharmaceutical compositions comprising a pharmaceutically acceptable salt thereof or a compound salt thereof, of formula (I) or a pharmaceutically acceptable compound of formula (I) as is described herein , in ...
The panâKv7 (KCNQ) Channel Opener Retigabine Inhibits Striatal Excitability by Direct Action on Striatal Neurons In VivoKv7/KCNQ channelsStriatumRetigabineHaloperidolExcitabilityc-Fos expressionp>Central Kv7 (KCNQ) channels are voltage-dependent potassium channels composed of different combinations ...
7.5 voltage-gated potassium channel(kcnq2 – 5)opener,retigabine,reduces capsaicin-induced visceral pain in mice.)”《神经科学通信(neurosci.lett)》.413(2007)159 – 162;mosad a.ghareeb等人,“艳山姜(姜科)叶提取物的多酚类成分及其体内抗炎、抗伤害和退热活性的hplc-esi-ms/ms分析(hplc-esi-ms/ms p...
”《药理学、生物化学和行为学 (Pharmacol.Biochem.Behav.)》.101(2012)320–328;Kazufumi Hirano等人,“Kv7.2‑7.5电 压门控钾离子通道(KCNQ2‑5)开放剂,瑞替加滨,减少辣椒素诱导的小鼠内脏疼痛(Kv7.2– 7.5 voltage‑gated potassium channel(KCNQ2–5)opener,retigabine,reduces capsaicin‑induced ...
Intriguingly, many of the synaptic proteins with downregulated PTMs corresponded to potassium channel subunits or their related proteins; these included Kv1.4, Kv2.1, Kv3.1, Kv3.3, Kv7.2, and Kv7.3 (Fig. 5f). Of the Kv channels, Kv7.2 and Kv7.3 were particularly interesting because they ...
In this paper, we summarized the activation characteristics, activation sites and clinical application of Kv7/KCNQ channel openers.Keywords Kv7 channel; KCNQ channel; opener; seizure; pain 电压门控型钾离子通道Kv7家族由KCNQ基因编码。Kv7/KCNQ电压门控钾通道在控制细胞兴奋性中发挥着重要作用[1]。针对Kv7...
The M-channel opener, retigabine, had opposite effects. The higher the [K+]o, the greater the effects of XE991 and retigabine. Similar pharmacological modulation of EPSPs recorded intracellularly from CA1 pyramidal neurons, while blocking postsynaptic K+ channels with intracellular Cs+, confirmed ...
a selective KCNQ/M channel opener, not only inhibited the bone cancerinduced hyperexcitability of dorsal horn WDR neurons, but also alleviated mechanical allodynia and thermal hyperalgesia in the bone cancer rats, while all of these effects of retigabine could be blocked by KCNQ/M-channel antagonist...
A specific KCNQ/M-channel opener, retigabine, exerts an analgesic action in several models of neuropathic pain, inflammatory pain, and visceral pain, and these effects of retigabine can be reversed by KCNQ/M channel blocker such as linopirdine or XE-991. These findings suggest that the KCNQ/...
The identification of the M-current as a main culprit in SENP2 deficiency is supported by the observations that both seizures and AV blocks can be prevented by the Kv7 channel opener retigabine. Our findings unravel an important physiological role of SENP2 in regulation of the M-current and ...