Drug induced liver injury (DILI) and tissue discoloration led to the recent discontinuation of the therapeutic use of the closely related drugs flupirtine and retigabine, respectively. Experience gained with these drugs strongly suggests that heterodimer, voltage‐gated potassium channels 2 and 3 (KV2/3) are valid targets for effective treatment of pain and epilepsy. Because the adverse effects are not related to the mechanism of action, it appears promising to investigate chemical modifications of these clinically validated, drug‐like leads. In the present retro metabolic drug design study, a series of 44 compounds were synthesized and characterized with regards to KV7.2/3 opening activity and efficacy. The most active compounds displays e...
Flupirtine (Flu), a triaminopyridine derivative, is a centrally acting, non-opiate analgesic agent. ...
Copyright © 2012 Sheng-Nan Wu et al. This is an open access article distributed under the Creative C...
Background: Most chemotherapeutic agents have serious side effects that can lead to dose reduction o...
Abstract The KV7 potassium channel openers flupirtine and retigabine have been valuable options in ...
Neuronal Kv7 channels represent important pharmacological targets for hyperexcitability disorders in...
Kv7 channels, especially Kv7.2 (KCNQ2) and Kv7.3 (KCNQ3), are key determinants for membrane excitabi...
The Kv7 K+ channels play a fundamental role in controlling neuronal excitability, representing an at...
Flupirtine is the first representative in a class of triaminopyridines that exhibits pharmacological...
Flupirtine is a centrally acting, non-opioid analgesic that is available in a number of European cou...
Epilepsy is among the most prevalent neurological disorders, affecting approximately 1% of the human...
Background: Flupirtine is an analgesic with muscle-relaxing properties that activates Kv7 potassium ...
Kv7 K+ channels play a pivotal role in controlling neuronal excitability, representing attractive p...
Background: The Kv7 (KCNQ) subfamily of voltage-gated potassium channels consists of 5 members (Kv7....
Kv7.2/7.3 potassium channels represent an attractive pharmacological targets for the treatment of d...
Flupirtine is a non-opioid, centrally acting analgesic which is marketed for oral and per rectal use...
Flupirtine (Flu), a triaminopyridine derivative, is a centrally acting, non-opiate analgesic agent. ...
Copyright © 2012 Sheng-Nan Wu et al. This is an open access article distributed under the Creative C...
Background: Most chemotherapeutic agents have serious side effects that can lead to dose reduction o...
Abstract The KV7 potassium channel openers flupirtine and retigabine have been valuable options in ...
Neuronal Kv7 channels represent important pharmacological targets for hyperexcitability disorders in...
Kv7 channels, especially Kv7.2 (KCNQ2) and Kv7.3 (KCNQ3), are key determinants for membrane excitabi...
The Kv7 K+ channels play a fundamental role in controlling neuronal excitability, representing an at...
Flupirtine is the first representative in a class of triaminopyridines that exhibits pharmacological...
Flupirtine is a centrally acting, non-opioid analgesic that is available in a number of European cou...
Epilepsy is among the most prevalent neurological disorders, affecting approximately 1% of the human...
Background: Flupirtine is an analgesic with muscle-relaxing properties that activates Kv7 potassium ...
Kv7 K+ channels play a pivotal role in controlling neuronal excitability, representing attractive p...
Background: The Kv7 (KCNQ) subfamily of voltage-gated potassium channels consists of 5 members (Kv7....
Kv7.2/7.3 potassium channels represent an attractive pharmacological targets for the treatment of d...
Flupirtine is a non-opioid, centrally acting analgesic which is marketed for oral and per rectal use...
Flupirtine (Flu), a triaminopyridine derivative, is a centrally acting, non-opiate analgesic agent. ...
Copyright © 2012 Sheng-Nan Wu et al. This is an open access article distributed under the Creative C...
Background: Most chemotherapeutic agents have serious side effects that can lead to dose reduction o...