Abstract
(S)-N-[1-(3-Morpholin-4-ylphenyl)ethyl]-3-phenylacrylamide (2) was synthesized as an orally bioavailable KCNQ2 potassium channel opener. In a rat model of migraine, 2 demonstrated significant oral activity in reducing the total number of cortical spreading depressions induced by potassium chloride.
MeSH terms
-
Acrylamides / chemical synthesis*
-
Acrylamides / chemistry
-
Acrylamides / pharmacology
-
Administration, Oral
-
Animals
-
Biological Availability
-
Cell Line
-
Cerebral Cortex / drug effects*
-
Cerebral Cortex / physiopathology
-
Disease Models, Animal
-
Dogs
-
Humans
-
Ion Channel Gating
-
KCNQ2 Potassium Channel
-
Migraine Disorders / metabolism
-
Migraine Disorders / physiopathology*
-
Morpholines / chemical synthesis*
-
Morpholines / chemistry
-
Morpholines / pharmacology
-
Oocytes / drug effects
-
Oocytes / physiology
-
Patch-Clamp Techniques
-
Potassium Channels / drug effects*
-
Potassium Channels / physiology
-
Potassium Channels, Voltage-Gated
-
Rats
-
Rats, Sprague-Dawley
-
Stereoisomerism
-
Structure-Activity Relationship
-
Xenopus laevis
Substances
-
Acrylamides
-
KCNQ2 Potassium Channel
-
KCNQ2 protein, human
-
Kcnq2 protein, rat
-
Morpholines
-
N-(1-(3-morpholin-4-ylphenyl)ethyl)-3-phenylacrylamide
-
Potassium Channels
-
Potassium Channels, Voltage-Gated