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Application Notes
Sodium Pump
The Na/K-ATPase or Na-pump is the pharmacological receptor for cardiac glycosides, which are widely used in the treatment of heart failure. Furthermore, it is possibly also the physiological receptor for endogenous ouabain compounds.
GABAA Receptors
GABAA receptors are targets for many clinically important drugs like anxiolytics, anticonvulsants, anesthetics, sedatives, muscle relaxants, barbiturates, and benzodiazepines.
IKs Currents (KCNE1)
Mutations in these ion channels lead to disorders that may increase the risk of death from cardiac arrhythmia (long QT syndrome or LQTS) and Jervell and Lange-Nielsen syndrome, associated with congenital deafness.
nACh Receptors
nAChRs play a key role in the signal transmission between cells at the nerve/muscle synapses. Various studies demonstrated their involvement in high brain functions and in important neurodegenerative pathologies.
Application Notes
P2X Receptors
P2X receptors are nucleotide-gated cation channels playing important physiological and pathophysiological roles and are therefore promising targets for drug development.
Kv4.3 K+ Channels
Kv4.3 channels display rapidly inactivating K+ currents in brain and heart, which regulate neuronal firing and heart pacing. Altered Kv4.3 expression occurs under pathological conditions like heart failure.
Cardiac Na+ Channels
These voltage-gated channels initiate action potentials in excitable cells. Local anesthetics such as lidocaine block Na+ channels and have been used to manage cardiac arrhythmias, and non-specific drug binding to the SCN5A channel can alter normal cardiac rhythm.
hERG Channels
hERG channels critically contribute to cardiac repolarization. Drugs blocking these channels can lead to a prolongation of the action potential. Also, inhibition of hERG due to unwanted drug side effects means a significant risk factor for cardiac safety.