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Benzenesulfonamides act as open-channel blockers on K V 3.1 potassium channel
(2019-02-07)
K V 3.1 blockers can serve as modulators of the rate of action potential firing in neurons with high rates of firing such as those of the auditory system. We studied the effects of several bioisosteres of N-alkylbenzenes ...
Rational design and synthesis of selective blockers of the K2P channel TASK-3.
(2015)
K+ channels allow the selective transfer of K+ ions inside or outside of the cell. Within this
family we find K2P channels, with four transmembrane segments and two pore domains
per subunit to form a functional dimer. These ...
Rational design and biological activity of synthetic compounds as blockers of potassium channels TASK
(2017)
Potassium (K+) channels are part of one of the most abundant family of transmembrane proteins. K+ channels
allow the selective transfer of K+ ions inside or outside of the cell. Within this family we find K2P channels, ...
Structure-based study of TASK channels blockers
(2016)
Two-pore domain potassium (K2P) channels trigger the background K+
currents in mammalian cells. K2P channels are separated into six subfamilies
based on their structural and functional properties. The acid-sensitive ...
Understanding the structural mechanism of selective blockers of pH-gated K2P channels
(2018)
Two-‐pore
domain
potassium
(K2P)
channels
underlie
the
background
K+
currents
in
mammalian
cells.
They
can
be
segregated
into
six
subfamilies
based
on
their
structure
and
functional
properties.
The
acid-‐
sensitive
TAS ...
4-Chloro-3-nitro-N-butylbenzenesulfonamide acts on KV3.1 channels by an open-channel blocker mechanism
(2017-11-01)
The effects of 4-chloro-3-nitro-N-butylbenzenesulfonamide (SMD2) on KV3.1 channels, heterologous expressed in L-929 cells, were studied with the whole cell patch-clamp technique. SMD2 blocks KV3.1 in a reversible and ...
Intracellular Blockers Design Targeting TASK-3 Potassium Channels
(2015)
TASK-‐3
is
a
two-‐pore
domain
potassium
(K2P)
channel
highly
expressed
in
hippocampus,
cerebellum
and
cortex.
TASK-‐3
regulates
neurotransmitter
functions
as
well
as
the
mediating
effect
of
the
neurotransmitter
activa ...
Structure-based Discovery of New Two-Pore-Domain Potassium Channels TASK blockers
(2017)
The two-pore domain potassium (K2P) channel TASK-3 is a highly expressed
in hippocampus, cerebellum and cortical areas of the brain. Besides regulating
neurotransmitter functions, TASK-3 has an oncogenic potential and it ...
Molecular Modeling and Structural Analysis of TASK-1 Potassium Channel Interacting with the Blocker A1899
(2014)
Two-pore domain potassium (K2P) channels are expressed as functional dimers in the central
nervous system, cardiovascular system, genitourinary system and gastrointestinal system. They are
related with several pathologies ...
Potent nor-triterpenoid blockers of the voltage-gated potassium channel Kv1.3 from Spachea correae
(1998)
The isolation and structure elucidation of two novel nor-triterpenoid KV1.3 potassium channel blockers correolide and dehydrocorreolide from the Costa Rican tree Spachea correae are reported.
The first potent and selective ...