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Allosteric Block of KCa2 Channels by Apamin*
TLDR
This multidisciplinary approach suggested that apamin does not behave as a classical pore blocker but blocks using an allosteric mechanism that is consistent with observed differences between binding affinity and potency of block. Expand
Synthesis and radioligand binding studies of methoxylated 1,2,3,4-tetrahydroisoquinolinium derivatives as ligands of the apamin-sensitive Ca2+-activated K+ channels.
TLDR
The 6,7,8-trimethoxy derivative 3f is the first tertiary amine in the series to possess an affinity close to that of N- methyl-laudanosine and N-methyl-noscapine, and electrophysiological studies show that the most effective compound 4f blocks the apamin-sensitive afterhyperpolarization in rat dopaminergic neurons. Expand
SK channel blockade promotes burst firing in dorsal raphe serotonergic neurons
TLDR
The results suggest that SK channel blockade promotes bursting activity in 5‐HT neurons via a direct action, and an input which is present only in vivo seems to be important for the induction of this firing pattern in these cells. Expand
Synthesis and radioligand binding studies of bis-isoquinolinium derivatives as small conductance Ca(2+)-activated K(+) channel blockers.
TLDR
The original bis-isoquinolinium derivatives were synthezised and evaluated using binding studies, electrophysiology, and molecular modeling and demonstrate the blocking potential of the apamin-sensitive after-hyperpolarization. Expand
Ion‐Channel Modulators: More Diversity Than Previously Thought
TLDR
Recent evidence suggests that in several ion channels, the region around the outer mouth of the pore is rich in binding sites and could be exploited therapeutically and should be adapted to define these various actions. Expand
The sigma agonist 1,3-di-o-tolyl-guanidine directly blocks SK channels in dopaminergic neurons and in cell lines.
TLDR
1,3-di-o-tolyl-guanidine (DTG) inhibited the mAHP in a concentration-dependent manner, and it is concluded that DTG directly blocks SK channels. Expand
Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca(2+)-activated K(+) channel blockers.
TLDR
AG525E1 is the discovery of a chiral bis-tertiary amine with SK blocking properties from chemical modulation of laudanosine, which has an affinity for SK channels and can reach central SK targets. Expand
Inhibition of KCa2.2 and KCa2.3 channel currents by protonation of outer pore histidine residues
TLDR
Mutagenesis revealed that local interactions involving the outer turret histidine residues are crucial to enable high conductance openings, with protonation inhibiting current by changing pore shape. Expand
New pyridobenzoxazepine derivatives derived from 5-(4-methylpiperazin-1-yl)-8-chloro-pyrido[2,3-b][1,5]benzoxazepine (JL13): chemical synthesis and pharmacological evaluation.
TLDR
Results encourage further development of 2 as a novel second-generation antipsychotic agent and present the most promising in vitro binding profile in terms of multireceptor target strategy. Expand
The interactions of apamin and tetraethylammonium are differentially affected by single mutations in the pore mouth of small conductance calcium-activated potassium (SK) channels.
TLDR
Valine residues in the pore region of SK channels show that the three-dimensional structure of the SK tetramers can be disorganized in the outer pore regions leading to reduced interaction of apamin with its target. Expand
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