SKA-111, a Positive KCa Channel Gating Modulator with Selectivity for KCa3.1
نویسندگان
چکیده
منابع مشابه
New Positive Ca 2 1 - Activated K 1 Channel Gating Modulators with Selectivity for KCa 3 . 1 s
Small-conductance (KCa2) and intermediate-conductance (KCa3.1) calcium-activated K channels are voltage-independent and share a common calcium/calmodulin-mediated gating mechanism. Existing positive gating modulators like EBIO, NS309, or SKA-31 activate both KCa2 and KCa3.1 channels with similar potency or, as in the case of CyPPA and NS13001, selectively activate KCa2.2 and KCa2.3 channels. We...
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Temporal patterns of spiking often convey behaviorally relevant information. Various synaptic mechanisms and intrinsic membrane properties can influence neuronal selectivity to temporal patterns of input. However, little is known about how synaptic mechanisms and intrinsic properties together determine the temporal selectivity of neuronal output. We tackled this question by recording from midbr...
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Aquaporin 4 (AQP4) is the predominant water channel in the mammalian brain and is mainly expressed in the perivascular glial endfeet at the brain-blood interface. AQP4 has been described as an important entry and exit site for water during formation of brain edema and regulation of AQP4 is therefore of therapeutic interest. Phosphorylation of some aquaporins has been proposed to regulate their ...
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Similar to GABAA receptor-channels the calciummediated gating of the small-conductance KCa2 and the intermediate-conductance KCa3.1 channels can be positively or negatively modulated by small molecule drugs, which, in analogy to the GABA field, have been termed positive (PAM) or negative allosteric modulators. While positive gating modulators like EBIO, NS309, SKA-31 and SKA-121 shift the calci...
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Large conductance, voltageand Ca 2 -activated K (BK Ca ) channels regulate blood vessel tone, synaptic transmission, and hearing owing to dual activation by membrane depolarization and intracellular Ca 2 . Similar to an archeon Ca 2 -activated K channel, MthK, each of four subunits of BK Ca may contain two cytosolic RCK domains and eight of which may form a gating ring. The structure of the Mth...
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ژورنال
عنوان ژورنال: Biophysical Journal
سال: 2014
ISSN: 0006-3495
DOI: 10.1016/j.bpj.2013.11.3556