IndraLab

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Spadin inhibits KCNK2. 20 / 20
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"Although spadin may completely inactivate TREK-1 through channel blockage and internalization to exert antidepressant effects, the inhibitor is less specific than gene knockout or shRNA-mediated knockdown of TREK-1 expression."
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"Moreover, spadin also inhibited a TREK1-like component of I in thalamocortical neurons (Bista et al., 2012) and a TREK1-like current induced by RIL in mouse nodose ganglion neurons (Fernández-Fernández et al., 2018)."
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"Among these inhibitors, spadin, a peptide, has been reported to selectively inhibit TREK-1 over TREK-2 or other K2P channels [70,72,73]."
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"Studies have shown that the activity of the TREK-1 channel in mice may undergo significant changes after pre-exposuring to spadin, which is likely achieved through a deformation mechanism, thus disrupting the subsequent activation of TREK-1 current by AA Ma and Lewis (2020)."
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"This hypothesis was validated by the discovery of spadin, that is a sortilin derived peptide and that specifically blocks TREK-1 channels [28], [30]."
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"Other drugs under clinical trial include spadin and its analogs, which specifically block TREK-1 (Djillani et al., 2017), and ezogabine (retigabine), a K 7 channel modulator (Friedman et al., 2016)."
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"Recently, we demonstrated that TREK-1 channels are inhibited by spadin, a peptide that represents a new concept in antidepressant drug design [28]."
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"Here, we showed that spadin blocked TREK-1 current exactly as it did for the transiently transfected TREK-1 channels (Figure 4A–C)."
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"To address the question whether pharmacological blockade of TREK-1 by spadin affects 5-HT neurotransmission, mice were given a 10 μM dose of spadin as an i.p injection and the unitary extracellular ac[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Taken together, these data confirmed that the newly generated neurons by spadin are indeed functional and able to interact within the neuronal complex network.Despite the high homology in structure, f[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Meanwhile, spadin reduces acid induced activity of TREK-1 and TREK-2 tandem heterodimeric channels [XREF_BIBR]."
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"Electrophysiological studies show that spadin efficiently blocks the TREK-1 activity in COS-7 cells, cultured pyramidal neurons, as well as CA3 hippocampal neurons in brain slices of wild-type mice and not in kcnk2 -/- mice, suggesting a specific effect of spadin on the TREK-1 channel."
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"Direct inhibition of TREK-1 by spadin may also contribute to enhanced 5-HT neuron excitability."
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"Mini-spadin and spadin slightly blocked TREK-1 activity without prior AA activation."
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"Moreover, spadin blocks TREK-1 with higher affinity, IC 50 ~ 40-60 nM vs. IC 50 ~ 6 muM for the most used SSRI fluoxetine."
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"In a previous study, pharmacological inhibition of TREK-1 by spadin increased the proportion of mature spines without affecting spine densities in cultured cortical neurons [24]."
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"The difference in findings between the two independent studies is likely due to the varied approaches that were used for TREK-1 manipulation; the genetic knockout was used in our study, whereas in the study reported by others, spadin was used to pharmacologically inhibit TREK-1 in cultured cortical neurons."
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"Recently, spadin, a sortilin-derived peptide, has been found to block TREK-1 with a high affinity and specificity, and suggested to inhibit approximately 60% of the TREK-1 current stimulated by arachidonic acid [22]."
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"It should be noted that spadin blocks homomeric TREK-1 and heteromeric TREK-1 and TREK-2 channels but not homomeric TREK-2 channels (Moha Ou Maati et al. 2012)."
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"These findings illustrate that blockage of TREK-1 by spadin leads to the repression of A1-like reactive astrocytes in a rat model of MDD via the NF-κB signaling pathway."
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