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NS 1619 activates KCNMA1. 35 / 36
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"Surprisingly, BK channel activator NS1619 (30muM) also increases the basal tension and amplitude in intact bladder strips."
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"In addition, pretreatment with BK channel activator NS-1619 or blocker iberiotoxin and PKC inhibitor Bis1 did not affect H 2 O 2 -elicited increases of the basal tension and amplitude."
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"NS1619, niflumic acid, and phloretin were tested by using excised inside-out membrane patches from HEK 293 cells and were found to increase the activity of hSlo BK channels and produce a leftward shift in the G/Gmax-versus-voltage relationship of these channels."
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"Furthermore, other lysosome acidifying agents, including the TRPML1 agonist ML-SA1 and the BK channel activator NS1619, also blocked the entry of pseudo-SARS-CoV-2."
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"The BK channel activation by NS 1619 appears to be independ- ent of ligand receptors, G-proteins or channel phos- phorylation."
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"The ATP activated K+ current was inhibited by iberiotoxin (200 nM), and it was potentiated by the BK channel activator NS-1619 (30 microM)."
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"To explore the role of BK channels in regulation of apoptosis in human ovarian cancer cells, the effects of the specific BK channel activator NS1619 on induction of apoptosis in A2780 cells were observed."
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"As a complementary approach we then examined the efficacy of a specific BK channel activator NS1619 in restoring the precision of pacemaking."
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"Recent observations have shown that some BK channel activators, such as NS1619 and BMS191011, attenuate renal fibrosis and promote proper kidney function in animal models (Yan et al., 2022)."
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"It has also been reported that NS1619 activates Slo1 by functionally interacting with the S6/RCK linker connecting the transmembrane S6 segment with the cytosolic RCK1 domain [XREF_BIBR]."
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"NS19504 is a novel BK channel activator having a higher specificity than the commonly used BK channel activator NS1619, NS19504, which does not activate the small-conductance potassium channel (IK channels) while activating the BK channels (Nausch et al., 2014; Catacuzzeno et al., 2015)."
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"The inhibitory effects of MA on voltage-gated sodium currents need to be further clarified in the future.The inhibitory effect of MA on I K and BK channel activity mimicked that of the selective BK ch[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"From a pharmaco-genomic perspective, this is the first study to show that cardioprotection in the intact heart by the putative SLO1 activators NS1619 and NS11021 actually requires the Slo1 gene product (XREF_FIG and XREF_FIG)."
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"Unfortunately this can not be tested experimentally using Slo1 -/- mice, because post-IR Slo1 -/- hearts treated with NS1619 are incompetent at the contractile level (XREF_FIG and XREF_FIG), so they can not respond to nicotine anyway, regardless of their neuronal status."
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"Application of the selective BK channel activator NS-1619 (1 muM; Oelsen et al., 1994) also mimicked the actions of insulin, causing 50 +/-6.4% inhibition of the oscillatory activity (n = 31 cells / n[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Similarly, addition of the selective BK channel activator NS-1619 inhibited the spontaneous Ca 2+ oscillations in a readily reversible manner."
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"Iberiotoxin (50 nM), a selective blocker of large-conductance, voltage gated Ca2 +-activated K+ (K (Ca)) (BK) channel, dramatically increased both contraction amplitude and frequency whereas NS-1619 (30 microM), which increases BK channel activity, decreased them."
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"Furthermore, we found that intrathecal administration of the specific BK channel activator NS1619 had no significant effect on nociceptive thresholds in control rats but dose dependently attenuated mechanical allodynia and hyperalgesia in nerve-ligated rats."
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"Furthermore , in cell lines HK-2 , NRK49 , and NRK-52E , BK channel activation by NS1619 led to increased caveolae formation and facilitated localization of TGF-beta receptors in the microdomains of lipid rafts ."
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"Leptin effects were mimicked by the synthetic BK channel activator NS1619 (1,3-dihydro-1-[2-hydroxy-5-(trifluoromethyl) phenyl]-5-(trifluoromethyl)-2H-benzimidazol-2-one), and inhibited by the BK channel inhibitors, iberiotoxin and charybdotoxin."
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"Thus, the primary effect of the BK channel activator NS1619 was to increase the P o or channel gating."
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"Another salient finding of our study is that intrathecal injection of the specific BK channel activator NS1619 dose dependently reduced mechanical allodynia and hyperalgesia in nerve-ligated rats."
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"Physiological experiments further support the origin of mitoBK (Ca) as a Kcnma1 product because NS1619 mediated cardioprotection was absent in Kcnma1 knockout mice."
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"In pressurized, myogenic (60 mmHg) control arteries transfected with scrambled siRNA, the BK channel activator NS1619 stimulated a mean vasodilation of ~ 34.7 mum, and the specific BK channel inhibitor, iberiotoxin, produced a mean constriction of ~ 25.5 mum (XREF_FIG)."
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"In Fura-2 imaging, the BK channel activator NS1619 elevated resting [Ca 2+ ] i in both RPMs and TGPMs."
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"Both native and recombinant BK channel activities are enhanced by the BK channel activator NS1619 and inhibited by the selective blocker paxilline [XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR]."
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"The relaxation to BK channel activator NS1619 was attenuated in the coronary artery with adenovirus transfected MuRF1."
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"The human DSM single BK channel currents exhibited properties consistent with those reported for these channels in other systems : the mean single-channel conductance of more than 200 pS, P o highly dependent on the voltage and intracellular Ca 2+ concentration, enhancement of single-channel activity by the BK channel activator NS1619 and blockade by the selective BK channel inhibitor paxilline."
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"Both BK channel activators, such as the benzimidazolone NS1619 [25], and inhibitors such as paxilline are available [26]."
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"They further demonstrated that mitochondrial uptake of K + was blunted by charybdotoxin and iberiotoxin and accelerated by the BK channel activator NS1619."
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"The ability of leptin to modulate this activity requires activation of BK, but not K (ATP), channels as the effects of leptin were mimicked by the BK channel activator NS-1619, and inhibited by the BK channel inhibitors, iberiotoxin and charybdotoxin."
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"Indeed Stowe et al. found that pre-treatment with the BK channel activation by NS1619 in isolated perfused guinea pig hearts attenuated mitochondrial calcium accumulation following an ischemic event."
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"BK channel activation by NS-1619 is partially mediated by intracellular Ca2+ release in smooth muscle cells of porcine coronary artery."
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"BK channel activation by NS1619 reveals key binding interactions, offering insights for designing targeted therapeutic agents."
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"Neither the BK channel blocker iberiotoxin (100nM) nor the BK channel activator NS-1619 (30muM) affected the H 2 O 2 -induced augmentation of spontaneous contractions (XREF_FIG, XREF_TABLE)."
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