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Charybdotoxin (0):
Recent article
Charybdotoxin
Abstract
We investigated the effects of the chemokines IL-8 and RANTES on the activity of the Gardos channel (GC) of sickle red blood cells (SSRBCs). SSRBCs expressing the Duffy antigen receptor for chemokines (DARC) incubated under oxygenated conditions exhibit GC activation. The deoxygenation-stimulated K(...
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PMID: 20199879
PDF is available here.
PDF is available here.
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Abstract
We define distinctive differences in pharmacological properties of Slo3 and Slo1 currents, examine blockade in terms of distinct blocking models, and, for some blockers, use mutated constructs to evaluate determinants of block. Slo3 is resistant to block by the standard Slo1 blockers, iberiotoxin, c...
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PMID: 19934650
PDF is available here.
PDF is available here.
Abstract
Our result showed that alpha-ZAL (10(-10)-10(-5) M) induced both endothelium-dependent and -independent relaxation of rat thoracic aortas rings. The vasorelaxing effects of alpha-ZAL were dose-dependent whether the endothelium was intact or not. In endothelium-intact aortas rings, alpha-ZAL-induced...
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PMID: 19764345
PDF is available here.
PDF is available here.
Abstract
Our data indicate that the EDHF response in mice is caused by hydrogen peroxide, but not by P450 eicosanoids. Moreover, P450 eicosanoids are vasodilatory, largely through their ability to activate endothelial NO synthase (eNOS) and NO release....
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PMID: 18927469
PDF is available here.
PDF is available here.
Journal of Hypertension (26)12 2008
Abstract
L-Serine evoked a greater maximal fall in mean arterial pressure [L-serine vs. D-serine in Sprague-Dawley rats, mean +/- standard error of the mean values (mmHg): 30 +/- 3 vs. 20 +/- 5, P < 0.05; in control WKY rats: 46 +/- 3 vs. 30 +/- 4, P < 0.05; in NG nitro L-arginine methyl ester-treated WKY ra...
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PMID: 19062365
PDF is available here.
PDF is available here.
Journal of Molecular Biology (382)1 2008
Abstract
We report the electrophysiological and pharmacological properties of Kv1.2 and the paddle chimera channels in planar lipid bilayers. We demonstrate that Pichia yeast produce 'normally functioning' mammalian Kv channels with qualitatively similar features to the Shaker K(+) channel in the absence of...
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PMID: 18638484
PDF is available here.
PDF is available here.
Abstract
In diabetic coronary arteries, CHTX + APA did not change while LNA + INDO elevated the basal tension. PG-induced contractions were enhanced by CHTX + APA and by LNA + INDO in all the three groups of animals. CHTX + APA decreased the maximal relaxations to ACh in a partly insulin-dependent manner. LN...
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PMID: 18394024
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (283)35 2008
Structural basis for toxin resistance of beta4-associated calcium-activated potassium (BK) channels.
Abstract
We demonstrated that four mSlo turrets decentralized distally from the channel pore to provide a wide open conformation and that the mSlo and hbeta4 subunits together formed a "helmet" containing three basic residues (Lys-120, Arg-121, and Lys-125), which impeded the entry of charybdotoxin (ChTX) by...
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PMID: 18559348
PDF is available here.
PDF is available here.
Abstract
Alpha-calcitonin gene-related peptide dose dependently impaired angiotensin II-mediated vasoconstriction in human radial arteries, independent of nitric oxide and all potassium channels except the barium-sensitive Kir channel. Thus, calcitonin gene-related peptide is an endogenous inhibitor of angio...
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PMID: 18692643
PDF is available here.
PDF is available here.
Abstract
We characterized age-dependent ACh-hypotensive responses in vivo in 1-, 4-, 8-, and 16-wk-old rabbits and the contribution of THETAs and HEETAs to these responses. In anesthetized rabbits, blood pressure responses to ACh (4-4,000 ng/kg) were determined in the presence of vehicle or various inhibitor...
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PMID: 18456739
PDF is available here.
PDF is available here.
Abstract
We have determined the identity and functional properties of mouse beta3 variants. Whereas beta1, beta2, and beta4 subunits exhibit 83.2%, 95.3%, and 93.8% identity between mouse and human, the mouse beta3 subunit, excluding N-terminal splice variants, shares only 62.8% amino acid identity with its...
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PMID: 18591419
PDF is available here.
PDF is available here.
Abstract
These results indicate that hypertension induced by chronic ouabain treatment is accompanied by increased endothelial nitric oxide participation and impaired endothelium-dependent hyperpolarizing factor contribution in acetylcholine-induced relaxation. These effects might explain the lack of effect...
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PMID: 19043981
PDF is available here.
PDF is available here.
Abstract
We have systematically evaluated the signaling mechanisms underlying stimulated nitric oxide (NO) synthesis by estrogen (E2) and other vasoactive agents at the level of a single endothelium-derived cell. To do so, we have characterized and contrasted rapid E2-evoked NO synthesis with that of ATP usi...
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PMID: 18367584
PDF is available here.
PDF is available here.
Abstract
We investigated the effects of mibefradil on the membrane potential and ion channels in murine B cell lines, WEHI-231 and Bal-17. In the whole-cell patch clamp experiments, mibefradil blocked Kv and LK bg current with half inhibitory concentration (IC50), 1.9 and 2.3 microM, respectively. Interestin...
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PMID: 18188587
PDF is available here.
PDF is available here.
Abstract
We examined the effects of NT on GABAergic transmission and the involved cellular and signaling mechanisms of NT in the hippocampus. Application of NT dose-dependently increased the frequency of spontaneous inhibitory postsynaptic currents (sIPSCs) recorded from CA1 pyramidal neurons with no effects...
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PMID: 18337367
PDF is available here.
PDF is available here.
Abstract
Palmatine inhibited carbachol-induced Ca(2+)-activated Cl(-) secretion and the carbachol-induced increase of intracellular Ca(2+) concentration. Palmatine also inhibited cAMP-activated Cl(-) secretion induced by prostaglandin E(2) (PGE(2)) or forskolin. Palmatine prevented the elevation of intracell...
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PMID: 18204477
PDF is available here.
PDF is available here.
Abstract
We describe the synthesis of a chemically releasable, irreversible K(+) channel inhibitor and its iterative application to tally the number of beta-subunits in a KCNQ1/KCNE1 K(+) channel complex. Using this inhibitor in electrical recordings, we definitively show that there are two KCNE subunits in...
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PMID: 18223154
PDF is available here.
PDF is available here.
Abstract
These results suggest that the hindlimb vasodilator response to ACh has an initial L-NAME-resistant component mediated by the activation of K(Ca) channels and a sustained L-NAME-dependent component. The results with ebselen suggest that the L-NAME-resistant component of the depressor response involv...
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PMID: 18032519
PDF is available here.
PDF is available here.
Abstract
These results suggest that when diabetes and hypercholesterolaemia impair endothelium-dependent relaxation, due to a diminished contribution from NO, a compensatory contribution of EDHF to endothelium-dependent relaxation of the aorta is revealed. The attenuation of NO-mediated relaxation, at least...
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PMID: 17941894
PDF is available here.
PDF is available here.
Abstract
These results indicate that [Ca(2+)](i) can both activate and block IK(Ca) and SK(Ca) channels in endothelial cells, and that these channels regulate the resting membrane potential and intracellular calcium in native endothelium....
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PMID: 18195387
PDF is available here.
PDF is available here.
Abstract
We expressed wild-type BK channels and mutants E386N/E389N, D326N, E329Q, and D326N/E329Q channels on Xenopus laevis oocytes, and measured the expressed currents under patch clamp. Contribution of E329 to the conductance is negligible and single channel conductance of D326N/E329Q channels measured a...
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PMID: 18227273
PDF is available here.
PDF is available here.
Abstract
Modulation of afterhyperpolarization (AHP) represents an important mechanism by which excitability of a neuron can be regulated. In the leech brain, sensitization enhances excitability of the S-cell, an interneuron thought to play an important role in this form of nonassociative learning. This incre...
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PMID: 18046001
PDF is available here.
PDF is available here.
European Journal of Pharmacology (578)2-3 2008
Abstract
We investigated the effects of selective AT(2) receptor stimulation on myocardial contractility and lusitropy. Effects of selective AT(2) receptor activation were evaluated in rabbit right papillary muscles (n=96) by adding increasing concentrations of H-9395, an AT(2) receptor agonist, alone or in...
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PMID: 17961546
PDF is available here.
PDF is available here.
Vascular Pharmacology (49)4-6 2008
Abstract
Structural changes of PA in COPD could alter the response to hypoxia due to changes in BK(Ca) potassium channel distribution. Since BK(Ca) channels contribute to diminish vascular tone, their increased expression in remodeled PA might play a role in attenuating HPV....
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PMID: 18723123
PDF is available here.
PDF is available here.
Biochimica et Biophysica Acta (1777)7-8 2008
Abstract
We provide evidence for the potential presence of a potassium channel in skeletal muscle mitochondria. In isolated rat skeletal muscle mitochondria, Ca(2+) was able to depolarize the mitochondrial inner membrane and stimulate respiration in a strictly potassium-dependent manner. These potassium-spec...
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PMID: 18515063
PDF is available here.
PDF is available here.
Cell Calcium (42)6 2007
Abstract
We suggest a working model for the generation of oscillation based on a membrane oscillator where ion channels in both endothelial cells and SMC interact via a current running between the two cell types through myoendothelial gap junctions, which sets up a near anti-phase oscillation of [Ca2+]i in t...
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PMID: 17524481
PDF is available here.
PDF is available here.
Abstract
Elevated EET levels regulate Ca(2+) influx into endothelial cells and the subsequent activation of K(Ca) channels, via a cAMP/PKA-dependent mechanism that involves the intracellular translocation of Trp channels....
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PMID: 17872452
PDF is available here.
PDF is available here.
European Journal of Pharmacology (575)1-3 2007
Abstract
The administration of agmatine elicits an antidepressant-like effect in the mouse forced swimming test by a mechanism dependent on the inhibition of the NMDA receptors and the L-arginine-nitric oxide (NO) pathway. Since it has been reported that the NO can activate different types of potassium (K(+)...
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PMID: 17761162
PDF is available here.
PDF is available here.
Abstract
These results suggest that apamin-sensitive K(+) conductance and 4-AP-sensitive K(+) conductance may contribute to the resting membrane potential of circular smooth muscle cells. The early, rapid repolarization of slow waves appears to result from the opening of apamin-sensitive K(+) conductance. 4-...
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PMID: 17602242
PDF is available here.
PDF is available here.
Abstract
These results indicate that human mammary epithelial cells express multiple P2 receptor subtypes and that Ca(2+) mobilization evoked by P2Y receptor agonists stimulates Na(+) absorption by increasing the activity of Ca(2+)-activated K(+) channels located in the basolateral membrane....
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PMID: 17715387
PDF is available here.
PDF is available here.
Abstract
Anandamide caused a significant concentration-dependent vasorelaxation in rat aorta. This vasorelaxation was significantly inhibited by Pertussis toxin, by a non-CB1/non-CB2 cannabinoid receptor antagonist, by endothelial denudation, by inhibition of nitric oxide synthesis or inhibition of prostanoi...
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PMID: 17704831
PDF is available here.
PDF is available here.
Abstract
VSN16 relaxed mesenteric arteries in an endothelium-dependent manner. The vasorelaxation was antagonized by high concentrations of the classical cannabinoid antagonists, rimonabant and AM 251, as well as by O-1918, an antagonist at the abnormal-cannabidiol receptor but not at CB1 or CB2 receptors. I...
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PMID: 17891160
PDF is available here.
PDF is available here.
Abstract
These results suggest that STOCs in porcine coronary ASMCs are mediated by BK(Ca) channels. Extracellular Ca(2+) is essential for STOCs activity, while Ca(2+) entry through L-VDCCs has little effect on STOCs. Intracellular Ca(2+) release induced by RyRs is responsible for the regulation of STOCs, wh...
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PMID: 17879066
PDF is available here.
PDF is available here.
Abstract
We examined whether endothelium-dependent relaxation is sensitive to inhibitors of these channels (apamin and charybdotoxin) in resistance-sized vessels from human with EH. Subcutaneous gluteal biopsies were performed on 12 humans with EH and 12 matched control subjects. Resistance arteries were dis...
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PMID: 17508013
PDF is available here.
PDF is available here.
Abstract
The vasodilating efficacy of levosimendan and its relaxation mechanism differs between the arteries from males and females, which may have clinical consequences in the treatment of heart failure....
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PMID: 17703356
PDF is available here.
PDF is available here.
Abstract
Mice are useful animal models to study pathogenic mechanisms involved in pulmonary vascular disease. Altered expression and function of voltage-gated K(+) (K(V)) channels in pulmonary artery smooth muscle cells (PASMCs) have been implicated in the development of pulmonary arterial hypertension. K(V)...
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PMID: 17581857
PDF is available here.
PDF is available here.
Abstract
We report that intermediate-conductance Ca(2+)-activated K(+) (IKCa1) channels play a critical role in the development of EC. The expression of IKCa1 at both mRNA and protein levels in EC tissues was greatly increased than that in atypical hyperplasia and normal tissues. Treatment of EC cells with c...
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PMID: 17310992
PDF is available here.
PDF is available here.
Abstract
We determined the contributions of various endothelium-derived relaxing factors to control of basal vascular tone and endothelium-dependent vasodilation in the mouse hindlimb in vivo. Under anesthesia, catheters were placed in a carotid artery, jugular vein, and femoral artery (for local hindlimb ci...
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PMID: 17468338
PDF is available here.
PDF is available here.
Abstract
We propose that the BK(i) channels in small diameter DRG sensory neurons might play an important role in regulating nociceptive input to the central nervous system (CNS)....
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PMID: 17523149
PDF is available here.
PDF is available here.
Abstract
We show that PGE(2), by activating cAMP-dependent protein kinase A (PKA), enhanced ACh-induced, Ca(2+)-mediated current and changes in [Ca(2+)](i) in mucous cells. PGE(2) pretreatment sensitized ACh-induced I(SC) (DeltaI(SC)) by activating endoprostanoid (EP(2)) receptors. PKA inhibitors 14-22 amide...
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PMID: 17483294
PDF is available here.
PDF is available here.
Abstract
We investigated effects of TRAM-34 on microglial cells stimulated with lysophosphatidylcholine (LPC). LPC-induced increases in the intracellular Ca(2+) concentration of microglial cells were effectively reduced in the presence of TRAM-34. At a concentration of 1 microM, TRAM-34 inhibited LPC-induced...
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PMID: 17318643
PDF is available here.
PDF is available here.
Abstract
We used on-mitoplast and whole-mitoplast patches. Single BK channels had a conductance of 276+/-9 pS under symmetrical K(+) solutions, were Ca(2+)- and voltage-dependent and were inhibited by 0.1 microM charybdotoxin. In response to hypoxia, BK increased open probability, shifted its reversal potent...
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PMID: 17481584
PDF is available here.
PDF is available here.
Biochemistry (Washington) (46)18 2007
Abstract
We show that by minimizing the differences in binding free energy between selective and nonselective alpha-KTx we are able to identify all of the determinants of alpha-KTx specificity for calcium-activated versus voltage-dependent potassium channels. Because these determinants correspond to unique f...
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PMID: 17439246
PDF is available here.
PDF is available here.
Abstract
The human channel is potentiated by alcohol, although the presence of the beta1, and to a lesser extent, beta4-subunit, significantly reduced acute ethanol potentiation. Potentiation increased with concentration up to an asymptote, at which point potentiation decreased. The concentration of the asym...
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PMID: 17391339
PDF is available here.
PDF is available here.
Abstract
We have called "silent" myocytes and myocytes with STOCs have been called "active." STOCs recorded in active myocytes were voltage dependent and were inhibited by ryanodine, caffeine, and charybdotoxin. Forskolin was reported to increase STOCs frequency in myocytes isolated from resistance arteries....
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PMID: 17192282
PDF is available here.
PDF is available here.
Abstract
We developed a dual-chambered organ bath in which both membrane potential and force are independently determined in endothelium-intact and -denuded regions of a single annulus of artery. Hyperpolarizations and relaxations to endothelium-dependent vasodilators like bradykinin (BK) and substance P in...
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PMID: 17340126
PDF is available here.
PDF is available here.
Abstract
Endothelium dependent hyperpolarization of vascular smooth muscle contributes to the development of hyperdynamic circulation in ALF....
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PMID: 17354116
PDF is available here.
PDF is available here.
Abstract
We have previously shown that stimulation of acid secretion in parietal cells causes rapid initial cell shrinkage, followed by Na(+)/H(+) exchange-mediated regulatory volume increase (RVI). The factors leading to the initial cell shrinkage are unknown. We therefore monitored volume changes in cultur...
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PMID: 17095754
PDF is available here.
PDF is available here.
Abstract
We evaluated differences in gene expression patterns with low and high Ca(2+) (o) in an immortalized GnRH neuron line, GT1-7 cells. Mouse global oligonucleotide microarray was used to evaluate transcriptional differences among the genes regulated by elevated Ca(2+) (o). Our result identified two int...
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PMID: 17285630
PDF is available here.
PDF is available here.
Abstract
We used a panel prokaryote/eukaryote K+ channel chimeras to generate K+ channel arrays. Their behaviour in solution was compared with that when spotted on a nitrocellulose-supported film and their responses to selective high affinity ligands, including polypeptide toxins and TEA, were studied....
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PMID: 17198678
PDF is available here.
PDF is available here.
Journal of Physiology (579)Pt 1 2007
Abstract
We investigated the contribution of calcium-activated potassium channels (KCa) and endothelium-derived autacoids to CVD. Local delivery (1 microm micropipette tip; 500-2000 ms pulse) of acetylcholine (ACh) at the downstream end initiated a local increase in endothelial cell [Ca2+]i (Fura-PE3; Deltar...
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PMID: 17138602
PDF is available here.
PDF is available here.
Abstract
We investigate the signal transduction pathway involved in the activation of BK(Ca) channels by 11,12-EET and 11,12-EET stable analogs in rat mesenteric vascular smooth muscle cells. 11,12-EET and the 11,12-EET analogs, 11-nonyloxy-undec-8(Z)-enoic acid (11,12-ether-EET-8-ZE), 11-(9-hydroxy-nonyloxy...
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PMID: 17259072
PDF is available here.
PDF is available here.
Abstract
The transient receptor vanilloid-4 (TRPV4) is a mechanosensitive, swell-activated cation channel that is abundant in the renal distal tubules. Immunolocalization studies, however, present conflicting data as to whether TRPV4 is expressed along the apical and/or basolateral membranes. To disclose the...
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PMID: 16954339
PDF is available here.
PDF is available here.
Alcohol and Alcoholism (42)4 2007
Abstract
The purpose of this study was to investigate the role of K+ channels in duodenal dismotility induced by ethanol in vitro. The amplitude of spontaneous contractions was reduced by ethanol in longitudinal and circular muscle, while frequency did not change. Charybdotoxin antagonized ethanol-induced in...
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PMID: 17533163
PDF is available here.
PDF is available here.
Abstract
We showed that both agents also made the response significantly more transient in nature. These results show that inhibition of endothelial factor pathways can influence both the magnitude and dynamics of the response of isolated rat coronary arteries to flow....
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PMID: 17337908
PDF is available here.
PDF is available here.
Abstract
We tested if EDHF would regulate vascular tone in rat lungs of control and monocrotaline (MCT)-induced pulmonary hypertension. Inhibition of EDHF with a combination of K(Ca) blockers, charybdotoxin (50 nM) plus apamin (50 nM), increased baseline vascular tone in MCT-induced hypertensive lungs. Thaps...
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PMID: 17438361
PDF is available here.
PDF is available here.
Current Medicinal Chemistry (14)13 2007
Abstract
We will review the physiological properties, the structure activity relationships of the existing peptide and small molecule modulators and the therapeutic importance of the three small-conductance channels KCa2.1-KCa2.3 (a.k.a. SK1-SK3) and the intermediate-conductance channel KCa3.1 (a.k.a. IKCa1)...
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PMID: 17584055
PDF is available here.
PDF is available here.
Journal of Neurochemistry (100)2 2007
Abstract
We posit that aggregated, misfolded and oxidized alpha-synuclein (a major constituent of Lewy bodies), released or secreted from dying dopaminergic neurons, induces microglial ROS production that is regulated by ion channels and as such affects disease progression. To address this hypothesis, we per...
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PMID: 17241161
PDF is available here.
PDF is available here.
Toxicology (228)2-3 2006
Abstract
We have examined the effect of clotrimazole on the cells simultaneously treated with CdCl(2), PbCl(2), or HgCl(2) using rat thymocytes and a flow cytometer with fluorescent probes. The simultaneous application of clotrimazole and CdCl(2) significantly decreased cell viability, even though the concen...
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PMID: 17055140
PDF is available here.
PDF is available here.
Abstract
We hypothesized that a unique interaction between the Kv4.2 channel and a DPLP found in brain (DPPX-S) may remodel the channel's voltage-sensing domain. To test this hypothesis, we implemented a robust experimental system to measure Kv4.2 gating currents and study gating charge dynamics in the absen...
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PMID: 17130523
PDF is available here.
PDF is available here.