apamin definition: Noun (uncountable) 1. (biochemistry) A neurotoxin originally isolated from Apis mellifera, the Western honey bee....
Apamin-sensitive, non-nitric oxide (NO) endothelium-dependent relaxations to bradykinin in the bovine isolated coronary artery: no role for cytochrome P450 and
The results show that SK2 subunits are necessary for the apamin-sensitive component of the ImAHP. In SK1 Δ/Δ or SK3 T/T(dox) mice, the apamin-sensitive component of the ImAHP was not significantly different from control, there were no significant changes in the levels of SK2 mRNA, and SK2 protein levels were not obviously upregulated, suggesting that only SK2 is necessary for the apamin-sensitive component of the ImAHP. This is consistent with previous suggestions based on the pharmacological profile of the current and the high specificity of apamin (Stocker et al., 1999; Sailer et al., 2002).. In heterologous expression studies, mouse and rat SK1 subunits, different from human SK1 subunits, do not form functional homomeric channels in the plasma membrane, but they are incorporated into heteromeric channels with SK2 or SK3 subunits (Benton et al., 2003; Monaghan et al., 2003). These data suggest that SK1 subunits may contribute to the number of functional SK2-containing channels, although the ...
UCL 1530: blocks actions mediated by the small conductance, apamin-sensitive Ca2+-activated K+ channels in cultured sympathetic neurones and isolated hepatocytes; structure given
Apamin is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom). Dry bee venom consists of 2-3% of apamin. Apamin selectively blocks SK channels, a type of Ca2+-activated K+ channel expressed in the central nervous system. Toxicity is caused by only a few amino acids, these are cysteine1, lysine4, arginine13, arginine14 and histidine18. These amino acids are involved in the binding of apamin to the Ca2+-activated K+ channel. Due to its specificity for SK channels, apamin is used as a drug in biomedical research to study the electrical properties of SK channels and their role in the afterhyperpolarizations occurring immediately following an action potential. The first symptoms of apitoxin (bee venom), that are now thought to be caused by apamin, were described back in 1936 by Hahn and Leditschke. Apamin was first isolated by Habermann in 1965 from Apis mellifera, the Western honey bee. Apamin was named after this bee. Bee venom contains many other compounds, like histamine, ...
The purpose of the present study was to examine how apamin interacts with the three cloned subtypes of small-conductance Ca2+-activated K+ channels (hSK1, rSK2 and rSK3). Expression of the SK channel subtypes in Xenopus laevis oocytes resulted in large outward currents (0.5-5 microA) after direct in …
Drosophila nociceptive neurons convert high-intensity stimuli into characteristic fluctuations of firing rates, quiescent periods of which are regulated by hyperpolarization through small conductance Ca2+-activated K+ channels.
Having left the field a while ago, for reasons that I wont go into, suffice it to say I no longer have access to the relevant literature, Ive been drawn quite by accident to consider the recent proposal that the inhibitory junction potential (IJP) recorded in the gastrointestinal smooth muscle has its origin in cells…
Izabela Rutkowska-Wlodarczyk, M. Isabel Aller, Sergio Valbuena, Jean-Charles Bologna, Laurent Prézeau, et al.. (see pages 5171-5179). Kainate receptors (KARs) have the structure of ionotropic glutamate receptors, but unlike AMPA and NMDA receptors, KARs can activate metabotropic signaling as well as passing ionic current. Several metabotropic effects of KARs have been demonstrated, including inhibition of voltage-sensitive calcium channels, inhibition of glutamate and GABA release, and inhibition of the slow afterhyperpolarization current (IAHP). All these effects are blocked by pertussis toxin and involve phospholipase C, suggesting they are mediated by Go proteins, but how KARs activate G-proteins has remained an open question.. To answer this question, Rutkowska-Wlodarczyk et al. performed a proteomic analysis on mouse brain homogenates and identified proteins that interacted with the intracellular C-terminal portion of GluK1b, a KAR subunit. They found 22 proteins that specifically ...
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इस पाक की महिमा का वर्णन भगवान महादेवजी ने पार्वतीजी के समक्ष किया था । नारदजी ने इसे ब्रम्हाजी के श्रीमुख से सुना व अश्विनीकुमारों ने इस पाक का निर्माण किया था । इसके सेवन से बल,बुद्धि,स्मृति,उत्तम वाणी,सौंन्दर्य,सुकुमारता तथा सौभाग्य की प्राप्ति होती है । माताओं के लिए यह खास वरदानस्वरूप है प्रसूति के बाद सेवन से दूध खुलकर आता है तथा संभावित कई व्याधियों से रक्षा होती है ।सर्दियों ...
TY - JOUR. T1 - The contribution of d-tubocurarine-sensitive and Apamin-sensitive K-channels to EDHF-mediated Relaxation of Mesenteric Arteries from eNOS-/- Mice. AU - Chen, Xiaoliang. AU - Li, Yang. AU - Hollenberg, Morley. AU - Triggle, Christopher. AU - Ding, Hong. PY - 2012/5. Y1 - 2012/5. N2 - The nature of the potassium channels involved in determining endothelium-derived hyperpolarizing factor-mediated relaxation was investigated in first-order small mesenteric arteries from male endothelial nitric oxide synthase (eNOS-/-)-knockout and control (+/+) mice. Acetylcholine-induced endothelium-dependent relaxation of small mesenteric arteries of eNOS-/- was resistant to N-nitro-L-arginine and indomethacin and the guanylyl cyclase inhibitor, 1H-(1,2,4) oxadiazolo (4,3-a) quinoxalin-1-one. Apamin and the combination of apamin and iberiotoxin or apamin and charybdotoxin induced a transient endothelium-dependent contraction of small mesenteric arteries from both eNOS-/- and +/+ mice. ...
TY - JOUR. T1 - The effects of apamin in rats with pretrigeminal or high spinal transsection of the central nervous system. AU - Janicki, P.. AU - Gumulka, S. W.. AU - Krzaścik, P.. AU - Habermann, E.. PY - 1985. Y1 - 1985. N2 - P. Janicki, S.W. Gumulka, P. Krzaścik and E. Habermann. The effects of apamin in rats with pretrigeminal or high spinal transsection of the central nervous system. Toxicon 23, 993-996, 1985. - Rats were injected in one lateral cerebral ventricle (i.c.v.) with apamin (100 ng per animal). The resulting desynchronisation pattern in the electrocorticogram (ECoG) and the symptoms of poisoning were monitored before and after transsection at different levels, and following morphine. Apamin acts primarily on the brain stem and spinal cord, i.e. structures possessing a sensory input, and then indirectly on the higher integrating systems. There is no general parallelism between receptor density and locus of action.. AB - P. Janicki, S.W. Gumulka, P. Krzaścik and E. Habermann. ...
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Action potentials in vertebrate neurons are followed by an afterhyperpolarization (AHP) that may persist for several seconds and may have profound consequences for the firing pattern of the neuron. Each component of the AHP is kinetically distinct and is mediated by different calcium-activated potassium channels. The protein encoded by this gene is activated before membrane hyperpolarization and is thought to regulate neuronal excitability by contributing to the slow component of synaptic AHP. This gene is a member of the KCNN family of potassium channel genes. The encoded protein is an integral membrane protein that forms a voltage-independent calcium-activated channel with three other calmodulin-binding subunits. Alternate splicing of this gene results in multiple transcript variants. [provided by RefSeq, May 2013 ...
Forms a voltage-independent potassium channel activated by intracellular calcium. Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization. The channel is blocked by apamin (By similarity).
Background. Small conductance Ca2+-activated K+ (SK) channels play significant roles in regulating the excitability of cardiomyocytes (CMs). SK channels are unique in that they are gated solely by intracellular Ca2+ and hence, function to integrate intracellular Ca2+ and membrane potentials on a beat-to-beat basis in the heart. Our previous studies revealed that cardiac SK2 channels coupled with L-type Ca2+ channels (LTCCs) through a physical bridge, α-actinin2, suggesting that LTCCs may be functionally coupled with SK2 channels by providing local Ca2+ domain to activate the SK channels. However, a recent study suggested that sarcoplasmic reticulum (SR) Ca2+ release is necessary and sufficient for the activation of cardiac SK channels. The objective of the study is to examine the mechanisms of SK channel activation in native CMs.. Methods and Results. By using a voltage-clamp protocol in rabbit CMs to activate LTCCs followed immediately by a test voltage to monitor the SK currents, we recorded ...
TY - JOUR. T1 - SK channels and NMDA receptors form a Ca2+-mediated feedback loop in dendritic spines. AU - Ngo-Anh, Thu Jennifer. AU - Bloodgood, Brenda L.. AU - Lin, Michael. AU - Sabatini, Bernardo L.. AU - Maylie, James. AU - Adelman, John. PY - 2005/5. Y1 - 2005/5. N2 - Small-conductance Ca2+-activated K+ channels (SK channels) influence the induction of synaptic plasticity at hippocampal CA3-CA1 synapses. We find that in mice, SK channels are localized to dendritic spines, and their activity reduces the amplitude of evoked synaptic potentials in an NMDA receptor (NMDAR)-dependent manner. Using combined two-photon laser scanning microscopy and two-photon laser uncaging of glutamate, we show that SK channels regulate NMDAR-dependent Ca2+ influx within individual spines. SK channels are tightly coupled to synaptically activated Ca2+ sources, and their activity reduces the amplitude of NMDAR-dependent Ca2+ transients. These effects are mediated by a feedback loop within the spine head; during ...
KCNN4 antibody (potassium intermediate/small conductance calcium-activated channel, subfamily N, member 4) for ELISA, WB. Anti-KCNN4 pAb (GTX87069) is tested in Human, Mouse, Rat samples. 100% Ab-Assurance.
The whole-cell current clamp and voltage clamp techniques were used to record the slow Na+ action potentials (APs) and the inward current in cultured single ventricular cells isolated from young (3 day-old) embryonic chicks. The slow Na+ APs had a +Vmax of 21.5 +/- 7.5 V/s (in 10 different single ce …
The Ca2+-activated Cl channel anoctamin-1 (Ano1; Tmem16A) plays a variety of physiological roles, including epithelial fluid secretion. Ano1 is activated by increases in intracellular Ca2+, but there is uncertainty whether Ca2+ binds directly to Ano1 or whether phosphorylation or additional Ca2+-binding subunits like calmodulin (CaM) are required. Here we show that CaM is not necessary for activation of Ano1 by Ca2+ for the following reasons. (a) Exogenous CaM has no effect on Ano1 currents in inside-out excised patches. (b) Overexpression of Ca2+-insensitive mutants of CaM have no effect on Ano1 currents, whereas they eliminate the current mediated by the small-conductance Ca2+-activated K+ (SK2) channel. (c) Ano1 does not coimmunoprecipitate with CaM, whereas SK2 does. Furthermore, Ano1 binds very weakly to CaM in pull-down assays. (d) Ano1 is activated in excised patches by low concentrations of Ba2+, which does not activate CaM. In addition, we conclude that reversible ...
SKŁAD , CENA , DOSTĘPNOŚĆ. Skład kremu jest bardzo bogaty i zadowoli każdą z Was. Głównym składnikiem produktu pielęgnacyjnego jest bowiem witamina C - "królowa pielęgnacji skóry" i "królowa młodości". Witamina C stymuluje syntezę kolagenu i kwasu hialuronowego, rozjaśnia skórę i niweluje przebarwienia poprzez hamowanie produkcji melaniny, złuszcza naskórek, jest najsilniejszym przeciwutleniaczem, hamuje wypłukiwanie kolagenu i elastyny, przez co utrzymuje skórę jędrną i napiętą, zmniejsza zaczerwienienia skóry, uszczelnia naczynia krwionośne, wzmacnia barierę lipidową skóry, przez co utrzymuje odpowiedni poziom nawilżenia. Łagodzi, koi i regeneruje skórę, działa antybakteryjnie i minimalizuje niedoskonałości skórne, wspomaga ochronę UVA/UVB, wzmacnia odporność skóry. Można by wymieniać bez końca. Działanie witaminy C w kremie LA ROCHE-POSAY zostało wzmocnione dwoma składnikami aktywnymi: mannozą, czyli cukrem przywracającym skórze ...
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休日明けとなる今日の読売ジャイアンツは、韓国のSKワイバーンズと練習試合を行った。・★G出場野手雑感①ショート 坂本3打数1安打 盗塁1*バットの先セカンドハーフライナー*強引にレフト前ヒット(その後盗塁)*見切って四球*詰まってセカンドゴ
[ChEMBL Target Description] ID:CHEMBL3381, Name:Small conductance calcium-activated potassium channel protein 3, Description:, Synonyms:
The SK channel was first cloned in 1996 and is known to be responsible for afterhyperpolarization the controls neuronal discharges. It is also known to be present in the atria, but its function in the ventricles was unclear. Studies from the Peng-Sheng Chen Laboratory documented that the SK current is upregulated in failing rabbit ventricles. SK current activation during ventricular fibrillation shortens the APD and is responsible for inducing recurrent VF in failing rabbit ventricles. The lab then performed studies in failing human ventricles to document the presence of SK current upregulation. In the failing ventricles, SK current is important in steepening the action potential duration restitution curve at rapid rates, which help induce VF.. On the other hand, the SK current is also upregulated in failing ventricles during bradycardia and help maintain the repolarization reserve and prevent afterdepolarization and torsades de pointes ventricular arrhythmia. These findings provided new ...
Department of Anatomy and Neurobiology, Washington University School of Medicine, St. Louis, Missouri (A.D.W.); Departments of Microbiology and Molecular Genetics (G.A.G.) and Physiology and Biophysics (K.G.C.), University of California, Irvine, Irvine, California; Molecular and Cellular Physiology Department, Stanford University, Stanford, California (R.A.); Department of Medical Pharmacology and Toxicology, University of California, Davis, Davis, California (H.W.); and Department of Applied Physiology, University Ulm, Ulm, Germany (S.G.) ...
Bee venom is a natural compound produced by the honey bee (Apis mellifera), and has been reported as having the biological and pharmacological activities, including anti-bacterial, anti-viral and anti-inflammation. In the present study, the inhibitory effects of bee venom and its major peptide components on the tumor invasion were demonstrated. It was confirmed the inhibitory effects of bee venom, melittin, and apamin on the EGF-induced invasion of breast cancer cells. Transwell invasion and wound-healing assays showed that bee venom and melittin significantly inhibits the EGF-induced invasion and migration of breast cancer cells. Also, bee venom and melittin reduced the EGF-stimulated F-actin reorganization at the leading edge, but apamin did not affect. Particularly, melittin inhibited the EGF-induced MMP-9 expression via blocking the NF-κB and PI3K/Akt/mTOR pathway. In addition, melittin significantly suppressed the EGF-induced FAK phosphorylation through inhibition of mTOR/p70S6K/4E-BP1 ...
Bee venom is a natural compound produced by the honey bee (Apis mellifera), and has been reported as having the biological and pharmacological activities, including anti-bacterial, anti-viral and anti-inflammation. In the present study, the inhibitory effects of bee venom and its major peptide components on the tumor invasion were demonstrated. It was confirmed the inhibitory effects of bee venom, melittin, and apamin on the EGF-induced invasion of breast cancer cells. Transwell invasion and wound-healing assays showed that bee venom and melittin significantly inhibits the EGF-induced invasion and migration of breast cancer cells. Also, bee venom and melittin reduced the EGF-stimulated F-actin reorganization at the leading edge, but apamin did not affect. Particularly, melittin inhibited the EGF-induced MMP-9 expression via blocking the NF-κB and PI3K/Akt/mTOR pathway. In addition, melittin significantly suppressed the EGF-induced FAK phosphorylation through inhibition of mTOR/p70S6K/4E-BP1 ...
Effective, safe, and tolerable pharmacological treatment for atrial fibrillation (AF) remains an unmet need. The latest medication to reach the market for intravenous cardioversion was the combined sodium and potassium channel inhibitor vernakalant, however not yet available in the United States. Vernakalant terminated ≈50% of episodes of AF lasting ,7 days in randomized controlled studies, with its highest conversion rate during the first few days while after 8 to 45 days of AF, the conversion rate was ,10%, which was not statistically different from that of placebo.1,2. If lasting for ,24 hours, AF promotes further progression of the disease-a phenomenon described as AF begets AF.3 If atrial remodeling continues, AF often progresses to more sustained forms and becomes more resistant to both pharmacological and nonpharmacological treatments, including ablation.4-6 Among contributing factors, an increased influx of calcium seems to promote fibrosis development and remodeling.7. Three subtypes ...
Results: Bee venom inhibited cell invasion and migration, and also suppressed MMP-9 activity and expression, processes related to tumor invasion and metastasis, in PMA-induced MCF-7 cells. Bee venom specifically suppressed the phosphorylation of p38/JNK and at the same time, suppressed the protein expression, DNA binding and promoter activity of NF-κB. The levels of phosphorylated ERK1/2 and c-Jun did not change. We also investigated MMP-9 inhibition by melittin, apamin and PLA2, representative single component of bee venom. We confirmed that PMA-induced MMP-9 activity was significantly decreased by melittin, but not by apamin and phospholipase A2. These data demonstrated that the expression of MMP-9 was abolished by melittin, the main component of bee venom ...
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In these experiments, the extracellular solution contained Ca2+ (2 mM). TTX (1 μM) was present to block voltage-gated Na+ currents, and 4-AP (5 mM) was present to block IA in all experiments. In different sets of experiments, the extracellular solution also contained a blocker of one known type of KCa, so that the effect of haloperidol on the other type of KCa could be tested specifically. For example, the experimental solution in Figure 8A contained apamin (300 nM) in addition to TTX and 4-AP to block SK-type KCa channels. 16 Figure 8A shows outward currents evoked by a voltage command to +30 mV from a holding potential of −70 mV. Under the experimental conditions, the evoked current is expected to consist of the persistent component of the voltage-gated K+ current and KCa flowing through BK-type channels. Haloperidol had little effect on the amplitude of the outward current. This small effect might be expected if the evoked outward current consisted entirely of the persistent component of ...
Atrial fibrillation (AF) is the most common type of arrhythmia. Current pharmacological treatment for AF is moderately effective and/or increases the risk of serious ventricular adverse effects. To avoid ventricular adverse effects, a new target has been considered, the small conductance calcium-activated K+ channels (KCa2.X, SK channels). In the heart, KCa2.X channels are functionally more important in atria compared to ventricles, and pharmacological inhibition of the channel confers atrial selective prolongation of the cardiac action potential and converts AF to sinus rhythm in animal models of AF. Whether antiarrhythmic drugs (AADs) recommended for treating AF target KCa2.X channels is unknown. To this end, we tested a large number of AADs on the human KCa2.2 and KCa2.3 channels to assess their effect on this new target using automated whole-cell patch clamp. Of the AADs recommended for treatment of AF only dofetilide and propafenone inhibited hKCa2.X channels, with no subtype selectivity. ...
1 the alpha(2)-adrenoceptor function in mesenteric arteries of spontaneously hypertensive rats (SHR) was investigated by comparing membrane potential changes in response to adrenergic agonists in preparations from female SHR, Wistar-Kyoto (WKY) and normotensive Wistar rats (NWR).2 Resting membrane potential was found to be less negative in mesenteric arteries from SHR than in those from NWR and WKY. Apamin induced a decrease in the membrane potential of mesenteric artery rings without endothelium from NWR and WKY, but had no effects in those from SHR. Both UK 14,304 and adrenaline, in the presence of prazosin, induced a hyperpolarization that was significantly lower in de-endothelialized mesenteric rings from SHR than in those from NWR and WKY. in mesenteric rings with endothelium, however, similar hyperpolarization was observed in the three strains.3 in NWR mesenteric rings with endothelium the hyperpolarization induced by activation of alpha(2)-adrenoceptors was abolished by apamin, whereas in ...
Sk ra .. budowie sk ry wyr niono podzia na: nask rek, sk r w a ciw , tkank podsk rn oraz przydatki tj. mieszki w osowe, gruczo y, paznokcie. Od zewn trz sk r pokrywa warstwa lipidowa i z uszczona keratyna. Unaczynienie sk ry odgrywa podstawow rol w termoregulacji ustroju. W sk rze w a ciwej oraz na j... Sk ra w a ciwa i tkanka podsk rna .. budowana jest z kom rek i w kien cznotkankowych, zawiera naczynia, zako czenia nerwowe oraz przydatki sk ry. W jej obr bie wyr niono warstw brodawkow i znajduj c si ni ej warstw siateczkow . Podstaw budowy s : w kna kolagenowe, retikulinowe oraz spr yste nadaj ce sk rze spr ysto i wyt... ...
Uchwała nr XXXI/471/2013 Rady Miasta Wisła z dnia 31 października 2013r. w sprawie określenia warunków i trybu składania deklaracji oraz informacji w podatkach i opłatach lokalnych za pomocą środków komunikacji elektronicznej . Tekst pierwotny. Największa bezpłatna baza aktów prawnych.
MGI protein superfamily detail pages represent the protein classification set for a homeomorphic superfamily from the Protein Information Resource SuperFamily (PIRSF) site.. Mouse superfamily members are shown with links to their corresponding HomoloGene Classes. Note that pseudogenes are included in PIRSF families but not in orthology sets used here. You can select a given mouse superfamily member and download (or forward to NCBI BLAST) FASTA formatted protein sequences of that mouse gene and its mouse, human and rat homologs, as defined in the corresponding HomoloGene Class. The numbers of mouse, human and rat genes in the HomoloGene Class are shown. You can also "Select all" mouse superfamily members to obtain their protein sequences and the protein sequences for all mouse, human and rat homologs of the mouse superfamily members.. The number of protein sequences returned does not always match the numbers of homologs shown, because the same protein sequence can be associated with multiple ...
human KCNN3 protein: a small conductance calcium-regulated potassium channel; mutations in gene shows a possible association with schizophrenia; RefSeq NM_002249
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KCNN3兔多克隆抗体(ab28631)可与人样本反应并经WB, ELISA实验严格验证,被1篇文献引用。所有产品均提供质保服务,中国75%以上现货。
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