A highly neurotoxic polypeptide from the venom of the honey bee (Apis mellifera). It consists of 18 amino acids with two disulfide bridges and causes hyperexcitability resulting in convulsions and respiratory paralysis.
Venoms obtained from Apis mellifera (honey bee) and related species. They contain various enzymes, polypeptide toxins, and other substances, some of which are allergenic or immunogenic or both. These venoms were formerly used in rheumatism to stimulate the pituitary-adrenal system.
A 37-amino acid residue peptide isolated from the scorpion Leiurus quinquestriatus hebraeus. It is a neurotoxin that inhibits calcium activated potassium channels.
A major class of calcium-activated potassium channels that are found primarily in excitable CELLS. They play important roles in the transmission of ACTION POTENTIALS and generate a long-lasting hyperpolarization known as the slow afterhyperpolarization.
Endogenously-synthesized compounds that influence biological processes not otherwise classified under ENZYMES; HORMONES or HORMONE ANTAGONISTS.
A class of drugs that act by inhibition of potassium efflux through cell membranes. Blockade of potassium channels prolongs the duration of ACTION POTENTIALS. They are used as ANTI-ARRHYTHMIA AGENTS and VASODILATOR AGENTS.
Potassium channels whose activation is dependent on intracellular calcium concentrations.
Cell membrane glycoproteins that are selectively permeable to potassium ions. At least eight major groups of K channels exist and they are made up of dozens of different subunits.
A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90)
Venoms from animals of the order Scorpionida of the class Arachnida. They contain neuro- and hemotoxins, enzymes, and various other factors that may release acetylcholine and catecholamines from nerve endings. Of the several protein toxins that have been characterized, most are immunogenic.
That phase of a muscle twitch during which a muscle returns to a resting position.
An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6)
A major class of calcium-activated potassium channels that were originally discovered in ERYTHROCYTES. They are found primarily in non-excitable CELLS and set up electrical gradients for PASSIVE ION TRANSPORT.
One of the POTASSIUM CHANNEL BLOCKERS, with secondary effect on calcium currents, which is used mainly as a research tool and to characterize channel subtypes.
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
Arteries which arise from the abdominal aorta and distribute to most of the intestines.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also been tried in patients with asthma. (Martindale, The Extra Pharmacopoeia, 30th ed, p352)
Drugs used to cause dilation of the blood vessels.
A neuromuscular blocker and active ingredient in CURARE; plant based alkaloid of Menispermaceae.
Paracrine substances produced by the VASCULAR ENDOTHELIUM with VASCULAR SMOOTH MUSCLE relaxation (VASODILATION) activities. Several factors have been identified, including NITRIC OXIDE and PROSTACYCLIN.
A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.
A topical bacteriostat that is available as various salts. It is used in wound dressings and mouth infections and may also have antifungal action, but may cause skin ulceration.
Use of electric potential or currents to elicit biological responses.
Abrupt changes in the membrane potential that sweep along the CELL MEMBRANE of excitable cells in response to excitation stimuli.
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Single pavement layer of cells which line the luminal surface of the entire vascular system and regulate the transport of macromolecules and blood components.
A major class of calcium activated potassium channels whose members are voltage-dependent. MaxiK channels are activated by either membrane depolarization or an increase in intracellular Ca(2+). They are key regulators of calcium and electrical signaling in a variety of tissues.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.
A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes.
A powerful vasodilator used in emergencies to lower blood pressure or to improve cardiac function. It is also an indicator for free sulfhydryl groups in proteins.
Inorganic compounds that contain barium as an integral part of the molecule.
The relationship between the dose of an administered drug and the response of the organism to the drug.
The recording of muscular movements. The apparatus is called a myograph, the record or tracing, a myogram. (From Stedman, 25th ed)
An aminoperhydroquinazoline poison found mainly in the liver and ovaries of fishes in the order TETRAODONTIFORMES, which are eaten. The toxin causes paresthesia and paralysis through interference with neuromuscular conduction.
Insect members of the superfamily Apoidea, found almost everywhere, particularly on flowers. About 3500 species occur in North America. They differ from most WASPS in that their young are fed honey and pollen rather than animal food.
Works containing information articles on subjects in every field of knowledge, usually arranged in alphabetical order, or a similar work limited to a special field or subject. (From The ALA Glossary of Library and Information Science, 1983)
A sulfur-containing analog of butyrylcholine which is hydrolyzed by butyrylcholinesterase to butyrate and thiocholine. It is used as a reagent in the determination of butyrylcholinesterase activity.
A sweet viscous liquid food, produced in the honey sacs of various bees from nectar collected from flowers. The nectar is ripened into honey by inversion of its sucrose sugar into fructose and glucose. It is somewhat acidic and has mild antiseptic properties, being sometimes used in the treatment of burns and lacerations.

Acetylcholine-induced membrane potential changes in endothelial cells of rabbit aortic valve. (1/590)

1. Using a microelectrode technique, acetylcholine (ACh)-induced membrane potential changes were characterized using various types of inhibitors of K+ and Cl- channels in rabbit aortic valve endothelial cells (RAVEC). 2. ACh produced transient then sustained membrane hyperpolarizations. Withdrawal of ACh evoked a transient depolarization. 3. High K+ blocked and low K+ potentiated the two ACh-induced hyperpolarizations. Charybdotoxin (ChTX) attenuated the ACh-induced transient and sustained hyperpolarizations; apamin inhibited only the sustained hyperpolarization. In the combined presence of ChTX and apamin, ACh produced a depolarization. 4. In Ca2+-free solution or in the presence of Co2+ or Ni2+, ACh produced a transient hyperpolarization followed by a depolarization. In BAPTA-AM-treated cells, ACh produced only a depolarization. 5. A low concentration of A23187 attenuated the ACh-induced transient, but not the sustained, hyperpolarization. In the presence of cyclopiazonic acid, the hyperpolarization induced by ACh was maintained after ACh removal; this maintained hyperpolarization was blocked by Co2+. 6. Both NPPB and hypertonic solution inhibited the membrane depolarization seen after ACh washout. Bumetanide also attenuated this depolarization. 7. It is concluded that in RAVEC, ACh produces a two-component hyperpolarization followed by a depolarization. It is suggested that ACh-induced Ca2+ release from the storage sites causes a transient hyperpolarization due to activation of ChTX-sensitive K+ channels and that ACh-activated Ca2+ influx causes a sustained hyperpolarization by activating both ChTX- and apamin-sensitive K+ channels. Both volume-sensitive Cl- channels and the Na+-K+-Cl- cotransporter probably contribute to the ACh-induced depolarization.  (+info)

Charybdotoxin and apamin block EDHF in rat mesenteric artery if selectively applied to the endothelium. (2/590)

In rat mesenteric artery, endothelium-derived hyperpolarizing factor (EDHF) is blocked by a combination of apamin and charybdotoxin (ChTX). The site of action of these toxins has not been established. We compared the effects of ChTX and apamin applied selectively to the endothelium and to the smooth muscle. In isometrically mounted arteries, ACh (0.01-10 micrometers), in the presence of indomethacin (2.8 microM) and Nomega-nitro-L-arginine methyl ester (L-NAME) (100 microM), concentration dependently relaxed phenylephrine (PE)-stimulated tone (EC50 50 nM; n = 10). Apamin (50 nM) and ChTX (50 nM) abolished this relaxation (n = 5). In pressurized arteries, ACh (10 microM), applied intraluminally in the presence of indomethacin (2.8 microM) and L-NAME (100 microM), dilated both PE-stimulated (0.3-0.5 microM; n = 5) and myogenic tone (n = 3). Apamin (50 nM ) and ChTX (50 nM) applied intraluminally abolished ACh-induced dilatations. Bath superperfusion of apamin and ChTX did not affect ACh-induced dilatations of either PE-stimulated (n = 5) or myogenic tone (n = 3). This is the first demonstration that ChTX and apamin act selectively on the endothelium to block EDHF-mediated relaxation.  (+info)

Role of K+ channels in A2A adenosine receptor-mediated dilation of the pressurized renal arcuate artery. (3/590)

1. Adenosine A2A receptor-mediated renal vasodilation was investigated by measuring the lumenal diameter of pressurized renal arcuate arteries isolated from the rabbit. 2. The selective A2A receptor agonist CGS21680 dilated the arteries with an EC50 of 130 nM. The CGS21680-induced vasodilation was, on average, 34% less in endothelium-denuded arteries. 3. The maximum response and the EC50 for CGS21680-induced vasodilation in endothelium-intact arteries were not significantly affected by incubation with the K+ channel blockers apamin (100 nM), iberiotoxin (100 nM), 3,4-diaminopyridine (1 mM), glibenclamide (1 microM) or Ba2+ (10 microM). However, a cocktail mixture of these blockers did significantly inhibit the maximum response by almost 40%, and 1 mM Ba2+ alone or 1 mM Ba2+ in addition to the cocktail inhibited the maximum CGS21680-response by 58% and about 75% respectively. 4. CGS21680-induced vasodilation was strongly inhibited when the extracellular K+ level was raised to 20 mM even though the dilator response to 1 microM levcromakalim, a K(ATP) channel opener drug, was unaffected. 5. CGS21680-induced vasodilation was inhibited by 10 microM ouabain, an inhibitor of Na+/K(+)-ATPase, but ouabain had a similar inhibitory effect on vasodilation induced by 30 nM nicardipine (a dihydropyridine Ca2+ antagonist) or 1 microM levcromakalim. 6. The data suggest that K+ channel activation does play a role in A(2A) receptor-mediated renal vasodilation. The inhibitory effect of raised extracellular K+ levels on the A(2A) response may be due to K(+)-induced stimulation of Na+/K(+)-ATPase.  (+info)

Blockade of SK-type Ca2+-activated K+ channels uncovers a Ca2+-dependent slow afterdepolarization in nigral dopamine neurons. (4/590)

Sharp electrode current-clamp recording techniques were used to characterize the response of nigral dopamine (DA)-containing neurons in rat brain slices to injected current pulses applied in the presence of TTX (2 microM) and under conditions in which apamin-sensitive Ca2+-activated K+ channels were blocked. Addition of apamin (100-300 nM) to perfusion solutions containing TTX blocked the pacemaker oscillation in membrane voltage evoked by depolarizing current pulses and revealed an afterdepolarization (ADP) that appeared as a shoulder on the falling phase of the voltage response. ADP were preceded by a ramp-shaped slow depolarization and followed by an apamin-insensitive hyperpolarizing afterpotential (HAP). Although ADPs were observed in all apamin-treated cells, the duration of the response varied considerably between individual neurons and was strongly potentiated by the addition of TEA (2-3 mM). In the presence of TTX, TEA, and apamin, optimal stimulus parameters (0.1 nA, 200-ms duration at -55 to -68 mV) evoked ADP ranging from 80 to 1,020 ms in duration (355.3 +/- 56.5 ms, n = 16). Both the ramp-shaped slow depolarization and the ensuing ADP were markedly voltage dependent but appeared to be mediated by separate conductance mechanisms. Thus, although bath application of nifedipine (10-30 microM) or low Ca2+, high Mg2+ Ringer blocked the ADP without affecting the ramp potential, equimolar substitution of Co2+ for Ca2+ blocked both components of the voltage response. Nominal Ca2+ Ringer containing Co2+ also blocked the HAP evoked between -55 and -68 mV. We conclude that the ADP elicited in DA neurons after blockade of apamin-sensitive Ca2+-activated K+ channels is mediated by a voltage-dependent, L-type Ca2+ channel and represents a transient form of the regenerative plateau oscillation in membrane potential previously shown to underlie apamin-induced bursting activity. These data provide further support for the notion that modulation of apamin-sensitive Ca2+-activated K+ channels in DA neurons exerts a permissive effect on the conductances that are involved in the expression of phasic activity.  (+info)

Differential effects of apamin- and charybdotoxin-sensitive K+ conductances on spontaneous discharge patterns of developing retinal ganglion cells. (5/590)

The spontaneous discharge patterns of developing retinal ganglion cells are thought to play a crucial role in the refinement of early retinofugal projections. To investigate the contributions of intrinsic membrane properties to the spontaneous activity of developing ganglion cells, we assessed the effects of blocking large and small calcium-activated potassium conductances on the temporal pattern of such discharges by means of patch-clamp recordings from the intact retina of developing ferrets. Application of apamin and charybdotoxin (CTX), which selectively block the small and large calcium-activated potassium channels, respectively, resulted in significant changes in spontaneous firings. In cells recorded from the oldest animals [postnatal day 30 (P30)-P45], which manifested relatively sustained discharge patterns, application of either blocker induced bursting activity. With CTX the bursts were highly periodic, short in duration, and of high frequency. In contrast, with apamin the interburst intervals were longer, less regular, and lower in overall spike frequency. These differences between the effects of the two blockers on spontaneous activity were documented by spectral analysis of discharge patterns. Filling cells from which recordings were made with Lucifer yellow revealed that these effects were obtained in all three morphological classes of cells: alpha, beta, and gamma. These findings provide the first evidence that apamin- and CTX-sensitive K+ conductances can have differential effects on the spontaneous discharge patterns of retinal ganglion cells. Remarkably, the bursts of activity obtained after apamin application in more mature neurons appeared very similar to the spontaneous bursting patterns observed in developing neurons. These findings suggest that the maturation of calcium-activated potassium channels, particularly the apamin-sensitive conductance, may contribute to the changes in spontaneous firings exhibited by retinal ganglion cells during the course of normal development.  (+info)

Coordinate regulation of gonadotropin-releasing hormone neuronal firing patterns by cytosolic calcium and store depletion. (6/590)

Elevation of cytosolic free Ca2+ concentration ([Ca2+]i) in excitable cells often acts as a negative feedback signal on firing of action potentials and the associated voltage-gated Ca2+ influx. Increased [Ca2+]i stimulates Ca2+-sensitive K+ channels (IK-Ca), and this, in turn, hyperpolarizes the cell and inhibits Ca2+ influx. However, in some cells expressing IK-Ca the elevation in [Ca2+]i by depletion of intracellular stores facilitates voltage-gated Ca2+ influx. This phenomenon was studied in hypothalamic GT1 neuronal cells during store depletion caused by activation of gonadotropin-releasing hormone (GnRH) receptors and inhibition of endoplasmic reticulum (Ca2+)ATPase with thapsigargin. GnRH induced a rapid spike increase in [Ca2+]i accompanied by transient hyperpolarization, followed by a sustained [Ca2+]i plateau during which the depolarized cells fired with higher frequency. The transient hyperpolarization was caused by the initial spike in [Ca2+]i and was mediated by apamin-sensitive IK-Ca channels, which also were operative during the subsequent depolarization phase. Agonist-induced depolarization and increased firing were independent of [Ca2+]i and were not mediated by inhibition of K+ current, but by facilitation of a voltage-insensitive, Ca2+-conducting inward current. Store depletion by thapsigargin also activated this inward depolarizing current and increased the firing frequency. Thus, the pattern of firing in GT1 neurons is regulated coordinately by apamin-sensitive SK current and store depletion-activated Ca2+ current. This dual control of pacemaker activity facilitates voltage-gated Ca2+ influx at elevated [Ca2+]i levels, but also protects cells from Ca2+ overload. This process may also provide a general mechanism for the integration of voltage-gated Ca2+ influx into receptor-controlled Ca2+ mobilization.  (+info)

Endothelium-derived relaxing, contracting and hyperpolarizing factors of mesenteric arteries of hypertensive and normotensive rats. (7/590)

Differences in the acetylcholine (ACh)-induced endothelium-dependent relaxation and hyperpolarization of the mesenteric arteries of Wistar Kyoto rats (WKY) and stroke-prone spontaneously hypertensive rats (SHRSP) were studied. Relaxation was impaired in preparations from SHRSP and tendency to reverse the relaxation was observed at high concentrations of ACh in these preparations. Relaxation was partly blocked by NG-nitro-L-arginine (L-NOARG, 100 microM) and, in the presence of L-NOARG, tendency to reverse the relaxation was observed in response to higher concentrations of ACh, even in preparations from WKY. The relaxation remaining in the presence of L-NOARG was also smaller in preparations from SHRSP. The tendency to reverse the relaxation observed at higher concentrations of ACh in preparations from SHRSP or WKY in the presence of L-NOARG were abolished by indomethacin (10 microM). Elevating the K+ concentration of the incubation medium decreased relaxation in the presence of both indomethacin and L-NOARG. Relaxation in the presence of L-NOARG and indomethacin was reduced by the application of both apamin (5 microM) and charybdotoxin (0.1 microM). This suggests that the relaxation induced by ACh is brought about by both endothelium-derived relaxing factor (EDRF, nitric oxide (NO)) and hyperpolarizing factor (EDHF), which activates Ca2+-sensitive K+ channels. Electrophysiological measurement revealed that ACh induced endothelium-dependent hyperpolarization of the smooth muscle of both preparations in the presence of L-NOARG and indomethacin; the hyperpolarization being smaller in the preparation from SHRSP than that from WKY. These results suggest that the release of both NO and EDHF is reduced in preparations from SHRSP. In addition, indomethacin-sensitive endothelium-derived contracting factor (EDCF) is released from both preparations; the release being increased in preparations from SHRSP.  (+info)

Integrin-regulated secretion of interleukin 4: A novel pathway of mechanotransduction in human articular chondrocytes. (8/590)

Chondrocyte function is regulated partly by mechanical stimulation. Optimal mechanical stimulation maintains articular cartilage integrity, whereas abnormal mechanical stimulation results in development and progression of osteoarthritis (OA). The responses of signal transduction pathways in human articular chondrocytes (HAC) to mechanical stimuli remain unclear. Previous work has shown the involvement of integrins and integrin-associated signaling pathways in activation of plasma membrane apamin-sensitive Ca2+-activated K+ channels that results in membrane hyperpolarization of HAC after 0. 33 Hz cyclical mechanical stimulation. To further investigate mechanotransduction pathways in HAC and show that the hyperpolarization response to mechanical stimulation is a result of an integrin-dependent release of a transferable secreted factor, we used this response. Neutralizing antibodies to interleukin 4 (IL-4) and IL-4 receptor alpha inhibit mechanically induced membrane hyperpolarization and anti-IL-4 antibodies neutralize the hyperpolarizing activity of medium from mechanically stimulated cells. Antibodies to interleukin 1beta (IL-1beta) and cytokine receptors, interleukin 1 receptor type I and the common gamma chain/CD132 (gamma) have no effect on me- chanically induced membrane hyperpolarization. Chondrocytes from IL-4 knockout mice fail to show a membrane hyperpolarization response to cyclical mechanical stimulation. Mechanically induced release of the chondroprotective cytokine IL-4 from HAC with subsequent autocrine/paracrine activity is likely to be an important regulatory pathway in the maintenance of articular cartilage structure and function. Finally, dysfunction of this pathway may be implicated in OA.  (+info)

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 - Concomitant SK current activation and sodium current inhibition cause J wave syndrome. AU - Chen, Mu. AU - Xu, Dong Zhu. AU - Wu, Adonis Z.. AU - Guo, Shuai. AU - Wan, Juyi. AU - Yin, Dechun. AU - Lin, Shien-Fong. AU - Chen, Zhenhui. AU - Rubart-von der Lohe, Michael. AU - Everett, Thomas H.. AU - Qu, Zhilin. AU - Weiss, James N.. AU - Chen, Peng Sheng. PY - 2018/11/15. Y1 - 2018/11/15. N2 - The mechanisms of J wave syndrome (JWS) are incompletely understood. Here, we showed that the concomitant activation of small-conductance calcium-activated potassium (SK) current (IKAS) and inhibition of sodium current by cyclohexyl-[2-(3,5-dimethyl-pyrazol-1-yl)-6-methyl-pyrimidin-4-yl]-amine (CyPPA) recapitulate the phenotypes of JWS in Langendorff-perfused rabbit hearts. CyPPA induced significant J wave elevation and frequent spontaneous ventricular fibrillation (SVF), as well as sinus bradycardia, atrioventricular block, and intraventricular conduction delay. IKAS activation by CyPPA ...
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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Fingerprint Dive into the research topics of The antidepressant fluoxetine blocks the human small conductance calcium-activated potassium channels SK1, SK2 and SK3. Together they form a unique fingerprint. ...
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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Blocks small conductance calcium-activated potassium channels (PubMed:12239213). Shows activity on KCa2.2/KCNN2 (IC(50)=0.0243 nM), KCa2.3/KCNN3 (IC(50)=1.7 nM), and KCa2.1/KCNN1 (IC(50)=42 nM) (PubMed:12239213). Induces cell death when tested on Jurkat E6-1 and human mammary breast cancer MDA-MB-231 which constituvely express KCa2.2/KCNN2, but not on human peripheral blood lymphocytes (which do not express KCa2.2/KCNN2) (PubMed:24821061).
Abstract(s) :. (Anglais) Cholecystokinin (CCK) / sulfakinin (SK)-type neuropeptides regulate feeding and 37 digestion in chordates and protostomes (e.g. insects). Here we characterised CCK/SK-type 38 signalling for the first time in a non-chordate deuterostome - the starfish Asterias rubens 39 (phylum Echinodermata). In this species, two neuropeptides (ArCCK1, ArCCK2) derived from 40 the precursor protein ArCCKP act as ligands for a CCK/SK-type receptor (ArCCKR) and are 41 expressed in the nervous system, digestive system, tube feet and body wall. Furthermore, 42 ArCCK1 and ArCCK2 cause dose-dependent contraction of cardiac stomach, tube foot and 43 body wall apical muscle preparations in vitro and injection of these neuropeptides in vivo 44 triggers cardiac stomach retraction and inhibition of the onset of feeding in A. rubens. Thus, an 45 evolutionarily ancient role of CCK/SK-type neuropeptides as inhibitory regulators of feeding- 46 related processes in the Bilateria has been conserved in the ...
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 ...
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TY - JOUR. T1 - Effect of different calcium channel blockers on inhibitory junction potentials and slow waves in porcine ileum. AU - Borderies, J. R.. AU - Goñalons, E.. AU - Angel, F.. AU - Vergara, P.. AU - Jiménez, Marcel. PY - 1997/2/14. Y1 - 1997/2/14. N2 - The effect of several calcium channel blockers was evaluated: (i) on spontaneous electrical and mechanical activities and (ii) on the response to electrical field stimulation. The study was carried out on whole-thickness preparation of porcine ileum. Glass microelectrodes were used to record membrane potential from smooth muscle cells. Resting membrane potential was -60 ± 2 mV (n = 18) and preparations generated spontaneous slow waves. Electrical field stimulation (EFS) was applied using different parameters. The amplitude and duration of inhibitory junction potentials (IJPs) increased with EFS strength. IJPs were abolished by tetrodotoxin (1 μM). Nifedipine (1 μM) did not modify the amplitude or duration of IJPs. The frequency 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. ...
Tamapin is a peptide toxin isolated from the venom of the Indian red scorpion Mesobuthus Tamulus. Tamapin is amidated at its C-terminal tyrosine residue (contrary to recombinant tamapin, Smartox tamapin is amidated). It binds to small conductance Ca2+-activated K+ channels (SK channels) with high affinity and inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus as well as in cell lines expressing distinct SK channel subunits. Tamapin is an excellent toxin to discriminate among SK channel subtypes because it presents different affinities for SK1 (42 nM), SK2 (24 pM) and SK3 (1.7 nM) channels. This toxin is also the most potent SK2 channel blocker characterized so far (IC50 for SK2 channels = 24 pM). ...
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... ...
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Pi4 competes with apamin, another SK-channel toxin. IC50 is 0.5 ± 0.2 μM. Scorpion venoms can be toxic for mammals, insects, ...
Apamin is a neurotoxin that augments polysynaptic reflexes. MCD peptide destroys mast cells. Feeling only slight pain, Schmidt ... Since many small bees are categorized into a pain level of 1, most toxic polypeptides in bee venom are melittin, apamin, and ...
M. Stocker; M. Krause; P. Pedarzani (1999). "An apamin-sentisitive Ca2+-activated K+ current in hippocampal pyramidal neurons ... Examples of calcium-activated channel blockers include: Charybdotoxin Iberiotoxin Apamin Kaliotoxin, Lolitrem, BKCa-specific ...
Stocker M, Krause M, Pedarzani P (April 1999). "An apamin-sensitive Ca2+-activated K+ current in hippocampal pyramidal neurons ...
Hider RC and Ragnarsson U. A proposal for the structure of apamin. FEBS Letts., 1980; 111, 189-193. Hider RC, Drake AF, Inagaki ...
However, tamapin displaces Apamin in binding assays and is therefore a stronger toxin with respect to Apamin. SK 1 and SK 3 are ... Its sequence similarity to other toxins that can compete with the binding site of apamin is much lower. It is 31 amino acids ... Despite completely different sequences, Apamin (a bee venom toxin) and tamapin share at least in part, the same binding sites ... Tamapin-2 can also compete very effectively with apamin for binding to synaptosomes. The target of tamapin is the small ...
Gmachl, M; Kreil, G (1995). "The precursors of the bee Venom Constituents Apamin and MCD Peptide Are Encoded by two Genes in ... In addition to MCD peptide, melittin and apamin have also been identified in this venom and are also described as voltage- ... Although the MCD peptide sequence shows similarity with apamin, they have different toxic properties. MCD peptide belongs to a ...
In addition, SK channels (SK1-SK3) but not SK4 (IK) are sensitive to blockade by the bee toxin apamin, and the scorpion venoms ... Experiments using apamin have shown that specifically blocking SK channels can increase learning and long-term potentiation. In ... Blatz AL, Magleby KL (1986). "Single apamin-blocked Ca-activated K+ channels of small conductance in cultured rat skeletal ...
Zerrouk; Laraba-Djebari (2009). "Characterization of PO1 a new peptide ligand of the apamin-sensitive Ca2+ activated K+ channel ...
This toxin shows similarity in its physiological activity and binding specificity to apamin, but both toxins show no structural ... potent inhibitor of apamin binding from Leiurus quinquestriatus hebraeus venom". J. Biol. Chem. 263 (21): 10192-7. doi:10.1016/ ...
"Tetraethylammonium blockade of apamin-sensitive and insensitive Ca2+-activated K+ channels in a pituitary cell line." J. ... Inhibition of the electrogenic Na,K pump and Na,K-ATPase activity by tetraethylammonium, tetrabutylammonium, and apamin. ...
Jäger H, Adelman JP, Grissmer S (2000). "SK2 encodes the apamin-sensitive Ca2+-activated K+ channels in the human leukemic T ... 2004). "Calcium-dependent regulation of secretion in biliary epithelial cells: the role of apamin-sensitive SK channels". ...
... which act on apamin-sensitive Ca2+-activated K+ channels". European Journal of Biochemistry. 245 (2): 457-64. doi:10.1111/j. ... injection in mice it could very well compete to binding to the SKCa channel with the toxin iodinated apamin. Kv1.3 channels can ...
"Characterization of a new peptide from Tityus serrulatus scorpion venom which is a ligand of the apamin-binding site". FEBS ...
Unlike other toxins from the same family HsTx1 does not seem to affect the apamin-sensitive calcium-dependent potassium channel ...
It has a high affinity for the 125I-apamin acceptor-binding sites of the rat synaptosomal membranes (Ki = 1.45±0.22 nM) and ... Taicatoxin has an inhibitory effect by reducing the affinity of 125I-apamin for its acceptor and not by alteration of the ... 50 nM of taicatoxin blocks the apamin-sensitive after-hyperpolarizing slow tail K+ currents in rat chromaffin cells, but not ... blocks affinity-labeling of a 33-kDa 125I-apamin-binding polypeptide. Other neurotoxins that act on the calcium channels are ...
... termini and is readily blocked by apamin. The gene for KCa2.3, KCNN3, is located on chromosome 1q21. KCa2.3 is found in the ...
When the stimulus strength was reduced below the action potential threshold, apamin, a neurotoxin, was added to assess the ...
V. crabro venom contains neurotransmitters such as dopamine, serotonin, histamine and noradrenalineneurotoxin apamin, as well ...
On the other hand, TmTx does not seem to inhibit [125I] apamin binding to synaptic membranes in the rat brain or ionomycin- ...
This channel, the apamin sensitive, small conductance SK2 potassium channel, is activated by calcium that is likely released ...
... (MTX) blocks various K+ -channels: Apamin-sensitive small conductance Ca2+ - activated K+ channels (SK) Intermediate ...
Further protein components include apamin (2%), a neurotoxin, hyaluronidase (2%), which dilates blood vessels, increasing their ...
... apamin MeSH D20.888.065.115.580 - melitten MeSH D20.888.065.830 - scorpion venoms MeSH D20.888.065.830.150 - charybdotoxin MeSH ...
... induced relaxation by binding to and thereby opening their apamin-sensitive small conductance (SK) Calcium-activated potassium ...
... apamin MeSH D23.946.833.065.115.580 - melitten MeSH D23.946.833.065.830 - scorpion venoms MeSH D23.946.833.065.830.150 - ...
... is an element in bee venom. You can come into contact with apamin through bee venom, so the symptoms that are known are ... Apamin is an 18 amino acid globular peptide neurotoxin found in apitoxin (bee venom). Dry bee venom consists of 2-3% of apamin ... Apamin was first isolated by Habermann in 1965 from Apis mellifera, the Western honey bee. Apamin was named after this bee. Bee ... Apamin is the only neurotoxin acting purely on the central nervous system. The symptoms of apamin toxicity are not well known, ...
The LD50 of nicotine is 50 mg/kg for rats and 3 mg/kg for mice. 0.5-1.0 mg/kg can be a lethal dosage for adult humans, and 0.1 mg/kg for children.[19][20] However the widely used human LD50 estimate of 0.5-1.0 mg/kg was questioned in a 2013 review, in light of several documented cases of humans surviving much higher doses; the 2013 review suggests that the lower limit causing fatal outcomes is 500-1000 mg of ingested nicotine, corresponding to 6.5-13 mg/kg orally.[21] An accidental ingestion of only 6 mg may be lethal to children.[22] It is unlikely that a person would overdose on nicotine through smoking alone. The US Food and Drug Administration (FDA) stated in 2013: "There are no significant safety concerns associated with using more than one [over the counter] OTC [nicotine replacement therapy] NRT at the same time, or using an OTC NRT at the same time as another nicotine-containing product-including a cigarette."[23][24][25] Ingestion of nicotine pharmaceuticals, tobacco products, or ...
... biology)-induced relaxation by binding to and thereby opening their apamin-sensitive small conductance (SK) Calcium-activated ...
Apamin is an element in bee venom. You can come into contact with apamin through bee venom, so the symptoms that are known are ... Apamin is an 18 amino acid globular peptide neurotoxin found in apitoxin (bee venom). Dry bee venom consists of 2-3% of apamin ... Apamin was first isolated by Habermann in 1965 from Apis mellifera, the Western honey bee. Apamin was named after this bee. Bee ... Apamin is the only neurotoxin acting purely on the central nervous system. The symptoms of apamin toxicity are not well known, ...
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Categories: Apamin Image Types: Photo, Illustrations, Video, Color, Black&White, PublicDomain, CopyrightRestricted 4 images ...
Bram R, See AP, Amin-Hanjani S. Intervention for symptomatic vertebrobasilar disease. J Neurosurg Sci. 2021 Jan 22. [QxMD ...
Apamin (ap) blocks an initial component of the IAHP in all of the genotypes except SK2 Δ/Δ mice, which lack the apamin- ... 2B). In slices from wild-type mice, apamin blocked an early component of the IAHP and the apamin-sensitive component of the ... In particular, the IsAHP in mice lacking the least apamin-sensitive SK subunit, SK1, is similar to wild type and is not apamin ... It is interesting that SK2 channels, required for the apamin-sensitive ImAHP, may also be responsible for the effects of apamin ...
Melittin and apamin (Figure 1) were able to inhibit the growth of A. alternate sp. and A. pillows causing upper airway ... bee venom; antimicrobial properties; melittin; apamin; phospholipase A2 (PLA2). Key Contribution: Here, we critically review ... Apamin. A. alternate. NR. At 1 µg/mL inhibits 42.6% of interleukin (IL)-6 production. [3]. ... Shin, S.; Ye, M.; Choi, S.; Park, K. The effects of melittin and apamin on airborne Fungi-Induced chemical mediator and ...
MIN apa : MINeral name contains apa eg apatite.. *PDF 32-77 (PDF number contains 32-77) ...
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MIN apa : MINeral name contains apa eg apatite.. *PDF 32-77 (PDF number contains 32-77) ...
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These neurotoxins include agitoxin, charybdotoxin and margatoxin (scorpion stings), apamin (bee stings), and dendrotoxin (mamba ...
... apamin. Complete blockade was obtained with hydroxocobalamin or L-NAME+ charybdotoxin+apamin. 4. Repeated exposure to 100 nM BK ... Quinaprilat also relaxed vessels that, due to pretreatment with hydroxocobalamin or L-NAME+charybdotoxin+apamin, previously had ... apamin (both 100 nM), or the ACE inhibitor quinaprilat (10 microM). 3. BK and HT-BK dose-dependently relaxed preconstricted ...
Nitric Oxide Acts as a Volume Transmitter to Modulate Electrical Properties of Spontaneously Firing Neurons via Apamin- ... Nitric Oxide Acts as a Volume Transmitter to Modulate Electrical Properties of Spontaneously Firing Neurons via Apamin- ... Nitric Oxide Acts as a Volume Transmitter to Modulate Electrical Properties of Spontaneously Firing Neurons via Apamin- ... Nitric Oxide Acts as a Volume Transmitter to Modulate Electrical Properties of Spontaneously Firing Neurons via Apamin- ...
Perfusion with PP induced a TTX- and apamin-sensitive, concentration-dependent outward (22% of neurons) or inward current (21% ... Perfusion with PP induced a TTX- and apamin-sensitive, concentration-dependent outward (22% of neurons) or inward current (21% ... Perfusion with PP induced a TTX- and apamin-sensitive, concentration-dependent outward (22% of neurons) or inward current (21% ... Perfusion with PP induced a TTX- and apamin-sensitive, concentration-dependent outward (22% of neurons) or inward current (21% ...
The main components are peptides: melittin, apamin, peptide 401, adolapin, and protease inhibitors. Bee venom support the ...
apamin-SF.cif. 2015-11-25 11:47 1.1M. apamin.pdb. 2015-11-25 11:47 65K. ...
M. F. Shuba and I. A. Vladimirova, "Effect of apamin on the electrical response of smooth muscle to adenosine-5′-triphosphate ... I. A. Vladimirova and M. F. Shuba, "Effect of strychnine, hydrastatine, and apamin on synaptic transmission in smooth muscle ...
CARA MEMBUAT POMADE Sebenarnya membuat POMADE hampir bisa dilakukan oleh siapa saja, tidak perlu menjadi ahli kecantikan, gak perlu menjadi seorang hair stylist, ahli kimia dan sebagainya,semua lepas dari yang namanya embel-embel jabatan kompetensi (apalagi di jaman sekarang dimana media informasi mudah didapatkan dengan bantuan media internet salah satunya). Dan di internet pun sebenarnya banyak…
Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with ...
CARA MEMBUAT POMADE Sebenarnya membuat POMADE hampir bisa dilakukan oleh siapa saja, tidak perlu menjadi ahli kecantikan, gak perlu menjadi seorang hair stylist, ahli kimia dan sebagainya,semua lepas dari yang namanya embel-embel jabatan kompetensi (apalagi di jaman sekarang dimana media informasi mudah didapatkan dengan bantuan media internet salah satunya). Dan di internet pun sebenarnya banyak…
apamin. apitherapy. venom immunotherapy. Date de publication: jan-2019. Editeur: Science Domain International. ...
We conclude that in the rat LES, relaxation is mediated by NO and an apamin-sensitive mediator, and contraction primarily by ... We conclude that in the rat LES, relaxation is mediated by NO and an apamin-sensitive mediator, and contraction primarily by ... keywords = "Apamin, Interstitial cells of Cajal, Lower oesophageal sphincter, Nitric oxide, Ws/Ws rat, c-Kit", ... We conclude that in the rat LES, relaxation is mediated by NO and an apamin-sensitive mediator, and contraction primarily by ...
MIN apa : MINeral name contains apa eg apatite.. *PDF 32-77 (PDF number contains 32-77) ...
Influence of peptide conformation on oligosaccharide binding characteristics--a study using apamin-based chimeric peptide. C. W ...
These channels are sensitive to block by apamin (100 pM-10 nM), which distinguishes them from all other KCa channels. The group ...
The inhibitors of Ca2+-activated K+ channels charybdotoxin (0.5 x 10(-7) M) together with apamin (10(-6) M), and the cytochrome ... The inhibitors of Ca2+-activated K+ channels charybdotoxin (0.5 x 10(-7) M) together with apamin (10(-6) M), and the cytochrome ...
Apamin-sensitive, small-conductance, Ca2+-activated K + channels (SK channels) modulate neuronal excitability in CA1 neurons. ... Studies of SK channel knock-out mice reveal that of the three apamin-sensitive SK channel subunits (SK1-SK3), only SK2 subunits ... Studies of SK channel knock-out mice reveal that of the three apamin-sensitive SK channel subunits (SK1-SK3), only SK2 subunits ... Studies of SK channel knock-out mice reveal that of the three apamin-sensitive SK channel subunits (SK1-SK3), only SK2 subunits ...
Bram R, See AP, Amin-Hanjani S. Intervention for symptomatic vertebrobasilar disease. J Neurosurg Sci. 2021 Jan 22. [QxMD ...
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  • These neurotoxins include agitoxin, charybdotoxin and margatoxin (scorpion stings), apamin (bee stings), and dendrotoxin (mamba snake bites). (chemicool.com)
  • 2. Porcine coronary arteries (PCAs) were mounted in organ baths, preconstricted, and exposed to BK or the ACE-resistant BK analogue Hyp(3)-Tyr(Me)(8)-BK (HT-BK) with or without the NOS inhibitor L-NAME (100 microM), the NO scavenger hydroxocobalamin (200 microM), the Ca(2+)-dependent K(+)-channel blockers charybdotoxin+apamin (both 100 nM), or the ACE inhibitor quinaprilat (10 microM). (eur.nl)
  • pEC(50)'s were approximately 10 fold higher with quinaprilat, and approximately 10 fold lower with L-NAME or charybdotoxin+apamin. (eur.nl)
  • Complete blockade was obtained with hydroxocobalamin or L-NAME+ charybdotoxin+apamin. (eur.nl)
  • Quinaprilat also relaxed vessels that, due to pretreatment with hydroxocobalamin or L-NAME+charybdotoxin+apamin, previously had not responded to BK. (eur.nl)
  • Normal platelets contain three types of K+ channel, sensitive to the inhibitory actions of apamin (small-conductance calcium-dependent potassium channels), charybdotoxin (of less specificity, but probably intermediate-conductance calcium-dependent K+ channels), and α-dendrotoxin (voltage-sensitive K+ channels). (ox.ac.uk)
  • However, 86Rb+ efflux from the platelets of patients with Alzheimer-type dementia was not inhibited by either apamin or charybdotoxin. (ox.ac.uk)
  • This efflux was significantly inhibited by apamin (100 nmol/l), charybdotoxin (300 nmol/l) and alpha-dendrotoxin (100-200 nmol/l), blockers of SKCa channels, KCh channels and Kv channels respectively. (ox.ac.uk)
  • This efflux was significantly inhibited by apamin (100 nmol/l) and charybdotoxin (300 nmol/l). (ox.ac.uk)
  • Concomitant addition of l -NAME, apamin and charybdotoxin had no further effect. (thecannabisadvisory.com)
  • This was discovered because apamin and charybdotoxin applied in combination blocked EDHF responses, but iberiotoxin - a blocker of BKCa - was not able to substitute for charybdotoxin. (ox.ac.uk)
  • KT-5823-induced relaxations in small mesenteric arteries are greatly reduced by 35 mM K(+) or 50 nM charybdotoxin + 50 nM apamin, suggesting that endothelium-derived hyperpolarizing factor (EDHF) is the participating dilator. (ox.ac.uk)
  • Apamin is an 18 amino acid globular peptide neurotoxin found in apitoxin (bee venom). (wikipedia.org)
  • Dry bee venom consists of 2-3% of apamin. (wikipedia.org)
  • 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. (wikipedia.org)
  • Mellitin, Apamin, and a peptide that degranulates mast cells are unique to honeybee venom. (nzbees.net)
  • Apamin is also unique to bee venom (3%) and is a neurotoxin. (nzbees.net)
  • Alvarez-Fischer D, Noelker C, Vulinović F, Grünewald A, Chevarin C,Klein C, Oertel WH, Hirsch EC, Michel PP, Hartmann A (2013) Bee venom and its component apamin as neuroprotective agents in a Parkinson disease mouse model .PLoS One Apr 18;8(4):e61700. (movit.paris)
  • A research paper published in December 2016, The Journal of Microbiology by Md Bashir Uddin , Byeong-Hoon Lee , Chamilani stated that the bee venom contains 18 components with medicinal use including melittin (MLT), phospholipase A2 (PLA2), and apamin etc. (medium.com)
  • Influence of peptide conformation on oligosaccharide binding characteristics--a study using apamin-based chimeric peptide. (tbi.org.tw)
  • Apamin-sensitive, small-conductance, Ca 2+ -activated K + channels (SK channels) modulate neuronal excitability in CA1 neurons. (elsevier.com)
  • The blocker of ATP-modulated potassium channels (K(ATP)), glibenclamide (10 microM), and of small conductance calcium-activated potassium channels (SK(Ca)), apamin (30 nM), each failed to affect ODQ-sensitive or -resistant relaxations to DEA NONOate (n=3). (ox.ac.uk)
  • Carotid arteries from SHRSP and WKY did not contract to apamin (10-9 to 10"6 mol/L), an antagonist of the small conductance, calcium activated potassium channel. (elsevier.com)
  • Examination of transgenic mice, each lacking one of the three SK channel genes expressed in the CNS, reveals that mice without the SK2 subunit completely lack the apamin-sensitive component of the ImAHP in CA1 neurons, whereas the IsAHP is not different in any of the SK transgenic mice. (jneurosci.org)
  • Application of apamin to CA1 neurons increases excitability, which can be seen as a shortened interspike interval, especially early in a burst of action potentials, and increases the number of action potentials for a given current injection. (jneurosci.org)
  • In addition to contributing to the IAHP, apamin-sensitive channels in CA1 neurons also affect the induction of synaptic plasticity and memory encoding. (jneurosci.org)
  • Studies of SK channel knock-out mice reveal that of the three apamin-sensitive SK channel subunits (SK1-SK3), only SK2 subunits are necessary for the apamin-sensitive currents in CA1 hippocampal neurons. (elsevier.com)
  • To determine the specific influence of SK2 channels on hippocampal synaptic plasticity, learning, and memory, we used gene targeting through homologous recombination in embryonic stem cells to generate transgenic mice that overexpress SK2 subunits by 10-fold (SK2+/T). In these mice, the apamin-sensitive current in CA1 neurons was increased by approximately fourfold, relative to wild-type (WT) littermates. (elsevier.com)
  • Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM. (selleckchem.com)
  • The SK(Ca) channel blocker apamin (1 μM) enhanced the methacholine-induced catecholamine responses. (elsevier.com)
  • The facilitatory effect of apamin on the methacholine-induced catecholamine responses was not observed during treatment with the L-type Ca 2+ channel blocker nifedipine (3 μM) or Ca 2+ -free solution. (elsevier.com)
  • Finally, we sought to rescue the observed phenotype by administration of the SK channel blocker Apamin. (mxwbio.com)
  • By administration of the SK channel inhibitor Apamin, which has previously been shown to be neuroprotective in ALS MN, we were able to achieve beneficial effects on an electrophysiological as well as transcriptional level. (mxwbio.com)
  • Apamin, which selectively suppresses a component of the mAHP, increases neuronal excitability and facilitates the induction of synaptic plasticity at Schaffer collateral synapses and hippocampal-dependent learning. (jneurosci.org)
  • Blocking all SK channel subtypes with apamin facilitates the induction of hippocampal synaptic plasticity and enhances hippocampal learning. (elsevier.com)
  • Combined IK(Ca) (1 microM TRAM-34) and SK(Ca) (100 nM apamin) blockade partially inhibited NO-independent relaxations, with residual relaxations sensitive to BK(Ca) or cytochrome P-450 inhibition (100 nM iberiotoxin, and 20 microM 17-ODYA or 10 microM MS-PPOH). (ox.ac.uk)
  • Apamin selectively blocks SK channels, a type of Ca2+-activated K+ channel expressed in the central nervous system. (wikipedia.org)
  • Apamin was first isolated by Habermann in 1965 from Apis mellifera, the Western honey bee. (wikipedia.org)
  • The kinetics of labeled derivatives of apamin were studied in vitro and in vivo in mice by Cheng-Raude et al. (wikipedia.org)
  • Nifedipine did not affect the methacholine-induced catecholamine responses, but it inhibited the responses during treatment with apamin. (elsevier.com)
  • 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. (wikipedia.org)
  • Binding of apamin to SK channels is mediated by amino acids in the pore region as well as extracellular amino acids of the SK channel. (wikipedia.org)
  • These channels are sensitive to block by apamin (100 pM-10 nM), which distinguishes them from all other KCa channels. (axonmedchem.com)
  • Apamin was separated from the other compounds by gel filtration and ion exchange chromatography. (wikipedia.org)
  • These amino acids are involved in the binding of apamin to the Ca2+-activated K+ channel. (wikipedia.org)
  • The channel is blocked by apamin. (abcam.cn)
  • Strips from SD and +/+ rats, responded to electrical neuronal stimulation with a relaxation that was in part L-NNA and in part apamin sensitive, followed by a contraction which was decreased by atropine. (uab.cat)
  • In Ws/Ws rats, similar to +/+ rats, neurally mediated relaxation was L-NNA and apamin sensitive and the contraction was decreased by atropine. (uab.cat)
  • We conclude that in the rat LES, relaxation is mediated by NO and an apamin-sensitive mediator, and contraction primarily by acetylcholine. (uab.cat)
  • The peptides melittin, apamin, and mast cell degranulating (MCD) peptides are exclusive to bee venom. (buzzaboutbees.net)
  • Bee venom is composed of 30 different components including the anti-inflammatory peptides melittin, and apamin. (beehabitat.com)
  • It is extracted from bees' sting and contains 40 kinds of natural ingredients such as melittin, apamin, and phospholipase. (theshopaholicbeauty.com)
  • Further, apamin application increased the firing rate to current injections and completely abolished the difference of the firing rate between control and NMDM. (mtu.edu)
  • The present findings show that, using Schaffer collateral stimulation, the effects of SNX and apamin are not mutually exclusive and SNX increases EPSPs independent of SK channel activity. (elsevier.com)
  • L-NAME, charybdotoxin + apamin, KCl, and ouabain shifted the bradykinin concentration-response curve (CRC) ≈10-fold to the right BaCl2 did not exert additional effects on top of ouabain. (eur.nl)
  • Full blockade of bradykinin was obtained when combining L-NAME with charybdotoxin + apamin, KCl or ouabain + BaCl2. (eur.nl)
  • Charybdotoxin + apamin shifted the L-SNC and L-SNG CRCs, but not the D-SNC or SNAP CRCs, ≈5-fold to the right. (eur.nl)
  • 1. The contribution of Ca2+-activated K+ currents (IK,Ca) to the control of electrical excitability of motor nerve terminals and the control of acetylcholine release was assessed by studying the effects of the specific K(Ca) channel blocking toxins charybdotoxin and apamin. (strath.ac.uk)
  • 2. Charybdotoxin (20-300 nM), but not apamin (10 nM-2.5 microM), selectively reduced the amplitude of an IK,Ca unmasked by prior blockade of the delayed rectifier K+ current with 3,4-diaminopyridine (3,4-DAP). (strath.ac.uk)
  • Iberiotoxin + apamin, alone or on top of L-NAME, did not affect bradykinin, SNAP or L-SNC. (eur.nl)
  • Riluzole (10 uM) also effectively increased * Ca2+-activated K+ current (IK(Ca)) which could be reversed by * iberiotoxin (200 nM) and paxilline (1 uM), but not by apamin * (200 nM). (nih.gov)
  • Apamin, the small-conductance Ca2+-reliant K+ (SK) route blocker was utilized at a focus of 10 M. All antagonists and inhibitors had been put into the shower at least 1 h before the begin of documenting. (bicycletouringoncarfreepaths.org)
  • To evaluate the part of calcium-activated K+ channels, aortic rings were incubated with the selective blockers, IbTX (BKCa blocker) (Determine 2C, Desk 1) and Apamin (SKCa blocker) (Determine 2E, Table 1), and the nonspecific blockers, ChTX (KCa and Kv blocker) (Figure 2G, Table 1). (icbinhibitor.com)
  • Other potential targets of action of H2S on GI easy muscle include apamin-sensitive SK channels and delayed rectifier potassium channels [14], [15]. (rockstarsagainstliveearth.com)
  • AP5A-induced vasorelaxation was not inhibited by Ca 2+ - or ATP-dependent K + channel blockade with clotrimazole, apamin, or glibenclamide. (aspetjournals.org)
  • Ikonen S, Riekkinen P (1999) Effects of apamin on memory processing of hippocampal-lesioned mice. (yale.edu)
  • Oil-red O staining indicates that the inhibition of apamin in the condition significantly prevents intracellular lipid deposition. (blogspot.com)
  • Hexamethonium (55?mol?kg?1, i.v., plus infusion of 17?mol?h?1) NIBR189 SDF-5 abolished the apamin-induced, atropine-resistant colonic propulsion (97% inhibition) and decreased the amplitude from the atropine-resistant contractions (52% inhibition). (informationalwebs.com)
  • In atropine-treated pets (6?mol?kg?1, i.v., plus infusion of just one 1.8?mol?h?1), apamin (30?nmol?kg?1, i.v.) restored colonic propulsion (+416%) and improved the amplitude of contractions (+367% when compared with atropine only). (informationalwebs.com)
  • In charge pets, apamin (30?nmol?kg?1, i.v.) improved colonic propulsion (+84%) and improved the amplitude of contractions (+68%), when compared with the automobile. (informationalwebs.com)
  • In apamin- and atropine-pretreated pets, only the best (1?mol?kg?1) dosage of SR 140333 or Guys 11420 significantly decreased the amplitude of contractions. (informationalwebs.com)
  • The original bis-isoquinolinium derivatives were synthezised and evaluated using binding studies, electrophysiology, and molecular modeling and demonstrate the blocking potential of the apamin-sensitive after-hyperpolarization. (semanticscholar.org)
  • Both the basal and ionomycin-induced I sc were inhibited by basolateral Ba 2+, and approximately 58% of the basolateral K + current was apamin sensitive.These studies demonstrate that cholangiocytes exhibit robust Ca 2+ -stimulated secretion significantly greater in magnitude than that stimulated by cAMP. (epfl.ch)
  • Currents were Ca 2+ dependent and were inhibited by apamin and by Ba 2+. (epfl.ch)
  • Treatment with apamin significantly decreased the apoptotic macrophages by decreasing the expression of pro-apoptotic genes Bax, caspase-3 and PARP protein levels, as well as through increasing expression of anti-apoptotic genes Bcl-2 and Bcl-xL protein levels in the absence and presence of oxLDL. (blogspot.com)
  • Apamin (10(-7) m) inhibited the relaxations to the erythro-isomer (maximum relaxation = 1.2 +/- 5.6%) and increasing [K(+)](o) from 4.6 to 30 mm blocked relaxations to both isomers. (nih.gov)
  • It was figured, in anaesthetized guinea-pigs, endogenous tachykinins, performing through both NK1 and NK2 receptors, become non-cholinergic excitatory neurotransmitters to advertise an apamin-evoked reflex propulsive activity of the distal digestive tract. (informationalwebs.com)