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)
Compounds with a core of fused benzo-pyran rings.
Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.
Unstable isotopes of potassium that decay or disintegrate emitting radiation. K atoms with atomic weights 37, 38, 40, and 42-45 are radioactive potassium isotopes.
An antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
A guanidine that opens POTASSIUM CHANNELS producing direct peripheral vasodilatation of the ARTERIOLES. It reduces BLOOD PRESSURE and peripheral resistance and produces fluid retention. (Martindale The Extra Pharmacopoeia, 31st ed)
A potent direct-acting peripheral vasodilator (VASODILATOR AGENTS) that reduces peripheral resistance and produces a fall in BLOOD PRESSURE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p371)
Unstable isotopes of rubidium that decay or disintegrate emitting radiation. Rb atoms with atomic weights 79-84, and 86-95 are radioactive rubidium isotopes.
A derivative of the NIACINAMIDE that is structurally combined with an organic nitrate. It is a potassium-channel opener that causes vasodilatation of arterioles and large coronary arteries. Its nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.
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.
Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS.
A benzothiadiazine derivative that is a peripheral vasodilator used for hypertensive emergencies. It lacks diuretic effect, apparently because it lacks a sulfonamide group.
Drugs used to cause dilation of the blood vessels.
A family of iminourea derivatives. The parent compound has been isolated from mushrooms, corn germ, rice hulls, mussels, earthworms, and turnip juice. Derivatives may have antiviral and antifungal properties.
A group of compounds that are monomethyl derivatives of pyridines. (From Dorland, 28th ed)
That phase of a muscle twitch during which a muscle returns to a resting position.
A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.
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.
An important compound functioning as a component of the coenzyme NAD. Its primary significance is in the prevention and/or cure of blacktongue and PELLAGRA. Most animals cannot manufacture this compound in amounts sufficient to prevent nutritional deficiency and it therefore must be supplemented through dietary intake.
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.
Heteromultimers of Kir6 channels (the pore portion) and sulfonylurea receptor (the regulatory portion) which affect function of the HEART; PANCREATIC BETA CELLS; and KIDNEY COLLECTING DUCTS. KATP channel blockers include GLIBENCLAMIDE and mitiglinide whereas openers include CROMAKALIM and minoxidil sulfate.
An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.
The portion of the descending aorta proceeding from the arch of the aorta and extending to the DIAPHRAGM, eventually connecting to the ABDOMINAL AORTA.
A 37-amino acid residue peptide isolated from the scorpion Leiurus quinquestriatus hebraeus. It is a neurotoxin that inhibits calcium activated potassium channels.
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)
The cartilaginous and membranous tube descending from the larynx and branching into the right and left main bronchi.
10-carbon saturated monocarboxylic acids.
Organic compounds containing both the hydroxyl and carboxyl radicals.
The nonstriated involuntary muscle tissue of blood vessels.
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.
An element that is an alkali metal. It has an atomic symbol Rb, atomic number 37, and atomic weight 85.47. It is used as a chemical reagent and in the manufacture of photoelectric cells.
Electrodes with an extremely small tip, used in a voltage clamp or other apparatus to stimulate or record bioelectric potentials of single cells intracellularly or extracellularly. (Dorland, 28th ed)
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.
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
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 craniosacral division of the autonomic nervous system. The cell bodies of the parasympathetic preganglionic fibers are in brain stem nuclei and in the sacral spinal cord. They synapse in cranial autonomic ganglia or in terminal ganglia near target organs. The parasympathetic nervous system generally acts to conserve resources and restore homeostasis, often with effects reciprocal to the sympathetic nervous system.
One of a pair of thick-walled tubes that transports urine from the KIDNEY PELVIS to the URINARY BLADDER.
A volatile vasodilator which relieves ANGINA PECTORIS by stimulating GUANYLATE CYCLASE and lowering cytosolic calcium. It is also sometimes used for TOCOLYSIS and explosives.
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.
Negative ions or salts derived from bromic acid, HBrO3.
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)
The terms, expressions, designations, or symbols used in a particular science, discipline, or specialized subject area.
Freedom from exposure to danger and protection from the occurrence or risk of injury or loss. It suggests optimal precautions in the workplace, on the street, in the home, etc., and includes personal safety as well as the safety of property.
Unforeseen occurrences, especially injuries in the course of work-related activities.
Databases devoted to knowledge about specific chemicals.
Authoritative treatises on drugs and preparations, their description, formulation, analytic composition, physical constants, main chemical properties used in identification, standards for strength, purity, and dosage, chemical tests for determining identity and purity, etc. They are usually published under governmental jurisdiction (e.g., USP, the United States Pharmacopoeia; BP, British Pharmacopoeia; P. Helv., the Swiss Pharmacopoeia). They differ from FORMULARIES in that they are far more complete: formularies tend to be mere listings of formulas and prescriptions.
The application of drug preparations to the surfaces of the body, especially the skin (ADMINISTRATION, CUTANEOUS) or mucous membranes. This method of treatment is used to avoid systemic side effects when high doses are required at a localized area or as an alternative systemic administration route, to avoid hepatic processing for example.
Analogs or derivatives of prostaglandins F that do not occur naturally in the body. They do not include the product of the chemical synthesis of hormonal PGF.
A synthetic prostaglandin F2alpha analog. The compound has luteolytic effects and is used for the synchronization of estrus in cattle.
The pressure of the fluids in the eye.

Acetylcholine-induced relaxation in blood vessels from endothelial nitric oxide synthase knockout mice. (1/374)

1. Isometric tension was recorded in isolated rings of aorta, carotid, coronary and mesenteric arteries taken from endothelial nitric oxide synthase knockout mice (eNOS(-/-) mice) and the corresponding wild-type strain (eNOS(+/+) mice). The membrane potential of smooth muscle cells was measured in coronary arteries with intracellular microelectrodes. 2. In the isolated aorta, carotid and coronary arteries from the eNOS(+/+) mice, acetylcholine induced an endothelium-dependent relaxation which was inhibited by N(omega)-L-nitro-arginine. In contrast, in the mesenteric arteries, the inhibition of the cholinergic relaxation required the combination of N(omega)-L-nitro-arginine and indomethacin. 3. The isolated aorta, carotid and coronary arteries from the eNOS(-/-) mice did not relax in response to acetylcholine. However, acetylcholine produced an indomethacin-sensitive relaxation in the mesenteric artery from eNOS(-/-) mice. 4. The resting membrane potential of smooth muscle cells from isolated coronary arteries was significantly less negative in the eNOS(-/-) mice (-64.8 +/- 1.8 mV, n = 20 and -58.4 +/- 1.9 mV, n = 17, for eNOS(+/+) and eNOS(-/-) mice, respectively). In both strains, acetylcholine, bradykinin and substance P did not induce endothelium-dependent hyperpolarizations whereas cromakalim consistently produced hyperpolarizations (- 7.9 +/- 1.1 mV, n = 8 and -13.8 +/- 2.6 mV, n = 4, for eNOS(+/+) and eNOS(-/-) mice, respectively). 5. These findings demonstrate that in the blood vessels studied: (1) in the eNOS(+/+) mice, the endothelium-dependent relaxations to acetylcholine involve either NO or the combination of NO plus a product of cyclo-oxygenase but not EDHF; (2) in the eNOS(-/-) mice, NO-dependent responses and EDHF-like responses were not observed. In the mesenteric arteries acetylcholine releases a cyclo-oxygenase derivative.  (+info)

Differential effects of pinacidil, cromakalim, and NS 1619 on electrically evoked contractions in rat vas deferens. (2/374)

AIM: To compare the inhibitory action of electrically evoked contractions of rat epididymal vas deferens by pinacidil (Pin), cromakalim (Cro), and NS 1619. METHODS: Monophasic contractions were evoked by electric field stimulation in rat isolated epididymal half of vas deferens. RESULTS: Newly developed ATP-sensitive K+ channel openers, Pin and Cro, concentration-dependently reduced the electrically evoked (0.3 Hz, 1 ms pulse duration, 60 V) contractions and glibenclamide but not charybdotoxin antagonized the inhibitory effects of both agents. Pin shifted the concentration-response curve for norepinephrine to the right with reducing the magnitude of the maximum contraction in a glibenclamide-sensitive fashion. The large-conductance Ca(2+)-activated K+ channel opener, NS 1619, inhibited the electrically evoked contractions in a concentration-dependent manner. Charybdotoxin (100 nmol.L-1) partially reduced the effect of NS 1619 but glibenclamide (10 mumol.L-1) showed no effect. None of these 3 agents affected the basal tension. CONCLUSION: Both ATP-sensitive and Ca(2+)-activated K+ channels presented in vas deferens smooth muscles involved in regulation of muscle contractility.  (+info)

Role of K+ channels in A2A adenosine receptor-mediated dilation of the pressurized renal arcuate artery. (3/374)

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)

ATP-sensitive potassium channels regulate in vivo dopamine release in rat striatum. (4/374)

ATP-sensitive K+ channels (K(ATP)) are distributed in a variety of tissues including smooth muscle, cardiac and skeletal muscle, pancreatic beta-cells and neurons. Since K(ATP) channels are present in the nigrostriatal dopamine (DA) pathway, the effect of potassium-channel modulators on the release of DA in the striatum of conscious, freely-moving rats was investigated. The extracellular concentration of DA was significantly decreased by the K(ATP)-channel opener (-)-cromakalim but not by diazoxide. (-)-Cromakalim was effective at 100 and 1000 microM concentrations, and the maximum decrease was 54% below baseline. d-Amphetamine significantly increased extracellular DA levels at the doses of 0.75 and 1.5 mg/kg, s.c. with a 770% maximum increase. (-)-Cromakalim had no effect on d-amphetamine-induced DA release, while glyburide, a K(ATP) blocker, significantly potentiated the effects of a low dose of d-amphetamine. These data indicate that K+ channels present in the nigrostriatal dopaminergic terminals modulate basal release as well as evoked release of DA.  (+info)

Thiopental and propofol impair relaxation produced by ATP-sensitive potassium channel openers in the rat aorta. (5/374)

ATP-sensitive potassium channel openers are used as vasodilators in the treatment of cardiovascular disorders. The effects of i.v. anaesthetics on arterial relaxation induced by ATP-sensitive potassium channel openers have not been studied. Therefore, in this study, we have examined if thiopental (thiopentone) and propofol affect the vascular response to the ATP-sensitive potassium channel openers, cromakalim and pinacidil, in the isolated rat aorta. Rings of rat thoracic aortas without endothelium were suspended for isometric force recording. Concentration-response curves were obtained in a cumulative manner. During submaximal contractions with phenylephrine 0.3 mumol litre-1, relaxation after cromakalim 0.1-30 mumol litre-1, pinacidil 0.1-30 mumol litre-1 and papaverine 0.1-300 mumol litre-1 was demonstrated. Thiopental 30-300 mumol litre-1, propofol 10-100 mumol litre-1, 10% Intralipid 45 microliters or glibenclamide 5 mumol litre-1 were applied 15 min before addition of phenylephrine. During contractions with phenylephrine, cromakalim and pinacidil induced concentration-dependent relaxation. A selective ATP-sensitive potassium channel antagonist, glibenclamide 5 mumol litre-1, abolished this relaxation, whereas it did not affect relaxation produced by papaverine. Thiopental concentrations > 30 mumol litre-1 significantly impaired relaxation produced by cromakalim or pinacidil. Propofol concentrations > 10 mumol litre-1 also significantly reduced relaxation produced by cromakalim or pinacidil, whereas Intralipid was ineffective. Thiopental 300 mumol litre-1 and propofol 100 mumol litre-1 did not alter relaxation produced by papaverine. These results suggest that the i.v. anaesthetics, thiopental and propofol, impaired vasodilatation mediated by ATP-sensitive potassium channels in vascular smooth muscle cells.  (+info)

Effects of nicorandil as compared to mixtures of sodium nitroprusside and levcromakalim in isolated rat aorta. (6/374)

1. The contribution of the relaxant mechanisms of nicorandil (NIC) were analysed by comparing its effects with those of sodium nitroprusside (SNP), levcromakalim (LEM) and mixtures (1:10, 1:30 and 1:100) of SNP:LEM in isolated endothelium-denuded rat aorta. 2. In rings precontracted with KCl (25 mM), the relative inhibitory potency of the soluble guanylate cyclase inhibitor ODQ and the K(ATP) channel inhibitor glibenclamide (GLI) on SNP:LEM mixtures showed a good correlation with the relative proportion of SNP and LEM in the mixtures. Furthermore, the degree of the inhibition by ODQ and GLI of the effects of the 1:30 SNP:LEM mixture varied as a function of the relative potency of SNP and LEM in KCl-, noradrenaline- (NA) or NA plus nifedipine-treated arteries. 3. The inhibitory effects of ODQ, GLI and ODQ plus GLI on NIC-induced relaxation was similar to that for the 1:30 SNP:LEM mixture in NA plus nifedipine-contracted arteries, but the inhibition of GLI or ODQ plus GLI was smaller in KCl-contracted arteries. 4. In conclusion, the relative importance of activation of the cyclic GMP pathway and K(ATP) channel opening in mixtures of SNP and LEM could be predicted by the proportion of the drugs in the mixtures and by the relative potency of SNP vs LEM in different experimental conditions. Furthermore, the present results suggest that besides these two mechanisms, a third ODQ- and GLI-insensitive mechanism, possibly involving Ca2+ channel blockade, also participates in the relaxant effects of NIC in KCl-induced contractions.  (+info)

Differential effects of lidocaine and mexiletine on relaxations to ATP-sensitive K+ channel openers in rat aortas. (7/374)

BACKGROUND: In cardiac myocytes, lidocaine reduces but mexiletine increases adenosine triphosphate (ATP)-sensitive K+ currents, suggesting that these class Ib antiarrhythmic drugs may differentially modify the activity of ATP-sensitive K+ channels. The effects of lidocaine and mexiletine on arterial relaxations induced by K+ channel openers have not been studied. Therefore, the current study was designed to evaluate whether lidocaine and mexiletine may produce changes in relaxations to the ATP-sensitive K+ channel openers cromakalim and pinacidil in isolated rat thoracic aortas. METHODS: Rings of rat thoracic aortas without endothelia were suspended for isometric force recording. Concentration-response curves were obtained in a cumulative fashion. During submaximal contractions to phenylephrine (3 x 10(-7) M), relaxations to cromakalim (10(-7) to 3 x 10(-5) M), pinacidil (10(-7) to 3 x 10(-5) M), or diltiazem (10(-7) to 3 x 10(-4) M) were obtained. Lidocaine (10(-5) to 3 x 10(-4) M), mexiletine (10(-5) to 10(-4) M) or glibenclamide (5 x 10(-6) M) was applied 15 min before addition of phenylephrine. RESULTS: During contractions to phenylephrine, cromakalim and pinacidil induced concentration-dependent relaxations. A selective ATP-sensitive K+ channel antagonist, glibenclamide (5 x 10(-6) M), abolished these relaxations, whereas it did not alter relaxations to a voltage-dependent Ca2+ channel inhibitor, diltiazem (10(-7) to 3 x 10(-4) M). Lidocaine (more than 10(-5) M) significantly reduced relaxations to cromakalim or pinacidil in a concentration-dependent fashion, whereas lidocaine (3 x 10(-4) M) did not affect relaxations to diltiazem. In contrast, mexiletine (more than 10(-5) M) significantly augmented relaxations to cromakalim or pinacidil. Glibenclamide (5 x 10(-6) M) abolished relaxations to cromakalim or pinacidil in arteries treated with mexiletine (10(-4) M). CONCLUSIONS: These results suggest that lidocaine impairs but mexiletine augments vasodilation mediated by ATP-sensitive K+ channels in smooth muscle cells.  (+info)

Inhibitory effect of 4-aminopyridine on responses of the basilar artery to nitric oxide. (8/374)

1. Voltage-dependent K+ channels are present in cerebral arteries and may modulate vascular tone. We used 200 microM 4-aminopyridine (4-AP), thought to be a relatively selective inhibitor of voltage-dependent K+ channels at this concentration, to test whether activation of these channels may influence baseline diameter of the basilar artery and dilator responses to nitric oxide (NO) and cyclic GMP in vivo. 2. Using a cranial window in anaesthetized rats, topical application of 4-AP to the basilar artery (baseline diameter = 240+/-5 microm, mean +/- s.e.mean) produced 10+/-1% constriction. Sodium nitroprusside (a NO donor), acetylcholine (which stimulates endothelial release of NO), 8-bromo cyclic GMP (a cyclic GMP analogue), cromakalim (an activator of ATP-sensitive K+ channels) and papaverine (a non-NO, non-K+ channel-related vasodilator) produced concentration-dependent vasodilator responses that were reproducible. 3. Responses to 10 and 100 nM nitroprusside were inhibited by 4-AP (20+/-4 vs 8+/-2% and 51+/-5 vs 33+/-5%, respectively, n=10; P<0.05). Responses to acetylcholine and 8-bromo cyclic GMP were also partially inhibited by 4-AP. In contrast, 4-AP had no effect on vasodilator responses to cromakalim or papaverine. These findings suggest that NO/cyclic GMP-induced dilator responses of the basilar artery are selectively inhibited by 4-aminopyridine. 4. Responses to nitroprusside were also markedly inhibited by 10 microM 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (an inhibitor of soluble guanylate cyclase; 16+/-4 vs 1+/-1% and 44+/-7 vs 7+/-1%; n=10; P<0.05). 5. Thus, dilator responses of the rat basilar artery to NO appear to be mediated by activation of soluble guanylate cyclase and partially by activation of a 4-aminopyridine-sensitive mechanism. The most likely mechanism would appear to be activation of voltage-dependent K+ channels by NO/cyclic GMP.  (+info)

TY - JOUR. T1 - Cromakalim and cicletanine against pacing-induced myocardial ischemia in conscious rabbits. AU - Szilvássy, Z.. AU - Koltai, Matyas. AU - Ferdinándy, P.. AU - Jakab, Ildiko. AU - Lonovics, J.. AU - Tarrade, Thierry. AU - Allard, Michel. AU - Braquet, Pierre G.. PY - 1994. Y1 - 1994. N2 - Myocardial ischemia assessed by intracavital ST-segment elevation, shortening of ventricular effective refractory period (VERP), and increase in left ventricular end-diastolic pressure (LVEDP) was provoked by ventricular overdrive pacing (VOP) in conscious rabbits. Cromakalim (10 μg/kg), an ATP-sensitive K+ channel opener, and cicletanine (30 mg/kg), a cGMP-phosphodiesterase inhibitor, reduced VOP-induced ST-segment elevation and LVEDP-increase. Under resting conditions, cromakalim lowered blood pressure, increased heart rate (HR), and shortened VERP, whereas cicletanine decreased HR, prolonged VERP without changing blood pressure. Co-administration of cromakalim and cicletanine additively ...
Cromakalim: 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)
Cromakalim | C16H18N2O3 | CID 443423 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
The effects of trans-5,6-dihydro-6-hydroxy-5,5-dimethyl-2-nitro-7-(2-oxopiperidin -1-yl)-7H- thieno[3,2-b]pyran (RWJ 26629) were compared with those of the standard potassium channel opener cromakalim and several standard calcium channel blockers. RWJ 26629 lowered the mean arterial blood pressure in conscious spontaneously hypertensive (ED30 = 10 micrograms/kg p.o. or 8 micrograms/kg i.v.) and renal hypertensive (15 ...
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Cromakalim (INN) is a potassium channel-opening vasodilator. The active isomer is levcromakalim. It acts on ATP-sensitive potassium channels and so causes membrane hyperpolarization. It can be used to treat hypertension as it will relax vascular smooth muscle to lower blood pressure. Hyperpolarisation of smooth muscle cell membranes pulls their membrane potential away from the threshold, so making it more difficult to excite them and thereby cause contraction. Reaction of 4-cyanophenol (4-Hydroxybenzonitrile) with 2-hydroxy-2-methyl-3-butyne under PTC probably proceeds to initial formation of a propargyl carbocation. The course of the reaction can be envisaged by assuming that this then attacks the aromatic ring; the resulting allylic cation can then capture the adjacent phenol oxygen and thus form the observed product (3). Treatment of that product with aqueous NBS leads to the addition of the elements of hypobromous acid and formation of the bromohydrin (4) as a mixture of the trans ...
The invention provides methods for determining the ability of compounds to regulate lipogenesis and lipolysis by acting as a sulfonylurea-1 (SUR 1) potassium channel activator, an adipocyte potassium channel activator, an SUR 1 antagonist, and an adipocyte specific SUR 1 antagonist. The present invention recognizes the presence of the sulfonylurea receptor in adipocytes and its utility in identifying compounds and in regulating lipogenesis and lipolysis.
Toxins that block voltage-dependent K(+) channels and those that modify Na(+) channel gating exhibit positive inotropic effect on skeletal muscle. We compared the effect of the venom of Tityus cambridgei (Tc) and Tityus serrulatus (Ts) scorpions on mouse diaphragm force, in vitro. In indirect and direct (using D-tubocurarine 7.3 mu M) stimulation, Tc, 10 mu g/mL increased the contractile force, an effect prevented by tetrodotoxin (TTX) while Ts, 0.5 mu g/mL, potentiated only indirectly stimulated diaphragm, thus indicating its activity is mainly mediated through acetylcholine release from nerve terminal. This effect is prevented by TTX and attenuated by the K(+) channel opener cromakalim. In conclusion, our data show that while the positive inotropic effect of both venoms appears associated to the activity of Na(+) and K(+) channels, only Tc venom acts also directly on skeletal muscle. This finding call for further studies on Tc venom to identify the toxin responsible for its direct inotropic ...
Purpose : To evaluate the pharmacologic and safety parameters of CKLP1 following topical application in hound dog eyes. Methods : Optimal concentration of CKLP1 for reduction of IOP was established in female hound dogs (n=5) by topical application to the eye with CKLP1 (5-20 mM). Following washout (14 days), the dogs were treated with the optimal dose once daily for 60 consecutive days. IOP was measured 3 times daily (1, 4 and 23 hours post treatment), 3-7 times per week. Blood pressure measurements were recorded using a tail cuff, once daily, 3-5 times per week. For pharmacokinetic studies, both eyes were treated with CKLP1 for 8 consecutive days. Blood samples were collected on days 1, 4 and 8 and concentration of CKLP1 and its parent compound levcromakalim were evaluated in the plasma by LC MS/MS. Necropsy was performed on all animals and systemic effects of drug administration were histologically evaluated in 40 different tissue samples from each animal. Results : The 10 mM topical dose of ...
Experimental and clinical studies have provided mechanistic evidence to support and explain the findings of the RCTs. Testosterone is a rapid‑onset arterial vasodilator within the coronary circulation and other vascular beds including the pulmonary vasculature and can reduce the overall peripheral systemic vascular resistance. Evidence has demonstrated that testosterone mediates this effect on vascular reactivity through calcium channel blockade (L‑calcium channel) and stimulates potassium channel opening by direct nongenomic mechanisms. Testosterone also stimulates repolarization of cardiac myocytes by stimulating the ultra‑rapid potassium channel‑operated current. Testosterone improves cardiac output, functional exercise capacity, VO2max and vagally mediated arterial baroreceptor cardiac reflex sensitivity in chronic heart failure. Independent of the benefit of testosterone on cardiac function, testosterone substitution may also increase skeletal muscle glucose metabolism and enhance ...
[150 Pages Report] Check for Discount on 2016 Minoxidil sulphate (CAS 83701-22-8) Industry Market Report report by Prof Research. The Global and Chinese Minoxidil sulphate Industry, 2011-2021 Market...
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The 203/266 Replacement Part Kit is for the electric can opener. The Kit contains 1 gear, 1 knife and 1 stud. Make sure the can opener is performing a
The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses
The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses
(2015) Sun et al. Frontiers in Neurology. High dose sodium salicylate causes moderate, reversible hearing loss and tinnitus. Salicylate-induced hearing loss is believed to arise from a reduction in the electromotile response of outer hair cells (OHCs) and/or reduction of KCNQ4 potassium currents ...
Effects of KRN4884 (5-amino-,i,N,/i,-[2-(2-chlorophenyl)ethyl]-,i,N,/i,-cyano-3-pyridinecarboxamidine), a novel K,sup,+,/sup, channel opener, on ionic currents were examined in rabbit femoral arterial myocytes (RFAMs). Under whole-cell clamp conditions where cells were superfused with 5.9 mM K,sup,+,/sup, bathing solution, KRN4884 elicited an outward current at −30 mV. KRN4884-induced current had a reversal potential of −78 mV and was abolished by application of glibenclamide (glib). KRN4884 was approximately 43 times more potent than levcromakalim in activating an ATP-sensitive K,sup,+,/sup, current (I,sub,K-ATP,/sub,). On the other hand, KRN4884 affected neither voltage-dependent Ca,sup,2+,/sup, nor delayed rectifier K,sup,+,/sup, channel currents. In the inside-out patch clamp configuration where cells were superfused with the symmetrical 140 mM K,sup,+,/sup, solution, KRN4884 activated 47 pS K,sup,+,/sup, channels in the presence of adenosine diphosphate. Similar 47 pS K,sup,+,/sup, ...
Lee Sang Eok , Han Ji Young , Kim Hyun Woo , Yang In Jun , Xu Wen-Xie , Lee Sang Jin , Kim Young Chul , Yun Hyo-Yung , Kim Dae Hoon , Son Seung Myeung , Choi Song-Yi , You Ra Young , Kim Chan Hyung , Choi Woong , Kim Hun Sik , Lim Yung Ji … channel opener, suppressed contractions to 30% (basal tone to −0.2 g) of the control. … The inhibitory effect of pinacidil on contraction was reversed to 59% of the control by glibenclamide (20 μM), a K,sub,ATP,/sub, … Pinacidil also inhibited the acetylcholine (ACh)-induced tonic and phasic contractions in a glibenclamide-sensitive manner (42% and 6% of the control, respectively). … Journal of Smooth Muscle Research 56(0), 29-45, 2020 J-STAGE ...
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TY - JOUR. T1 - The energetic state within hibernating myocardium is normal during dobutamine despite inhibition of ATP-dependent potassium channel opening with glibenclamide. AU - McFalls, Edward O.. AU - Kelly, Rosemary F.. AU - Hu, Qingsong. AU - Mansoor, Abdul. AU - Lee, Joseph. AU - Kuskowski, Michael. AU - Sikora, Joseph. AU - Ward, Herbert B.. AU - Zhang, Jianyi. PY - 2007/11. Y1 - 2007/11. N2 - Within hibernating myocardium, it is uncertain whether a normal energetic state is present at baseline and whether maintaining that energy state during a catecholamine challenge is dependent on ATP-dependent potassium channel opening. In this study, 16 swine underwent a thoracotomy with placement of an external constrictor on the left anterior descending coronary artery (LAD) (hibernation model). Seven additional swine underwent a sham operation. At 10 wk, the myocardial energetic state in the LAD region was assessed by 31P-NMR spectroscopy, and the ratio of phosphocreatine to ATP (PCr/ATP) was ...
There has been much recent interest in the roles played by smooth-muscle K+ channels in protecting cells against ischemic and anoxic insults and in therapeutic vaso- and bronchodilation (Buckingham 1990; Longmore & Weston 1990). A K+ channel, which is uniquely sensitive to cytoplasmic ATP (KATP), has been identified as a likely candidate for mediating these important functions (Standen et al. 1989). We now show, by using electrophysiological techniques in three different types of smooth muscle, that a large-conductance voltage and Ca2+ -sensitive channel, otherwise indistinguishable from the large-conductance Ca2+ -activated K+ channel (BK channel), is also sensitive to cytoplasmic ATP and cromakalim. ATP, in a dose-dependent manner, decreased the probability of channel opening (P0) of rabbit aortic, rabbit tracheal and pig coronary artery BK channels with a K1 of 0.2-0.6mM. Cromakalim, 10 μM, partially reversed the ATP induced inhibition and increased P0. Our observations raise the possibility ...
McCloskey, Conor, Bailey, Elizabeth H., Zhang, J. (Jie), Shmygol, Anatoly, Thornton, Steven, Catalano, Roberto D., England, Sarah, Rada, Cara and Blanks, Andrew M. (2011) The novel potassium channel Kir7.1 is a critical component of uterine quiescence in mice and human. Reproductive Sciences, Vol.18 (No.3). 159A-159A ...
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Synopsis Nicorandil belongs to the class of compounds known as potassium channel activators which are characterised by their arterial vasodilator properties. In addition, nicorandil has venodilating...
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Idiopathic generalized epilepsies account for about 40% of epilepsy up to age 40 and commonly have a genetic basis. One type is benign familial neonatal convulsions (BFNC), a dominantly inherited disorder of newborns. We have identified a sub-microscopic deletion of chromosome 20q13.3 that co-segreg …
Hydrogen peroxide and peroxynitrite induce relaxations via ATP-sensitive K+ channels, indicating that oxygen-derived free radicals may activate these channels. Levels of free radicals are increased throughout the arterial wall in animal models of atherosclerosis, and therefore, vasorelaxation via ATP-sensitive K+ channels may be augmented in chronic hypertension. The present study was designed to determine whether relaxations to an ATP-sensitive K+ channel opener, levcromakalim, are increased in the aorta from spontaneously hypertensive rats (SHR) and whether free radical scavengers reduce these relaxations. Rings of aortas without endothelium taken from age-matched Wistar-Kyoto rats (WKY) and SHR were suspended for isometric force recording. Relaxations to levcromakalim (10(-8) to 10(-5) M), which are abolished by glibenclamide (10(-5) M), were augmented in the aorta from SHR, compared to those in the aorta from WKY. In the aorta from SHR, catalase (1200 U/ml), but neither superoxide dismutase (150 U
Read Kinetic Analysis of the Inhibitory Effect of Glibenclamide on KATP Channels of Mammalian Skeletal Muscle, The Journal of Membrane Biology on DeepDyve, the largest online rental service for scholarly research with thousands of academic publications available at your fingertips.
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Tue May 19 2020 Hans Petter Jansson ,[email protected], - nss-fips-aes-keywrap-post.patch: Add AES Keywrap POST. - nss-fips-constructor-self-tests.patch: Accept EACCES in lieu of ENOENT when trying to access /proc/sys/crypto/fips_enabled (bsc#1170908). * Sun Apr 26 2020 Hans Petter Jansson ,[email protected], - nss-fips-constructor-self-tests.patch: Add Softoken POSTs for new DSA and ECDSA hash-and-sign update functinos. * Fri Apr 24 2020 Hans Petter Jansson ,[email protected], - nss-fips-combined-hash-sign-dsa-ecdsa.patch: Add pairwise consistency check for CKM_SHA224_RSA_PKCS. Remove ditto checks for CKM_RSA_PKCS, CKM_DSA and CKM_ECDSA, since these are served by the new CKM_SHA224_RSA_PKCS, CKM_DSA_SHA224, CKM_ECDSA_SHA224 checks. - nss-fips-constructor-self-tests.patch: Replace bad attempt at unconditional nssdbm checksumming with a dlopen(), so it can be located consistently and perform its own self-tests. * Tue Apr 21 2020 Hans Petter Jansson ,[email protected], - Add ...
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Glibenclamide Tablet is a medicine that is used for the treatment of Type 2 Diabetes Mellitus and other conditions. Glibenclamide Tablet contains Glibenclamide
BAYK 8644 is a L-type Ca2+ channel activator (EC50 = 17.3 nM). BAYK 8644 has positive inotropic, vasoconstrictive and behavioral effects in vivo.
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Iptakalim was unable to open pancreatic β-cell KATP channels, perhaps due to the presence of the SUR1, instead of the SUR2, subunit in these cells. Moreover, an intriguing finding was that iptakalim closed pancreatic β-cell-type KATP channels. It has been reported that PNU-99963, a nonsulfonylurea-based KATP channel inhibitor that has a structure similar to the KATP channel opener pinacidil, inhibits β-cell KATP channels (Cui et al., 2003). Structurally, iptakalim is also similar to the core portion of pinacidil; therefore, it is possible that KATP channel opener analogs with such a structure can inhibit KATP channels. Iptakalim may directly block β-cell KATP channels by acting on the Kir6.2 subunit (or some closely associated regulatory proteins). It is well documented that some KATP channel modulators, such as nicorandil, pinacidil, and glibenclamide, regulate KATP channel activity by targeting the regulating subunit SUR (Gribble and Ashcroft, 2000a; Hansen, 2006), whereas others (e.g., ...
The family of potassium channel openers regroups drugs that share the property of activating adenosine triphosphate-sensitive potassium (K(ATP)) channels, metabolic sensors responsible for adjusting membrane potential-dependent functions to match cellular energetic demands. K(ATP) channels, widely r …
Define glibenclamide. glibenclamide synonyms, glibenclamide pronunciation, glibenclamide translation, English dictionary definition of glibenclamide. n. See glyburide. American Heritage® Dictionary of the English Language, Fifth Edition. Copyright © 2016 by Houghton Mifflin Harcourt Publishing Company....
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The IUPHAR/BPS Guide to Pharmacology. nicorandil ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
The IUPHAR/BPS Guide to Pharmacology. nicorandil ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
"Response of guinea pig smooth and striated urethral sphincter to cromakalim, prazosin, nifedipine, nitroprusside, and ...
Traditional Bangladeshi healers use the bark as an antidiarrhoeal as it contains an antispasmodic similar to cromakalim. The ...
... cromakalim MeSH D03.438.150.500 - ellagic acid MeSH D03.438.150.600 - hematoxylin MeSH D03.438.150.909 - vitamin e MeSH D03.438 ... cromakalim MeSH D03.830.219.500 - ellagic acid MeSH D03.830.219.600 - hematoxylin MeSH D03.830.219.909 - vitamin e MeSH D03.830 ... cromakalim MeSH D03.383.129.578.399 - maleimides MeSH D03.383.129.578.399.418 - ethylmaleimide MeSH D03.383.129.578.617 - ...
Crolom cromakalim (INN) cromitrile (INN) cromoglicate lisetil (INN) cromoglicic acid (INN) Cromoptic cronidipine (INN) ...
... (INN) is a potassium channel-opening vasodilator. The active isomer is levcromakalim. It acts on ATP-sensitive ...
... is a member of the sodium channel blocking class of antiepileptic drugs.[60] This may suppress the release of glutamate and aspartate, two of the dominant excitatory neurotransmitters in the CNS.[61] It is generally accepted to be a member of the sodium channel blocking class of antiepileptic drugs,[62] but it could have additional actions since it has a broader spectrum of action than other sodium channel antiepileptic drugs such as phenytoin and is effective in the treatment of the depressed phase of bipolar disorder, whereas other sodium channel blocking antiepileptic drugs are not, possibly on account of its sigma receptor activity. In addition, lamotrigine shares few side-effects with other, unrelated anticonvulsants known to inhibit sodium channels, which further emphasises its unique properties.[63] It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and ...
The hormone prolactin stimulates lactation (production of breast milk). Dopamine, released by the hypothalamus stops the release of prolactin from the pituitary gland. Domperidone, by acting as an anti-dopaminergic agent, results in increased prolactin secretion, and thus promotes lactation (that is, it is a galactogogue). In some nations, including Australia, domperidone is used off-label, based on uncertain and anecdotal evidence of its usefulness, as a therapy for mothers who are having difficulty breastfeeding.[24][25] In the United States, domperidone is not approved for this or any other use.[26][27] A study called the EMPOWER trial was designed to assess the effectiveness and safety of domperidone in assisting mothers of preterm babies to supply breast milk for their infants.[28] The study randomized 90 mothers of preterm babies to receive either domperidone 10 mg orally three times daily for 28 days (Group A) or placebo 10 mg orally three times daily for 14 days followed by domperidone ...
... (DHP) is a molecule based upon pyridine, and the parent of a class of molecules that have been semi-saturated with two substituents replacing one double bond. They are particularly well known in pharmacology as L-type calcium channel blockers, used in the treatment of hypertension. Compared with certain other L-type calcium channel blockers (for example those of the phenylalkylamine class such as verapamil) that have significant action at the heart, they are relatively vascular selective in their mechanism of action in lowering blood pressure. ...
InChI=1S/C20H27N5O5S/c1-15-14-18(23-30-15)19(26)21-11-10-16-6-8-17(9-7-16)31(28,29)24-20(27)22-25-12-4-2-3-5-13-25/h6-9,14H,2-5,10-13H2,1H3,(H,21,26)(H2,22,24,27) ...
... (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain.[1] It is not effective for absence or myoclonic seizures.[1] It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder.[3][1] Carbamazepine appears to work as well as phenytoin and valproate for focal and generalised seizures.[4] Common side effects include nausea and drowsiness.[1] Serious side effects may include skin rashes, decreased bone marrow function, suicidal thoughts, or confusion.[1] It should not be used in those with a history of bone marrow problems.[1] Use during pregnancy may cause harm to the baby; however, stopping the medication in pregnant women with seizures is not recommended.[1] Its use during breastfeeding is not recommended.[1] Care should be taken in those with either kidney or liver problems.[1] Carbamazepine was discovered in 1953 by Swiss chemist Walter ...
A channel that is "inwardly-rectifying" is one that passes current (positive charge) more easily in the inward direction (into the cell) than in the outward direction (out of the cell). It is thought that this current may play an important role in regulating neuronal activity, by helping to stabilize the resting membrane potential of the cell. By convention, inward current (positive charge moving into the cell) is displayed in voltage clamp as a downward deflection, while an outward current (positive charge moving out of the cell) is shown as an upward deflection. At membrane potentials negative to potassium's reversal potential, inwardly rectifying K+ channels support the flow of positively charged K+ ions into the cell, pushing the membrane potential back to the resting potential. This can be seen in figure 1: when the membrane potential is clamped negative to the channel's resting potential (e.g. -60 mV), inward current flows (i.e. positive charge flows into the cell). However, when the ...
... also binds to and blocks α2δ subunit-containing VDCCs, similarly to gabapentin and pregabalin, and hence is a gabapentinoid.[9][16] Both (R)-phenibut and (S)-phenibut display this action with similar affinity (Ki = 23 and 39 μM, respectively).[9] Moreover, (R)-phenibut possesses 4-fold greater affinity for this site than for the GABAB receptor (Ki = 92 μM), while (S)-phenibut does not bind significantly to the GABAB receptor (Ki , 1 mM).[9] As such, based on the results of this study, phenibut would appear to have much greater potency in its interactions with α2δ subunit-containing VDCCs than with the GABAB receptor (between 5- to 10-fold).[9] For this reason, the actions of phenibut as a α2δ subunit-containing voltage-gated calcium channel blocker or gabapentinoid may be its true primary mechanism of action, and this may explain the differences between phenibut and its close relative baclofen (which, in contrast, has essentially insignificant activity as a gabapentinoid; Ki = 6 ...
InChI=1S/C24H34N2O/c1-21(2)19-27-20-24(25-15-9-10-16-25)18-26(23-13-7-4-8-14-23)17-22-11-5-3-6-12-22/h3-8,11-14,21,24H,9-10,15-20H2,1-2H3 ...
... (marketed as Depamide by Sanofi-Aventis) is a carboxamide derivative of valproic acid used in the treatment of epilepsy and some affective disorders. It is rapidly metabolised (80%) to valproic acid (another anticonvulsant) but has anticonvulsant properties itself. It may produce more stable plasma levels than valproic acid or sodium valproate and may be more effective at preventing febrile seizures. However, it is over one hundred times more potent as an inhibitor of liver microsomal epoxide hydrolase. This makes it incompatible with carbamazepine and can affect the ability of the body to remove other toxins. Valpromide is no safer during pregnancy than valproic acid. Valpromide is formed through the reaction of valproic acid and ammonia via an intermediate acid chloride. In pure form, valpromide is a white crystalline powder and has melting point 125-126 °C. It is practically insoluble in water but soluble in hot water. It is available on the market in some European countries. ...
Class Ib antiarrhythmic agents are sodium channel blockers. They have fast onset and offset kinetics, meaning that they have little or no effect at slower heart rates, and more effects at faster heart rates. Class Ib agents shorten the action potential duration and reduce refractoriness. These agents will decrease Vmax in partially depolarized cells with fast response action potentials. They either do not change the action potential duration, or they may decrease the action potential duration. Class Ib drugs tend to be more specific for voltage gated Na channels than Ia. Lidocaine in particular is highly frequency dependent, in that it has more activity with increasing heart rates. This is because lidocaine selectively blocks Na channels in their open and inactive states and has little binding capability in the resting state. Class Ib agents are indicated for the treatment of ventricular tachycardia and symptomatic premature ventricular beats, and prevention of ventricular fibrillation. Class Ib ...
... has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels.[1] How this effect is mediated and to what extent this mechanism is involved in the anxiolytic and analgesic effects of kavalactones on the central nervous system is unknown. Kavain's pharmacological activities have not been sufficiently investigated, and neither its effect as a serotonin reuptake inhibitor nor its monoamine (norepinephrine) uptake inhibitions and activation of NMDA receptors have been confirmed. The mechanism behind the psychotropic, sedative, and anxiolytic actions of kavain and related kavalactones is still debated. Direct binding to the benzodiazepine/flumazenil binding site of the GABA-A receptor does not occur with kavain enantiomers.[2] Many studies involved kava extracts from different plant parts and are, therefore, not applicable to kavain itself. In 2016, kavain was shown to bind at the α4β2δ GABAA receptor and ...
... has a potential for drug interactions; caution should be used in combining other medicines with it, including other antiepileptics and mood stabilizers.[12] Lower levels of carbamazepine are seen when administrated with phenobarbital, phenytoin, or primidone, which can result in breakthrough seizure activity. Carbamazepine, as a CYP450 inducer, may increase clearance of many drugs, decreasing their concentration in the blood to subtherapeutic levels and reducing their desired effects.[19] Drugs that are more rapidly metabolized with carbamazepine include warfarin, lamotrigine, phenytoin, theophylline, and valproic acid.[12] Drugs that decrease the metabolism of carbamazepine or otherwise increase its levels include erythromycin,[20] cimetidine, propoxyphene, and calcium channel blockers.[12] Carbamazepine also increases the metabolism of the hormones in birth control pills and can reduce their effectiveness, potentially leading to unexpected pregnancies.[12] As a drug that induces ...
... occludes the pore of calcium-activated voltage-gated shaker K+ channels by binding to one of four independent, overlapping binding sites.[6][7] It binds both to the open and the closed states. In addition, the block is enhanced as the ionic strength is lowered.[8] This block occurs as the Asn 30 on the CTX interacts with the Asp 381 on the K+ channel.[9] The blockade of K+ channels by the charybdotoxin peptide causes neuronal hyperexcitability. Mutations of the Lys31Gln and the Asn30Gln had the effect of lessening the CTX block of the pore on the shaker channel.[9] ...
... selectively binds to sulfonylurea receptors (SUR-1) on the surface of the pancreatic beta-cells. It was shown to provide cardiovascular protection as it does not bind to sulfonylurea receptors (SUR-2A) in the heart.[10] This binding effectively closes these K+ ion channels. This decreases the efflux of potassium from the cell which leads to the depolarization of the cell. This causes voltage dependent Ca2+ ion channels to open increasing the Ca2+ influx. The calcium can then bind to and activate calmodulin which in turn leads to exocytosis of insulin vesicles leading to insulin release.[citation needed] The mouse model of MODY diabetes suggested that the reduced gliclazide clearance stands behind their therapeutic success in human MODY patients, but Urbanova et al. found that human MODY patients respond differently and that there was no consistent decrease in gliclazide clearance in randomly selected HNF1A-MODY and HNF4A-MODY patients.[11] Its classification has been ambiguous, as ...
... has several uses including the treatment of abnormal heart rhythms or arrhythmias, chronic pain, and myotonia. In general when treating arrhythmias, mexiletine is reserved for use in dangerous heart rhythm disturbances such as ventricular tachycardia.[2] It is of particular use when treating arrhythmias caused by long QT syndrome.[3] The LQT3 form of long QT syndrome is amenable to treatment with mexiletine as this form is caused by defective sodium channels that continue to release a sustained current rather than fully inactivating, however other forms of long QT syndrome can also be treated with this medication.[3] Mexiletine has been used to treat chronic pain and may also be used to treat muscle stiffness resulting from myotonic dystrophy (Steinert's disease) or nondystrophic myotonias such as myotonia congenita (Thomsen syndrome or Becker syndrome).[4][5] ...
... is available as a generic medication and usually not too expensive.[7] Wholesale it costs between US$0.003 and US$0.15 per dose.[8] A month of treatment is about US$30 in the United States.[2] Since September 2012, the marketing licence in the UK has been held by Flynn Pharma Ltd, of Dublin, Ireland, and the product, although identical, has been called Phenytoin Sodium xxmg Flynn Hard Capsules. (The xxmg in the name refers to the strength-for example "Phenytoin sodium 25 mg Flynn Hard Capsules").[49] The capsules are still made by Pfizer's Goedecke subsidiary's plant in Freiburg, Germany and they still have Epanutin printed on them.[50] After Pfizer's sale of the UK marketing licence to Flynn Pharma, the price of a 28-pack of 25 mg phenytoin sodium capsules marked Epanutin rose from 66p (about $0.88) to £15.74 (about $25.06). Capsules of other strengths also went up in price by the same factor-2384%,[51] costing the UK's National Health Service an extra £43 million (about $68.44 ...
... is effective for prevention of shivering during surgery or recovery from surgery.[5][6] Nefopam was significantly more effective than aspirin as an analgesic in one clinical trial,[7] although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses.[8][9] The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine with comparable analgesic efficacy to morphine,[10][11][12] or oxycodone,[13] while Nefopam tends to produce fewer side effects, does not produce respiratory depression,[14] and has much less abuse potential, and so is useful either as an alternative to opioids, or as an adjunctive treatment for use alongside opioid(s) or other analgesics.[12][15] Nefopam is also used to treat severe hiccups.[16] ...
Cromakalim (INN) is a potassium channel-opening vasodilator. The active isomer is levcromakalim. It acts on ATP-sensitive ...
Cromakalim , C16H18N2O3 , CID 443423 - structure, chemical names, physical and chemical properties, classification, patents, ...
Cromakalim: A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also ... Cromakalim, (3R-trans)-Isomer; Cromakalim, (3S-cis)-Isomer; Cromakalim, (3S-trans)-Isomer; Cromakalim, (trans)-Isomer; ... Cromakalim (Levcromakalim). Subscribe to New Research on Cromakalim A potassium-channel opening vasodilator that has been ... Pre-treatment with cromakalim delayed the time to ischemic contracture (19.3 +/- 1.5 min v 15.3 +/- 0.6 for control, P , 0.05) ...
Pharmacologic and safety profile of the ocular hypotensive agent cromakalim prodrug 1 (CKLP1), a novel ATP-sensitive potassium ... Pharmacologic and safety profile of the ocular hypotensive agent cromakalim prodrug 1 (CKLP1), a novel ATP-sensitive potassium ... Pharmacologic and safety profile of the ocular hypotensive agent cromakalim prodrug 1 (CKLP1), a novel ATP-sensitive potassium ...
The antagonistic effect of Bdph against cromakalim was similar to that of 4-AP, a K+ channel blocker of Kv1 family, and ... Recently, we have observed that Bdph antagonized cromakalim, an ATP-dependent K+ channel opener, in guinea-pig trachea. Thus, ... we were interested in investigating whether Bdph at the dose without changing blood pressure antagonized cromakalim-induced ... surmountably but not parallelly rightward shifted the log dose-systolic pressure reduction curve of cromakalim, an ATP- ...
Cromakalim and cicletanine against pacing-induced myocardial ischemia in conscious rabbits. Z. Szilvássy, Matyas Koltai, P. ... Szilvássy, Z., Koltai, M., Ferdinándy, P., Jakab, I., Lonovics, J., Tarrade, T., ... Braquet, P. G. (1994). Cromakalim and ... Cromakalim and cicletanine against pacing-induced myocardial ischemia in conscious rabbits. / Szilvássy, Z.; Koltai, Matyas; ... Cromakalim (10 μg/kg), an ATP-sensitive K+ channel opener, and cicletanine (30 mg/kg), a cGMP-phosphodiesterase inhibitor, ...
... it was aimed to further indentify the intracellular action mechansm of cromakalim and levcromakalim in the porcine coronary ... Pharmacological Evidence that Cromakalim Inhibits $Ca^{2+}$. Release from Intracellular Stores in Porcine Coronary Artery 원문보기 ... Cromakalim (1 ${\mu}M$ ) caused a reduction in acetylcholine-induced increased $[Ca^{2+}]_i$ not only in the mormal ... In addition, cromakalim inhibited the $GTP{\gamma}S$ (100 . ${\mu}M$ , non-hydrolysable analogue of GTP)-induced increase in $[ ...
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When mitochondria were treated with the K(ATP) channel openers diazoxide or cromakalim, their ROS production increased by 40-50 ...
Cromakalim (10 microM, ic) increased CBF in eucapnia, but this was not seen in the presence of glibenclamide. The adenosine ... Cromakalim (10 microM, ic) increased CBF in eucapnia, but this was not seen in the presence of glibenclamide. The adenosine ... Effect of L-NMMA, cromakalim, and glibenclamide on cerebral blood flow in hypercapnia and hypoxia. ... Effect of L-NMMA, cromakalim, and glibenclamide on cerebral blood flow in hypercapnia and hypoxia. ...
cromakalim (Cro) at 10 and glipizide (Gli) at 10 Combination of enterocin S37 with each of K+ channel modulator was also ... Effect of the combinations of enterocin S37 with cromakalim (10 ) and glipizide (10 ) was less important on L. monocytogenes ... cromakalim (Cro; 10. ) and glipizide (Gli; 10 ). Values are the mean of three independent measurements. ... Combination of cromakalim and enterocin S37 resulted in 84.29% 2.5 inhibition of the growth of sensitive strain; this data is ...
Cromakalim had little effect on phospholipase D activity enhanced by the activated mast cell. Cromakalim inhibited the initial ... Cromakalim inhibited the phospholipid methylation increased in the activated mast cell. These results show that cromakalim ... Cromakalim resulted in a decrease in the amount of histamine and leukotrienes releases by 30% in the ovalumin-induced mast cell ... The effects of cromakalim on the mediator releases from guinea pig lung mast cell activated by specific antigen-antibody ...
Cardioprotective effect of cromakalim (potassium channel opener) in isoproterenol induced Cardioprotective effect of cromakalim ... Cromakalims beneficial effects on myocardium were in dose-dependent manner. Administration of cromakalim (po) lowered ... Animals pretreated with cromakalim (1 mg/kg,po) along with isoproterenol (85 mg/kg,sc) showed less myocardial degenerative ... Animals , Aspartate Aminotransferases/drug effects , Benzopyrans/pharmacology , Blood Coagulation/drug effects , Cromakalim , ...
Cromakalim. A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also ...
Cromakalim / pharmacology * Heart / physiopathology* * Heart Conduction System / drug effects * Heart Conduction System / ...
Cromakalim and lemakalim activate Ca^,2+,-dependent K^+ channels in canine colon CARL A ...
Cromakalim was obtained from Tocris, UK. Stock solution (10 mmol/L) for indomethacin, cromakalim and U46619 was prepared in 96 ... or cromakalim (3 μmol/L, n=4). *P,0.05 vs control. B, EDHF-mediated dilation to ACh in coronary arteries (preconstricted with ... or cromakalim (3 μmol/L, n=4). *P,0.05 for Emax. C, Myogenic constriction (percent decrease from passive diameter) in ... The KATP channel opener cromakalim (3 μmol/L, n=4) also prevented the development of myogenic constriction (Figure 2A) but had ...
Comparison of the effect of cromakalim in porcine and human coronary arteries. Cardiovasc Drugs Ther 1999;13:52 (A197).Google ... 1 μM GLI decreased the maximum of cromakalim-induced relaxation by 60% but did not affect the action of levosimendan. In ... Comparison of the vasorelaxant effect of cromakalim and the new inodilator, levosimendan, in human isolated portal vein. J ... was compared to cromakalim (0.0125-5 μM), the known activator of ATP-sensitive potassium (KATP) channels, in the presence of ...
Kir6 (KATP) channel opener; active enantiomer of cromakalim (Cat. No. 1377). 94535-50-9. ...
... cromakalim (BRL 34915), aprikalim, bimakalim, emakalim and lemakalim. Nicorandil, pinacidil, cromakalim and minoxidil are the ... 5,256,688 and 5,354,764 disclose the use of pinacidil or cromakalim for treating myocardial ischemia; U.S. Pat. No. 5,262,419 ... cromakalim (BRL 34915), aprikalim, bimakalim, emakalim, lemakalim, minoxidil, diazoxide, 9-chloro-7-(2-chlorophenyl)-5H- ...
Effect of pinacidil, minoxidil and cromakalim in the mouse forced swimming test. The test was performed 20 min after treatment ... cromakalim (30 μg per mouse i.c.v.), minoxidil (20 μg per mouse i.c.v.), aODN (3 nmol per single i.c.v. injection) and dODN (3 ... cromakalim) and aODN to mKv1.1 on immobility time was evaluated in the mouse forced swimming test, an animal model of ... and cromakalim (20-30 microg per mouse i.c.v.) increased immobility time when administered in the same experimental conditions ...
In some embodiments, the the agonist of a potassium channel is nicorandil; minoxidil, levcromakalim; lemakalim; cromakalim; L- ...
Cromakalim (Levcromakalim) 9. Carbon Monoxide 10. Angiotensin-Converting Enzyme Inhibitors (ACE Inhibitors) ...
wherein the compound of Formula (III) is a nitrosated cromakalim, a nitrosylated cromakalim, a nitrosated and nitrosylated ... cromakalim (BRL 34915), aprikalim, bimakalim, emakalim and lemakalim. Nicorandil, pinacidil, cromakalim and minoxidil are the ... 5,256,688 and 5,354,764 disclose the use of pinacidil or cromakalim for treating myocardial ischemia; U.S. Pat. No. 5,262,419 ... wherein the potassium channel activator is nicorandil, pinacidil, cromakalim, aprikalim, bimakalim, emakalim, lemakalim, ...
Cromakalim dilates rat cerebral arteries in vitro. T Nagao, S Sadoshima, M Kamouchi, M Fujishima ...
McCarron, J. G., Quayle, J. M., Halpern, W., and Nelson, M. T. (1991). Cromakalim and pinacidil dilate small mesenteric ...
Controlled release of cromakalim from the cromakalim/hyaluronan implant at a dose of 0.055 mg/kg significantly increased lumen ... Cromakalim was coupled to a viscous carrier, hyaluronan, 15% by weight. In vitro release kinetics studies showed a steady ... Prevention of cerebral vasospasm by local delivery of cromakalim with a biodegradable controlled-release system in a rat model ... The authors tested the efficacy of locally delivered intrathecal cromakalim, a PCO, incorporated into a controlled-release ...
Ion Channels in the Cardiovascular System in Health and Disease. William A. Coetzee [email protected] Tel: 263-8518. Hearts are Composed of Cells. The Cardiac Myocyte. Cells Have Membranes. Channels. Pore. Filter. Gate. Patch Clamping. open. closed. Ion Channels - Gating. Slideshow 85327...
Cromakalim, pinacidil and RP 49356 activate a tolbutamide-sensitive K+ conductance in human skeletal muscle fibres. ... Cromakalim (BRL 34915) restores in vitro the membrane potential of depolarized human skeletal muscle fibres. ...
Protective effect of cromakalim and diazoxide, and proulcerogenic effect of glibenclamide on indomethacin-induced gastric ...
  • 1. The effect of intracerebroventricular (i.c.v.) administration of different potassium channel blockers (tetraethylammonium, apamin, charybdotoxin, gliquidone), potassium channel openers (pinacidil, minoxidil, cromakalim) and aODN to mKv1.1 on immobility time was evaluated in the mouse forced swimming test, an animal model of depression. (nih.gov)
  • By contrast pinacidil (10-20 microg per mouse i.c.v.), minoxidil (10-20 microg per mouse i.c.v.) and cromakalim (20-30 microg per mouse i.c.v.) increased immobility time when administered in the same experimental conditions. (nih.gov)
  • Effect of pinacidil, minoxidil and cromakalim in the mouse forced swimming test. (nih.gov)
  • The K+ channel opener diazoxide, but not cromakalim or pinacidil, inhibited electrical activity and increased the whole-cell K+ conductance fourfold. (nih.gov)
  • These results suggest NNC 55-9216 is a SUR1-selective PCO that requires structural determinants, which differ from those needed for activation of the K ATP channel by pinacidil and cromakalim. (diabetesjournals.org)
  • When mitochondria were treated with the K(ATP) channel openers diazoxide or cromakalim, their ROS production increased by 40-50%, and this effect was blocked by 5-hydroxydecanoate. (mendeley.com)
  • Protective effect of cromakalim and diazoxide, and proulcerogenic effect of glibenclamide on indomethacin-induced gastric injury. (ugent.be)
  • Glyburide blocks the relaxation response to BRL 34915 (cromakalim), minoxidil sulfate and diazoxide in vascular smooth muscle. (semanticscholar.org)
  • In vitro and in vivo comparison of two K+ channel openers, diazoxide and cromakalim, and their inhibition by glibenclamide. (semanticscholar.org)
  • Cholesterol-enriched diet inhibits cardioprotection by ATP-sensitive K+ channel activators cromakalim and diazoxide , AMERICAN JOURNAL OF PHYSIOLOGY: HEART AND CIRCULATORY PHYSIOLOGY 306: (3) pp. (doktori.hu)
  • Wetter Rottweil 10 Tage between dosage adjustments normally Cromakalim Diazoxide Emakalim Levcromakalim Mazokalim days since the full response to a given dose is In addition, its effectiveness has that amount of time. (defiance-online.com)
  • KATP channel blockers include GLIBENCLAMIDE and mitiglinide whereas openers include CROMAKALIM and minoxidil sulfate. (harvard.edu)
  • Moreover, the antidepressant-like effect elicited by an effective dose of hesperidin (0.3 mg/kg, i.p.) in TST was abolished by the treatment of mice with pharmacological compounds K(+) channel openers (cromakalim and minoxidil). (sigmaaldrich.com)
  • Recently, we have observed that Bdph antagonized cromakalim, an ATP-dependent K + channel opener, in guinea-pig trachea. (biomedcentral.com)
  • Cromakalim (10 μg/kg), an ATP-sensitive K + channel opener, and cicletanine (30 mg/kg), a cGMP-phosphodiesterase inhibitor, reduced VOP-induced ST-segment elevation and LVEDP-increase. (elsevier.com)
  • Cardioprotective effect of cromakalim (potassium channel opener) in isoproterenol induced myocardial infarction in rats. (bvsalud.org)
  • 0.01), whereas the K ATP channel opener cromakalim (3 μmol/L) had no effect on EDHF-mediated dilation. (ahajournals.org)
  • The ATP-sensitive potassium channel opener, cromakalim, protects ischemic hearts and its effect can be reversed by glyburide. (aspetjournals.org)
  • The potassium channel opener, cromakalim, protected ischemic rat hearts (improved recovery of contractile function and reduced enzyme release) and this was abolished by glyburide. (aspetjournals.org)
  • Neither was found to effect the action of the potassium channel opener, cromakalim. (aspetjournals.org)
  • 9 14 15 Acetylcholine-induced hyperpolarization appears to be mediated by the opening of K + channels, since its effect is mimicked by cromakalim, a K + channel opener, and inhibited by increasing [K + ] o . 15 16 In coronary and mesenteric arteries and aorta, the relaxation and hyperpolarization are blocked by TEA but not by glibenclamide. (ahajournals.org)
  • The K+ channel opener cromakalim induced relaxation of vessels precontracted by serotonin but not by U46619 or high K+ containing solutions (60 mM), suggesting that K+ channels are involved. (hu-berlin.de)
  • 6. The K+ channel opener cromakalim (10 μM) evoked a sustained increase in NP(o) of the Ca2+-activated K+ channels which was not potentiated by the addition of bradykinin. (edu.au)
  • The effects of trans-5,6-dihydro-6-hydroxy-5,5-dimethyl-2-nitro-7-(2-oxopiperidin -1-yl)-7H- thieno[3,2-b]pyran (RWJ 26629) were compared with those of the standard potassium channel opener cromakalim and several standard calcium channel blockers. (biomedsearch.com)
  • Under normoxia, the ATP-sensitive K + -channel opener cromakalim (10 -5 M) inhibited the serotonergic response on postcapillary resistance and microvascular compliance, whereas during hypoxia cromakalim inhibited the potentiated effect of serotonin on both precapillary and postcapillary resistance, capillary pressure, and both microvascular and large-vessel compliances. (elsevier.com)
  • Effect of L-NMMA, cromakalim, and glibenclamide on cerebral blood flow in hypercapnia and hypoxia. (ox.ac.uk)
  • Cromakalim (10 microM, ic) increased CBF in eucapnia, but this was not seen in the presence of glibenclamide. (ox.ac.uk)
  • In the present study performed in the porcine epicardial coronary artery, the effect of levosimendan (0.009-3.2 μM) was compared to cromakalim (0.0125-5 μM), the known activator of ATP-sensitive potassium (K ATP ) channels, in the presence of glibenclamide (GLI), an inhibitor of K ATP channels and tetraethylammonium (TEA), the non-selective inhibitor of potassium channels. (springer.com)
  • 14 17 18 These data suggest that EDHF acts on the Ca 2+ -dependent K + channels inhibited by TEA and not the ATP-sensitive K + channels opened by cromakalim and inhibited by glibenclamide. (ahajournals.org)
  • Glibenclamide (10 μM) alone increased NP(o) and partially inhibited the cromakalim-induced increase in NP(o) with respect to control. (edu.au)
  • In the present study, it was aimed to further indentify the intracellular action mechansm of cromakalim and levcromakalim in the porcine coronary artery. (ndsl.kr)
  • mu}M$ ) strongly blocked the effect of cromakalim and levcromakalim. (ndsl.kr)
  • Based on these results, it is suggested that cromakalim and levcromakalim exert a potent vasorelaxation, in part, by acting on the $K^+$ channels of the intracellular sites (e.g., sarcoplasmic reticulum membrane), thereby, resulting in decrease in release of $Ca^{2+}$ from the intracellular storage site. (ndsl.kr)
  • 8. Discovery and Development of Cromakalim and Related Potassium Channel Activators 9. (textbookx.com)
  • The active enantiomer of cromakalim has been found to be effective in alleviating nocturnal asthma at plasma concentrations just threshold for relaxing human airways smooth muscle in vitro. (curehunter.com)
  • We evaluated the effects of BRL 38227, the active enantiomer of cromakalim, on the electrophysiologic and hemodynamic parameters in anesthetized dogs. (ovid.com)
  • The results suggest cardioprotective effect of cromakalim in isoproterenol induced myocardial infarction . (bvsalud.org)
  • 1 μM GLI decreased the maximum of cromakalim-induced relaxation by 60% but did not affect the action of levosimendan. (springer.com)
  • 5) Cromakalim in concentrations causing maximal relaxation did not increase the tissue level of either cyclic AMP or cyclic GMP in the BRP muscle, although the appropriate synthetic enzymes were present and could be stimulated by forskolin or NaNP. (gla.ac.uk)
  • In contrast, calcium ionophore A23187-elicited endothelium-dependent relaxation as well as cromakalim- and sodium nitroprusside-mediated endothelium-independent relaxation was unchanged following the same regime with 17β-estradiol. (hku.hk)
  • However, it has recently been observed that cromakalim inhibits the release of mediators from superfused tracheal and parenchymal strips or lung mast cells after passive sensitization with the IgG1 antibody. (bvsalud.org)
  • Furthermore, cromakalim reduces phosphatidylcholine production by inhibiting the methyltransferase, which decreases the conversion of phosphatidylcholine into arachidonic acid and inhibits the production of leukotrienes . (bvsalud.org)
  • It is presently unknown if glyburide can abolish the anti-ischemic effects of mechanistically different agents or if blockers of other potassium channels can abolish the protective effects of cromakalim. (aspetjournals.org)
  • In addition, cromakalim is unaffected by blockers of other potassium channels, further indicating selectivity of glyburide for ATP-sensitive potassium channels. (aspetjournals.org)
  • 3) Verapamil significantly reduced the relaxant effect of cromakalim in the guinea-pig trachea. (gla.ac.uk)
  • The antagonistic effect of Bdph against cromakalim was similar to that of 4-AP, a K+ channel blocker of Kv1 family, and partially similar to that of GBC, an ATP-sensitive K+ channel blocker. (biomedcentral.com)
  • This suggests that VERP shortening is not a prerequisite for the anti-ischemic effect of cromakalim, and the combination of these drugs may afford a potent and safe anti-ischemic effect without affecting hypotension induced cromakalim. (elsevier.com)
  • The inhibitory effect of cromakalim on the mediator release from mast cells caused by antigenantibody reactions was in controversy with the specific antigen used. (bvsalud.org)
  • Cromakalim had little effect on phospholipase D activity enhanced by the activated mast cell . (bvsalud.org)
  • Comparison of the vasorelaxant effect of cromakalim and the new inodilator, levosimendan, in human isolated portal vein. (springer.com)
  • Comparison of the effect of cromakalim in porcine and human coronary arteries. (springer.com)
  • The Effects of Cromakalim on Spasmogen- or Stretch-induced Contraction of a Variety of Smooth Muscle Preparations (1) The relaxant effect of cromakalim has been examined on four isolated preparations, the rabbit aortic strip, the BRP muscle, the guinea-pig trachea and the guinea-pig taenia coli contracted by either histamine, carbachol, noradrenaline or KCl. (gla.ac.uk)
  • 4) The relaxant effects of cromakalim on the BRP muscle and the guinea-pig taenia coli were unaffected by haemoglobin (3.3 muM) or apamin (0.5 muM) in concentrations which block completely the relaxant effect of respectively NANC nerve stimulation in these tissues respectively. (gla.ac.uk)
  • Fautsch, M. P. Effect of cromakalim prodrug 1 (CKLP1) on aqueous humor dynamics and feasibility of combination therapy with existing ocular hypotensive agents. (umn.edu)
  • Cromakalim (INN) is a potassium channel-opening vasodilator. (wikipedia.org)
  • Cromakalim (BRL 34915) restores in vitro the membrane potential of depolarized human skeletal muscle fibres. (uni-muenchen.de)
  • Thus, we were interested in investigating whether Bdph at the dose without changing blood pressure antagonized cromakalim-induced systolic pressure reduction in conscious rats. (biomedcentral.com)
  • Activation of KATP channels by cromakalim inhibited the frequency of carbachol-induced phasic activity of bladder strips, although strips from diabetic rats showed a trend towards being less sensitive to cromakalim. (edu.au)
  • 1989). We now show, by using electrophysiological techniques in three different types of smooth muscle, that a large-conductance voltage and Ca 2+ -sensitive channel, otherwise indistinguishable from the large-conductance Ca 2+ -activated K + channel (BK channel), is also sensitive to cytoplasmic ATP and cromakalim. (royalsocietypublishing.org)
  • Sur des anneaux aortiques dénudés de leur endothélium, nous avons mesuré les réponses contractiles à la phényléphrine (PhE) et au KCl en présence d'un bloqueur des canaux calciques dépendants du voltage (VDCC), la nifédipine, et d'activateurs des canaux potassiques à large conductance (BKCa) et ceux dépendants de l'ATP (KATP), respectivement le NS-1619 et la cromakalim. (umontreal.ca)
  • Intracellular electrophysiological studies showed that ischemia-induced depolarization was reversed with cromakalim, which increased the resting potential nearly back to preischemic levels. (curehunter.com)
  • The cardioprotective and electrophysiological effects of cromakalim are attenuated by meclofenamate through a cyclooxygenase-independent mechanism. (semanticscholar.org)
  • Cromakalim 's beneficial effects on myocardium were in dose -dependent manner. (bvsalud.org)
  • Sodium SaltA K+ channel antagonist which blocks the post-ischemic effects of the K+ channel activator cromakalim. (mpbio.com)
  • In contrast, cromakalim potentiated the relaxant effects of isoprenaline and NaNP in the guinea-pig trachea. (gla.ac.uk)
  • Publications] Kohji Okabe: 'Actions of cromakalim on ionic currents recorded from single smooth muscle cells of the rat portal vein. (nii.ac.jp)
  • Animals pretreated with cromakalim (1 mg/kg,po) along with isoproterenol (85 mg/kg,sc) showed less myocardial degenerative changes on histopathological examinations when compared with those treated with isoproterenol alone. (bvsalud.org)
  • Preparations of crushed due cromakalim into Asia may settle made some fights to remain damage programs on the additional dose, ' ADB came. (miniworldrotterdam.com)
  • Administration of cromakalim (po) lowered significantly the serum LDH and SGOT and depleted intracytoplasmic glycogen as demonstrated by periodic schiff staining procedure . (bvsalud.org)
  • Cicletanine did not change cromakalim-induced hypotension but abolished reflexogenic tachycardia. (elsevier.com)
  • Cromakalim (100 nM) relaxierte vollständig Serotonin-kontrahierte Gefäßringe (+)fat und (-)fat, aber konnte nicht U46619-kontrahierte Gefäßringe (+)fat und (-)fat relaxieren. (hu-berlin.de)
  • This did not happen when cromakalim was added at the peak of contraction. (gla.ac.uk)
  • Cromakalim (1 ${\mu}M$ ) caused a reduction in acetylcholine-induced increased $[Ca^{2+}]_i$ not only in the mormal physiological salt solution (PSS) but also in $Ca^{2+}$ -free PSS (containing 1 mM EGTA). (ndsl.kr)