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Pinacidil
Pinacidil is a cyanoguanidine drug that opens ATP-sensitive potassium channels producing peripheral vasodilatation of arterioles. It reduces blood pressure Blood pressure (BP) is the pressure of circulating blood against the walls of blood vessels. Most of this pressure results from the heart pumping blood through the circulatory system. When used without qualification, the term "blood pressure" r ... and peripheral resistance and produces fluid retention. Synthesis Condensation of 4-isothiocyanotopyridine 6105-84-5(1) and 3,3-dimethyl-2-butanamine 850-30-4(2) gives thiourea 7027-06-9(3). Treatment of that intermediate with a mixture of triphenylphosphine, carbon tetrachloride, and triethylamine leads to the unsymmetrical carbodiimideCID:20501933(4'). Addition of cyanamid affords pinacidil (5). References External links * Potassium channel openers 4-Pyridyl compounds Cyanamides {{cardiovascular-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Potassium Channel Openers
A potassium channel opener is a type of drug which facilitates ion transmission through potassium channels. Examples Some examples include: *Diazoxide vasodilator used for hypertension, smooth muscle relaxing activity *Minoxidil vasodilator used for hypertension, also used to treat hair loss *Nicorandil vasodilator used to treat angina *Pinacidil *Retigabine, an anticonvulsant * Flupirtine, analgesic with muscle relaxant and anticonvulsant properties See also * Potassium channel blocker Potassium channel blockers are agents which interfere with conduction through potassium channels. Medical uses Arrhythmia Potassium channel blockers used in the treatment of cardiac arrhythmia are classified as class III antiarrhythmic age ... References {{pharmacology-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pinacidil Synthesis
Pinacidil is a cyanoguanidine drug that opens ATP-sensitive potassium channels producing peripheral vasodilatation of arterioles. It reduces blood pressure Blood pressure (BP) is the pressure of circulating blood against the walls of blood vessels. Most of this pressure results from the heart pumping blood through the circulatory system. When used without qualification, the term "blood pressure" r ... and peripheral resistance and produces fluid retention. Synthesis Condensation of 4-isothiocyanotopyridine 6105-84-5(1) and 3,3-dimethyl-2-butanamine 850-30-4(2) gives thiourea 7027-06-9(3). Treatment of that intermediate with a mixture of triphenylphosphine, carbon tetrachloride, and triethylamine leads to the unsymmetrical carbodiimideCID:20501933(4'). Addition of cyanamid affords pinacidil (5). References External links * Potassium channel openers 4-Pyridyl compounds Cyanamides {{cardiovascular-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
2-cyanoguanidine
2-Cyanoguanidine is a nitrile derived from guanidine. It is a dimer of cyanamide, from which it can be prepared. 2-Cyanoguanidine is a colourless solid that is soluble in water, acetone, and alcohol, but not nonpolar organic solvents. Production and use 2-Cyanoguanidine is produced by treating cyanamide with base. It is produced in soil by decomposition of cyanamide. A variety of useful compounds are produced from 2-cyanoguanidine, guanidines and melamine. For example, acetoguanamine and benzoguanamine are prepared by condensation of cyanoguanidine with the nitrile: :(H2N)2C=NCN + RCN → (CNH2)2(CR)N3 Cyanoguanidine is also used as a slow fertilizer. Formerly, it was used as a fuel in some explosives. It is used in the adhesive industry as a curing agent for epoxy resins. Chemistry Two tautomeric forms exist, differing in the protonation and bonding of the nitrogen to which the nitrile group is attached. : 2-Cyanoguanidine can also exist in a zwitterionic form via a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ATP-sensitive Potassium Channel
An ATP-sensitive potassium channel (or KATP channel) is a type of potassium channel that is gated by intracellular nucleotides, ATP and ADP. ATP-sensitive potassium channels are composed of Kir6.x-type subunits and sulfonylurea receptor (SUR) subunits, along with additional components. KATP channels are found in the plasma membrane; however some may also be found on subcellular membranes. These latter classes of KATP channels can be classified as being either sarcolemmal ("sarcKATP"), mitochondrial ("mitoKATP"), or nuclear ("nucKATP"). Discovery and structure KATP channels were first identified in cardiac myocytes by the Akinori Noma group in Japan. They have also been found in pancreas where they control insulin secretion, but are in fact widely distributed in plasma membranes. SarcKATP are composed of eight protein subunits (octamer). Four of these are members of the inward-rectifier potassium ion channel family Kir6.x (either Kir6.1 or Kir6.2), while the other four ar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vasodilatation
Vasodilation is the widening of blood vessels. It results from relaxation of smooth muscle cells within the vessel walls, in particular in the large veins, large arteries, and smaller arterioles. The process is the opposite of vasoconstriction, which is the narrowing of blood vessels. When blood vessels dilate, the flow of blood is increased due to a decrease in vascular resistance and increase in cardiac output. Therefore, dilation of arterial blood vessels (mainly the arterioles) decreases blood pressure. The response may be intrinsic (due to local processes in the surrounding tissue) or extrinsic (due to hormones or the nervous system). In addition, the response may be localized to a specific organ (depending on the metabolic needs of a particular tissue, as during strenuous exercise), or it may be systemic (seen throughout the entire systemic circulation). Endogenous substances and drugs that cause vasodilation are termed vasodilators. Such vasoactivity is necessary for h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Arteriole
An arteriole is a small-diameter blood vessel in the microcirculation that extends and branches out from an artery and leads to capillaries. Arterioles have muscular walls (usually only one to two layers of smooth muscle cells) and are the primary site of vascular resistance. The greatest change in blood pressure and velocity of blood flow occurs at the transition of arterioles to capillaries.This function is extremely important because it prevents the thin, one-layer capillaries from exploding upon pressure. The arterioles achieve this decrease in pressure, as they are the site with the highest resistance (a large contributor to total peripheral resistance) which translates to a large decrease in the pressure. Structure Microanatomy In a healthy vascular system the endothelium lines all blood-contacting surfaces, including arteries, arterioles, veins, venules, capillaries, and heart chambers. This healthy condition is promoted by the ample production of nitric oxide by the end ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Blood Pressure
Blood pressure (BP) is the pressure of circulating blood against the walls of blood vessels. Most of this pressure results from the heart pumping blood through the circulatory system. When used without qualification, the term "blood pressure" refers to the pressure in the large arteries. Blood pressure is usually expressed in terms of the systolic pressure (maximum pressure during one heartbeat) over diastolic pressure (minimum pressure between two heartbeats) in the cardiac cycle. It is measured in millimeters of mercury ( mmHg) above the surrounding atmospheric pressure. Blood pressure is one of the vital signs—together with respiratory rate, heart rate, oxygen saturation, and body temperature—that healthcare professionals use in evaluating a patient's health. Normal resting blood pressure, in an adult is approximately systolic over diastolic, denoted as "120/80 mmHg". Globally, the average blood pressure, age standardized, has remained about the same since 1 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
