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Pinacidil
Pinacidil is a 2-cyanoguanidine, cyanoguanidine drug that opens ATP-sensitive potassium channels producing peripheral vasodilatation of arterioles. It reduces blood pressure and peripheral resistance and produces fluid retention. Synthesis Condensation of 4-isothiocyanotopyridine [76105-84-5] (1) and 3,3-dimethyl-2-butanamine [3850-30-4] (2) gives thiourea [67027-06-9] (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 Pinacidil is a 2-cyanoguanidine, cyanoguanidine drug that opens ATP-sensitive potassium channels producing peripheral vasodilatation of arterioles. It reduces blood pressure and peripheral resistance and produces fluid retention. Synthesis Cond ... * Retigabine, an anticonvulsant * Flupirtine, analgesic with muscle relaxant and anticonvulsant properties See also * Potassium channel blocker References {{pharmacology-stub ... [...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 widely distributed in plasma membranes; 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 Akinori Noma in Japan. Glucose-regulated KATP channel activity was found in pancreatic beta cells by Frances Ashcroft at the University of Oxford. The closure of KATP channels leads to increased insulin secretion in beta cells and reduces glucagon secretion in alpha cells. SarcKATP are composed of eight protein subunits ( octamer). Four of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vasodilatation
Vasodilation, also known as vasorelaxation, 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. Blood vessel walls are composed of endothelial tissue and a basal membrane lining the lumen of the vessel, concentric smooth muscle layers on top of endothelial tissue, and an adventitia over the smooth muscle layers. Relaxation of the smooth muscle layer allows the blood vessel to dilate, as it is held in a semi-constricted state by sympathetic nervous system activity. Vasodilation 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. Vascular resistance is the amount of force circulating blood must overcome in order to allow perfusion of body tissues. Narrow vessels create more vascular resi ... [...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 capillary, capillaries. Arterioles have vascular smooth muscle, 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 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 n ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Blood Pressure
Blood pressure (BP) is the pressure of Circulatory system, 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 a brachial artery, where it is most commonly measured. Blood pressure is usually expressed in terms of the systolic pressure (maximum pressure during one Cardiac cycle, heartbeat) over diastolic pressure (minimum pressure between two heartbeats) in the cardiac cycle. It is measured in Millimetre of mercury, millimetres of mercury (mmHg) above the surrounding atmospheric pressure, or in Pascal (unit), kilopascals (kPa). The difference between the systolic and diastolic pressures is known as pulse pressure, while the average pressure during a cardiac cycle is known as mean arterial pressure. Blood pressure is one of the vital signs—together with respiratory rate, heart rate, Oxygen saturation (me ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
