|
Lomerizine
Lomerizine (INN) (also known as KB-2796) is a diphenylpiperazine class L-type and T-type calcium channel blocker. This drug is currently used clinically for the treatment of migraines, while also being used experimentally for the treatment of glaucoma and optic nerve injury. Solubility Due to its lipophilic nature and small molecular size, lomerizine is able to cross the blood brain barrier. For delivery in aqueous systems, nanoparticle therapy may be used. Along with lipids, lomerizine is soluble in chloroform, methanol, and DMSO. Mechanism of Action Lomerizine works as a calcium antagonist by blocking voltage-dependent calcium channels. A study using 3H.html" ;"title="sup>3H">sup>3Hitrendipine showed that lomerizine allosterically inhibits binding in calcium channels at a different site from the 1,4 dihydropyridine binding site. However, its antimigraine effects are believed to be due not to the blocking of calcium channels, but to the antagonizing effects of lomerizin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lomerizine Synthesis
Lomerizine (INN) (also known as KB-2796) is a diphenylpiperazine class L-type and T-type calcium channel blocker. This drug is currently used clinically for the treatment of migraines, while also being used experimentally for the treatment of glaucoma and optic nerve injury. Solubility Due to its lipophilic nature and small molecular size, lomerizine is able to cross the blood brain barrier. For delivery in aqueous systems, nanoparticle therapy may be used. Along with lipids, lomerizine is soluble in chloroform, methanol, and DMSO. Mechanism of Action Lomerizine works as a calcium antagonist by blocking voltage-dependent calcium channels. A study using 3H.html" ;"title="sup>3H">sup>3Hitrendipine showed that lomerizine allosterically inhibits binding in calcium channels at a different site from the 1,4 dihydropyridine binding site. However, its antimigraine effects are believed to be due not to the blocking of calcium channels, but to the antagonizing effects of lomerizin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Flunarizine
Flunarizine, sold under the brand name Sibelium among others, is a drug classified as a calcium antagonist which is used for various indications. It is not available by prescription in the United States or Japan. The drug was discovered at Janssen Pharmaceutica (R14950) in 1968. Medical uses Flunarizine is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an add-on in the treatment of epilepsy where its effect is weak and not recommended. It has been shown to significantly reduce headache frequency and severity in both adults and children. Contraindications Flunarizine is contraindicated in patients with depression, in the acute phase of a stroke, and in patients with extrapyramidal symptoms or Parkinson's disease. It is also contraindicated in hypotension, heart failure and arrhythmia. Side effects Common side effects include drowsiness (20% of patients), weight gain (10%), as well as extrapyramida ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Flunarizine
Flunarizine, sold under the brand name Sibelium among others, is a drug classified as a calcium antagonist which is used for various indications. It is not available by prescription in the United States or Japan. The drug was discovered at Janssen Pharmaceutica (R14950) in 1968. Medical uses Flunarizine is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an add-on in the treatment of epilepsy where its effect is weak and not recommended. It has been shown to significantly reduce headache frequency and severity in both adults and children. Contraindications Flunarizine is contraindicated in patients with depression, in the acute phase of a stroke, and in patients with extrapyramidal symptoms or Parkinson's disease. It is also contraindicated in hypotension, heart failure and arrhythmia. Side effects Common side effects include drowsiness (20% of patients), weight gain (10%), as well as extrapyramida ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sodium-calcium Exchanger
The sodium-calcium exchanger (often denoted Na+/Ca2+ exchanger, exchange protein, or NCX) is an antiporter membrane protein that removes calcium from cells. It uses the energy that is stored in the electrochemical gradient of sodium (Na+) by allowing Na+ to flow down its gradient across the plasma membrane in exchange for the countertransport of calcium ions (Ca2+). A single calcium ion is exported for the import of three sodium ions. The exchanger exists in many different cell types and animal species. The NCX is considered one of the most important cellular mechanisms for removing Ca2+. The exchanger is usually found in the plasma membranes and the mitochondria and endoplasmic reticulum of excitable cells. Function The sodium–calcium exchanger is only one of the systems by which the cytoplasmic concentration of calcium ions in the cell is kept low. The exchanger does not bind very tightly to Ca2+ (has a low affinity), but it can transport the ions rapidly (has a high capa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pyrogallol Ethers
Pyrogallol is an organic compound with the formula C6H3(OH)3. It is a water-soluble, white solid although samples are typically brownish because of its sensitivity toward oxygen. It is one of three isomers of benzenetriols. Production and reactions It is produced in the manner first reported by Scheele in 1786: heating gallic acid to induce decarboxylation. Gallic acid is also obtained from tannin. Many alternative routes have been devised. One preparation involves treating ''para''-chlorophenoldisulfonic acid with potassium hydroxide, a variant on the time-honored route to phenols from sulfonic acids. When in alkaline solution, pyrogallol undergoes deprotonation of one or more phenolic groups. Such solutions absorb oxygen from the air, turning brown. This conversion can be used to determine the amount of oxygen in a gas sample, notably by the use of the Orsat apparatus. Polyhydroxybenzenes are relatively electron-rich. One manifestation is the easy C-acetylation of pyr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phosphorus Tribromide
Phosphorus tribromide is a colourless liquid with the formula P Br3. The liquid fumes in moist air due to hydrolysis and has a penetrating odour. It is used in the laboratory for the conversion of alcohols to alkyl bromides. Preparation PBr3 is prepared by treating red phosphorus with bromine. An excess of phosphorus is used in order to prevent formation of PBr5: :2 P + 3 Br2 → 2 PBr3 Because the reaction is highly exothermic, it is often conducted in the presence of a diluent such as PBr3. Reactions Phosphorus tribromide, like PCl3 and PF3, has both properties of a Lewis base and a Lewis acid. For example, with a Lewis acid such as boron tribromide it forms stable 1 :1 adducts such as Br3B · PBr3. At the same time PBr3 can react as an electrophile or Lewis acid in many of its reactions, for example with amines. The most important reaction of PBr3 is with alcohols, where it replaces an OH group with a bromine atom to produce an alkyl bromide. All three bromides ca ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trimetazidine
Trimetazidine (IUPAC: 1-(2,3,4-trimethoxybenzyl)piperazine) is a drug for angina pectoris (chest pain associated with blood flow to the heart) sold under many brand names. Trimetazidine is described as the first cytoprotective anti-ischemic agent developed and marketed by Laboratoires Servier (France). It is an anti-ischemic (antianginal) metabolic agent of the fatty acid oxidation inhibitor class, meaning that it improves myocardial glucose utilization through inhibition of fatty acid metabolism. Medical uses Trimetazidine is usually prescribed as a long-term treatment of angina pectoris, and in some countries (including France) for tinnitus and dizziness. It is taken twice a day. In 2012, the European Medicines Agency (EMA) finished a review of benefits and risks of trimetazidine and recommended restricting use of trimetazidine-containing medicines to just as an additional treatment of angina pectoris in cases of inadequate control by or intolerance to first-line antia ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IC50
The half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, ''in vitro'', a given biological process or biological component by 50%. The biological component could be an enzyme, cell, cell receptor or microorganism. IC50 values are typically expressed as molar concentration. IC50 is commonly used as a measure of antagonist drug potency in pharmacological research. IC50 is comparable to other measures of potency, such as EC50 for excitatory drugs. EC50 represents the dose or plasma concentration required for obtaining 50% of a maximum effect ''in vivo''. IC50 can be determined with functional assays or with competition binding assays. Sometimes, IC50 values are converted to the pIC50 scale. :\ce = -\log_ \ce Due to the minus sign, higher values of pIC50 indica ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Half-life
Half-life (symbol ) is the time required for a quantity (of substance) to reduce to half of its initial value. The term is commonly used in nuclear physics to describe how quickly unstable atoms undergo radioactive decay or how long stable atoms survive. The term is also used more generally to characterize any type of exponential (or, rarely, non-exponential) decay. For example, the medical sciences refer to the biological half-life of drugs and other chemicals in the human body. The converse of half-life (in exponential growth) is doubling time. The original term, ''half-life period'', dating to Ernest Rutherford's discovery of the principle in 1907, was shortened to ''half-life'' in the early 1950s. Rutherford applied the principle of a radioactive element's half-life in studies of age determination of rocks by measuring the decay period of radium to lead-206. Half-life is constant over the lifetime of an exponentially decaying quantity, and it is a characteristic unit for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
