Adenosine Reuptake Inhibitor
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Adenosine Reuptake Inhibitor
An adenosine reuptake inhibitor (AdoRI) is a type of drug which acts as a reuptake inhibitor for the purine nucleoside and neurotransmitter adenosine by blocking the action of one or more of the equilibrative nucleoside transporters (ENTs). This in turn leads to increased extracellular concentrations of adenosine and therefore an increase in adenosinergic neurotransmission. List of AdoRIs * Acadesine * Acetate * Barbiturates * Benzodiazepines * Calcium channel blockers * Carbamazepine * Carisoprodol * Cilostazol * Cyclobenzaprine * Dilazep * Dipyridamole * Estradiol * Ethanol * Flumazenil * Hexobendine * Hydroxyzine * Indomethacin * Inosine * KF24345 * Meprobamate * Nitrobenzylthioguanosine * Nitrobenzylthioinosine * Papaverine * Pentoxifylline * Phenothiazines * Phenytoin * Progesterone * Propentofylline * Propofol * Puromycin * R75231 * RE 102 BS * Soluflazine * Toyocamycin * Tracazolate * Tricyclic antidepressants See also * Adenosinergic * Reuptake inhibit ...
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Adenosin
Adenosine (symbol A) is an organic compound that occurs widely in nature in the form of diverse derivatives. The molecule consists of an adenine attached to a ribose via a β-N9-glycosidic bond. Adenosine is one of the four nucleoside building blocks of RNA (and its derivative deoxyadenosine is a building block of DNA), which are essential for all life. Its derivatives include the energy carriers adenosine mono-, di-, and triphosphate, also known as AMP/ADP/ATP. Cyclic adenosine monophosphate (cAMP) is pervasive in signal transduction. Adenosine is used as an intravenous medication for some cardiac arrhythmias. Adenosyl (abbreviated Ado or 5'-dAdo) is the chemical group formed by removal of the 5′-hydroxy (OH) group. It is found in adenosylcobalamin (an active form of vitamin B12) and as a radical in radical SAM enzymes. Medical uses Supraventricular tachycardia In individuals with supraventricular tachycardia (SVT), adenosine is used to help identify and convert the rhythm ...
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Calcium Channel Blocker
Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are a group of medications that disrupt the movement of calcium () through calcium channels. Calcium channel blockers are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients. Calcium channel blockers are also frequently used to alter heart rate (especially from atrial fibrillation), to prevent peripheral and cerebral vasospasm, and to reduce chest pain caused by angina pectoris. N-type, L-type, and T-type voltage-dependent calcium channels are present in the zona glomerulosa of the human adrenal gland, and CCBs can directly influence the biosynthesis of aldosterone in adrenocortical cells, with consequent impact on the clinical treatment of hypertension with these agents. CCBs have b ...
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Inosine
Inosine is a nucleoside that is formed when hypoxanthine is attached to a ribose ring (also known as a ribofuranose) via a β-N9-glycosidic bond. It was discovered in 1965 in analysis of RNA transferase. Inosine is commonly found in tRNAs and is essential for proper translation of the genetic code in wobble base pairs. Knowledge of inosine metabolism has led to advances in immunotherapy in recent decades. Inosine monophosphate is oxidised by the enzyme inosine monophosphate dehydrogenase, yielding xanthosine monophosphate, a key precursor in purine metabolism. Mycophenolate mofetil is an anti-metabolite, anti-proliferative drug that acts as an inhibitor of inosine monophosphate dehydrogenase. It is used in the treatment of a variety of autoimmune diseases including granulomatosis with polyangiitis because the uptake of purine by actively dividing B cells can exceed 8 times that of normal body cells, and, therefore, this set of white cells (which cannot operate purine salvage p ...
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Indomethacin
Indometacin, also known as indomethacin, is a nonsteroidal anti-inflammatory drug (NSAID) commonly used as a prescription drug, prescription medication to reduce fever, pain, joint stiffness, stiffness, and swelling (medical), swelling from inflammation. It works by inhibiting the production of prostaglandins, endogenous signaling molecules known to cause these symptoms. It does this by inhibiting cyclooxygenase, an enzyme that catalyzes the production of prostaglandins. It was patented in 1961 and approved for medical use in 1963. It is on the WHO Model List of Essential Medicines, World Health Organization's List of Essential Medicines. In 2020, it was the 320th most commonly prescribed medication in the United States, with more than 800thousand prescriptions. Medical uses As an NSAID, indometacin is an analgesic, anti-inflammatory, and antipyretic. Clinical indications for indometacin include: Joint diseases *rheumatoid arthritis *ankylosing spondylitis *osteoarthritis *gouty ...
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Hydroxyzine
Hydroxyzine, sold under the brand names Atarax, Vistaril and others, is an antihistamine medication. It is used in the treatment of itchiness, insomnia, anxiety, and nausea, including that due to motion sickness. It is used either by mouth or injection into a muscle. Common side effects include sleepiness, headache, and a dry mouth. Serious side effects may include QT prolongation. It is unclear if use during pregnancy or breastfeeding is safe. Hydroxyzine works by blocking the effects of histamine. It is a first-generation antihistamine in the piperazine family of chemicals. It was first made by Union Chimique Belge in 1956 and was approved for sale by Pfizer in the United States later that year. In 2020, it was the 70th most commonly prescribed medication in the United States, with more than 10million prescriptions. Medical uses Hydroxyzine is used in the treatment of itchiness, anxiety, and nausea due to motion sickness. A systematic review concluded that hydroxyzine out ...
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Hexobendine
Hexobendine is a vasodilator that acts as an adenosine reuptake inhibitor. Synthesis The reaction between 3,4,5-trimethoxybenzoyl chloride 521-61-3(1) and 3-chloropropanol 27-30-5(2) gives the corresponding ester, i.e. 3-chloropropyl 3,4,5-trimethoxybenzoateCID:12350731 029-24-9(3). The last step involves the reaction between two molar equivalents of 3 with one molar equivalent of N,N’-dimethylethanediamine 10-70-3(4) completing the synthesis of hexobendine (5). See also * Dilazep Dilazep is a vasodilator that acts as an adenosine reuptake inhibitor. It is used for the treatment of cardiopathy and renal disorders. Synthesis The reaction of bis-(3-hydroxypropyl)-ethylene diamine (1) with 1-Bromo-3-chloropropane (2) give ... References Vasodilators Phenol ethers Benzoate esters Amines Adenosine reuptake inhibitors {{cardiovascular-drug-stub ...
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Flumazenil
Flumazenil (also known as flumazepil, code name Ro 15-1788) is a selective GABAA receptor antagonist administered via injection, otic insertion, or intranasally. Therapeutically, it acts as both an antagonist and antidote to benzodiazepines (particularly in cases of overdose), through competitive inhibition. It was first characterized in 1981, and was first marketed in 1987 by Hoffmann-La Roche under the trade name Anexate. However, it did not receive FDA approval until December 20, 1991. The developer lost its exclusive patent rights in 2008; so at present, generic formulations of this drug are available. Intravenous flumazenil is primarily used to treat benzodiazepine overdoses and to help reverse anesthesia. Administration of flumazenil by sublingual lozenge and topical cream has also been tested. Medical uses Flumazenil benefits patients who become excessively drowsy after use of benzodiazepines for either diagnostic or therapeutic procedures. The drug has been used as ...
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Ethanol
Ethanol (abbr. EtOH; also called ethyl alcohol, grain alcohol, drinking alcohol, or simply alcohol) is an organic compound. It is an Alcohol (chemistry), alcohol with the chemical formula . Its formula can be also written as or (an ethyl group linked to a hydroxyl group). Ethanol is a Volatility (chemistry), volatile, Combustibility and flammability, flammable, colorless liquid with a characteristic wine-like odor and pungent taste. It is a psychoactive recreational drug, the active ingredient in alcoholic drinks. Ethanol is naturally produced by the fermentation process of Carbohydrate, sugars by yeasts or via Petrochemistry, petrochemical processes such as ethylene hydration. It has medical applications as an antiseptic and disinfectant. It is used as a chemical solvent and in the Chemical synthesis, synthesis of organic compounds, and as a Alcohol fuel, fuel source. Ethanol also can be dehydrated to make ethylene, an important chemical feedstock. As of 2006, world produ ...
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Estradiol
Estradiol (E2), also spelled oestradiol, is an estrogen steroid hormone and the major female sex hormone. It is involved in the regulation of the estrous and menstrual female reproductive cycles. Estradiol is responsible for the development of female secondary sexual characteristics such as the breasts, widening of the hips and a female-associated pattern of fat distribution. It is also important in the development and maintenance of female reproductive tissues such as the mammary glands, uterus and vagina during puberty, adulthood and pregnancy. It also has important effects in many other tissues including bone, fat, skin, liver, and the brain. Though estradiol levels in males are much lower than in females, estradiol has important roles in males as well. Apart from humans and other mammals, estradiol is also found in most vertebrates and crustaceans, insects, fish, and other animal species. Estradiol is produced especially within the follicles of the ovaries, but also in o ...
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Dipyridamole
Dipyridamole (trademarked as Persantine and others) is a nucleoside transport inhibitor and a PDE3 inhibitor medication that inhibits blood clot formation when given chronically and causes blood vessel dilation when given at high doses over a short time. Medical uses * Dipyridamole is used to dilate blood vessels in people with peripheral arterial disease and coronary artery disease * Dipyridamole has been shown to lower pulmonary hypertension without significant drop of systemic blood pressure * It inhibits formation of pro-inflammatory cytokines (MCP-1, MMP-9) in vitro and results in reduction of hsCRP in patients. * It inhibits proliferation of smooth muscle cells in vivo and modestly increases unassisted patency of synthetic arteriovenous hemodialysis grafts. * It increases the release of tissue plasminogen activator from brain microvascular endothelial cells. * It results in an increase of 13-hydroxyoctadecadienoic acid and decrease of 12-hydroxyeicosatetraenoic acid in ...
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Dilazep
Dilazep is a vasodilator that acts as an adenosine reuptake inhibitor. It is used for the treatment of cardiopathy and renal disorders. Synthesis The reaction of bis-(3-hydroxypropyl)-ethylene diamine (1) with 1-Bromo-3-chloropropane (2) gives homopiperazine 9970-80-0 (3). Esterification by reaction with 3,4,5-Trimethoxybenzoyl Chloride 521-61-3(4) completed the synthesis of Dilazep (5). See also * Hexobendine Hexobendine is a vasodilator that acts as an adenosine reuptake inhibitor An adenosine reuptake inhibitor (AdoRI) is a type of drug which acts as a reuptake inhibitor for the purine nucleoside and neurotransmitter adenosine by blocking the acti ..., a drug with similar chemical structure References Vasodilators Pyrogallol ethers Benzoate esters Diazepanes Adenosine reuptake inhibitors {{cardiovascular-drug-stub ...
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Cyclobenzaprine
Cyclobenzaprine (sold under the brand name Flexeril, among others) is a medication used for muscle spasms from musculoskeletal conditions of sudden onset. It is not useful in cerebral palsy. It is taken by mouth. Use is not recommended for more than a few weeks. Common side effects include headache, feeling tired, dizziness, and dry mouth. Serious side effects may include an irregular heartbeat. There is no evidence of harm in pregnancy, but it has not been well studied in this population. It should not be used with an MAO inhibitor. How it works is unclear. Cyclobenzaprine was approved for medical use in the United States in 1977. It is available as a generic medication. In 2020, it was the 39th most commonly prescribed medication in the United States, with more than 16million prescriptions. It was not available in the United Kingdom as of 2012. Medical use Cyclobenzaprine is used, in conjunction with physical therapy, to treat muscle spasms that occur because of acute m ...
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