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Descarboxylysergic Acid
Descarboxylysergic acid, or 8-descarboxylysergic acid, also known as 9,10-didehydro-6-methylergoline or as 6-methyl-9-ergolene, is a drug of the ergoline family related to lysergic acid and lysergamides like lysergic acid diethylamide (LSD). It is the analogue of lysergic acid in which the carboxyl group at the C8 position of the molecule has been removed. Descarboxylysergic acid was synthesized in an attempt to help elucidate the minimum structural requirements for biological activity of ergoline and lysergamide drugs like LSD. Pharmacology In contrast to lysergic acid, which is said to have "very unexceptional biological activity", descarboxylysergic acid was, surprisingly, found to produce effects in mice that were described as remarkably similar to those of LSD. However, it was said that the specific tests performed were not reliably indicative of hallucinogenic effects in humans. Moreover, no other assays of hallucinogen-type effects were carried out, and descarboxylysergi ...
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Drug
A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a re ...
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Serotonergic Agent
A serotonergic substance, medication, or receptor protein is one that affects neurotransmission pathways that involve serotonin, as follows: * Serotonergic drugs ** Serotonin receptor agonists ** Serotonin receptor antagonists ** Serotonin reuptake inhibitors ** Serotonin releasing agents ** Serotonergic psychedelics * Serotonergic cells ** Serotonergic cell groups A serotonergic substance, medication, or receptor protein is one that affects neurotransmission pathways that involve serotonin, as follows: * Serotonergic drugs ** Serotonin receptor agonists ** Serotonin receptor antagonists ** Serotonin reupta ...
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Lysergine
Lysergine, also known as 9,10-didehydro-6,8β-dimethylergoline, is an ergot alkaloid and serotonin receptor agonist of the ergoline family. It is a minor constituent of ergot. Pharmacology Lysergine shows selectivity for activation of the serotonin 5-HT2A receptor over several other closely related serotonin receptors (54-fold over the 5-HT2B receptor, 38-fold over the 5-HT2C receptor, and 127-fold over the 5-HT1A receptor). The drug is a partial agonist of the 5-HT2A receptor with moderate intrinsic activity (Emax = 57%). An analogue of lysergine, (+)-13-fluorolysergol, is an even more selective agonist of the 5-HT2A receptor than lysergine (EC50 for 5-HT2B and 5-HT2C of >10,000nM). However, this compound has relatively weak maximal efficacy in activating the receptor (Emax = 17%). See also * Descarboxylysergic acid * Lysergic acid * Ergine * Lysergol * SDZ SER-082 SER-082, or SDZ SER-082, is a binding selectivity, selective serotonin 5-HT2B receptor, 5-HT2B and 5 ...
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Lisdexamfetamine
Lisdexamfetamine, sold under the brand names Vyvanse and Elvanse among others, is a stimulant medication that is used as a treatment for attention deficit hyperactivity disorder (ADHD) in children and adults and for moderate-to-severe binge eating disorder in adults. Lisdexamfetamine is taken by mouth. Its effects generally begin within 90 minutes and last for up to 14 hours. Common side effects of lisdexamfetamine include loss of appetite, anxiety, diarrhea, trouble sleeping, irritability, and nausea. Rare but serious side effects include mania, sudden cardiac death in those with underlying heart problems, and psychosis. It has a high potential for substance abuse. Serotonin syndrome may occur if used with certain other medications. Its use during pregnancy may result in harm to the baby and use during breastfeeding is not recommended by the manufacturer. Lisdexamfetamine is an inactive prodrug that works after being converted by the body into dextroamphetamine, ...
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Robert Oberlender
Robert Arthur Oberlender (born July 25, 1956) is an American medicinal chemist known for his work in the areas of serotonergic and dopaminergic drugs as well as drug discrimination. He is most well-known for his discovery and development of lisdexamfetamine (lysine–dextroamphetamine), which is now marketed as a pharmaceutical drug under the brand name Vyvanse and is prescribed as a misuse-resistant stimulant in the treatment of attention deficit hyperactivity disorder (ADHD) and other conditions. Biography Oberlender attended the pharmacy school of Temple University in his hometown of Philadelphia, Pennsylvania, receiving a bachelor's degree, and worked for two years as a pharmacist. Then, he started a Ph.D. program in medicinal chemistry at Purdue University in 1981. He worked in the lab of psychedelic chemist David E. Nichols studying psychedelics, entactogens, and related drugs, first completing his Ph.D. and then continuing in the lab as a postdoc. His first publication w ...
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Side Chain
In organic chemistry and biochemistry, a side chain is a substituent, chemical group that is attached to a core part of the molecule called the "main chain" or backbone chain, backbone. The side chain is a hydrocarbon branching element of a molecule that is attached to a larger hydrocarbon backbone. It is one factor in determining a molecule's properties and reactivity. A side chain is also known as a pendant chain, but a pendant group (side group) has a different definition. Conventions The placeholder R is often used as a generic placeholder for alkyl (saturated hydrocarbon) group side chains in structural formulae. To indicate other non-carbon groups in structure diagrams, X, Y, or Z are often used. History The ''R'' symbol was introduced by 19th-century French chemist Charles Frédéric Gerhardt, who advocated its adoption on the grounds that it would be widely recognizable and intelligible given its correspondence in multiple European languages to the initial letter of "r ...
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Methysergide
Methysergide, sold under the brand names Deseril and Sansert, is a monoaminergic medication of the ergoline and lysergamide groups which is used in the prophylaxis and treatment of migraine and cluster headaches. It has been withdrawn from the market in the United States and Canada due to safety concerns. It is taken by mouth. The drug is a prodrug of methylergometrine (methylergonovine), which circulates at levels about 10times higher than those of methysergide during treatment with methysergide. Whereas methysergide is a mixed agonist of some serotonin receptors (e.g., the 5-HT1 receptors) and antagonist of other serotonin receptors (e.g., the 5-HT2 receptors), methylergonovine is a non-selective agonist of most of the serotonin receptors, including of both the serotonin 5-HT1 and 5-HT2 receptor subgroups. Methysergide and methylergometrine are ergolines and lysergamides and are related to the ergot alkaloids. Previously thought to be an exclusively synthetic compound, ...
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Ergonovine
Ergonovine, also known as ergometrine and lysergic acid propanolamide, is a medication used to cause contractions of the uterus to treat heavy vaginal bleeding after childbirth. It can be used either by mouth, by injection into a muscle, or injection into a vein. Common side effects include high blood pressure, vomiting, seizures, headache, and low blood pressure. Other serious side effects include ergotism. Ergonovine was discovered in 1932. It is on the World Health Organization's List of Essential Medicines. Ergonovine is controlled in some countries because it can be used to make the psychedelic drug lysergic acid diethylamide (LSD). It is also known to produce psychedelic effects itself at high doses. Medical uses Ergonovine has a medical use in obstetrics to facilitate delivery of the placenta and to prevent bleeding after childbirth by causing smooth muscle tissue in the blood vessel walls to narrow, thereby reducing blood flow. It is usually combined with oxytoci ...
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Potency (pharmacology)
In pharmacology, potency or biological potency is a measure of a drug's biological activity expressed in terms of the dose required to produce a pharmacological effect of given intensity. A highly potent drug (e.g., fentanyl, clonazepam, risperidone, benperidol, bumetanide) evokes a given response at low concentrations, while a drug of lower potency (e.g. morphine, alprazolam, ziprasidone, haloperidol, furosemide) evokes the same response only at higher concentrations. Higher potency does not necessarily mean greater effectiveness nor more side effects nor less side effects. Types of potency The International Union of Basic and Clinical Pharmacology (IUPHAR) has stated that "potency is an imprecise term that should always be further defined", and lists of types of potency as follows: Miscellaneous Lysergic acid diethylamide (LSD) is one of the most potent psychoactive drug A psychoactive drug, psychopharmaceutical, mind-altering drug, consciousness-altering drug, ...
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Sympatholytic
A sympatholytic (sympathoplegic) drug is a medication that opposes the downstream effects of postganglionic nerve firing in effector organs innervated by the sympathetic nervous system (SNS). They are indicated for various functions; for example, they may be used as antihypertensives. They are also used to treat anxiety, such as generalized anxiety disorder, panic disorder and PTSD. In some cases, such as with guanfacine, they have also shown to be beneficial in the treatment of ADHD. Mechanisms of action Antiadrenergic agents inhibit the signals of epinephrine and norepinephrine. They are primarily postsynaptic adrenergic receptor antagonists (alpha and beta adrenergic receptor antagonists, or "blockers"), inhibiting the downstream cellular signaling pathways of adrenergic receptors. However, there are exceptions: guanfacine and clonidine are adrenergic agonists at the α2 receptor; since this receptor is located presynaptically, agonism at this receptor inhibits the presynaptic r ...
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Oxytocic
A uterotonic, also known as an oxytocic or ecbolic, is a type of medication used to induce contraction or greater tonicity of the uterus. Uterotonics are used both to induce labor and to reduce postpartum hemorrhage. Labor induction in the third trimester of pregnancy may be required due to medical necessity, or may be desired for social reasons. Generally, labor induction is indicated when the risk of carrying the pregnancy outweighs the risk of delivering. These reason include, but are not limited to, pregnancies that are prolonged, prelabor rupture of the fetal membranes, and concerns about the health and safety of the mother and/or child. There are multiple techniques available to stimulate uterine contractions including mechanical, pharmacological, and alternative medicine methods to initiate contractions prior to spontaneous onset of labor. Postpartum hemorrhage, also known as PPH, is defined as a loss of 500 mL or greater of blood within 24 hours after giving birth. It ...
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