3,4-methylenedioxyphenethylamine
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3,4-methylenedioxyphenethylamine
3,4-Methylenedioxyphenethylamine, also known as 3,4-MDPEA, MDPEA, and homopiperonylamine, is a substituted phenethylamine formed by adding a methylenedioxy group to phenethylamine. It is structurally similar to MDA, but without the methyl group at the alpha position. According to Alexander Shulgin in his book '' PiHKAL'', MDPEA appears to be biologically inactive. This is likely because of extensive first-pass metabolism by the enzyme monoamine oxidase. However, if MDPEA were either used in high enough of doses (e.g., 1-2 grams), or in combination with a monoamine oxidase inhibitor (MAOI), it is probable that it would become sufficiently active, though it would likely have a relatively short duration of action. This idea is similar in concept to the use of selective MAOA inhibitors and selective MAOB inhibitors in augmentation of dimethyltryptamine (DMT) and phenethylamine (PEA), respectively. See also * Substituted methylenedioxyphenethylamine Substituted methylene ...
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Substituted Methylenedioxyphenethylamine
Substituted methylenedioxy- phenethylamines (MDxx) are a large chemical class of derivatives of the phenethylamines, which includes many psychoactive drugs that act as entactogens, psychedelics, and/or stimulants, as well as entheogens. These agents are used as research chemicals, designer drugs and as recreational substances. The base compound of the MDxx class is 3,4-methylenedioxyphenethylamine (MDPEA), and the prototypical agent of this class is 3,4-methylenedioxy-''N''-methylamphetamine (MDMA; "ecstasy"). Other mentionables include 3,4-methylenedioxyamphetamine (MDA), 3,4-methylenedioxy-''N''-ethylamphetamine (MDEA; "Eve"), ''N''-methyl-1,3-benzodioxolylbutanamine (MBDB; "Eden"), and 3,4-methylenedioxy-''N''-methylcathinone (βk-MDMA; "Methylone"). List of substituted methylenedioxyphenethylamines The compounds most commonly regarded as comprising the family of MDxx derivatives include: Related compounds In addition, there are a number of other compounds that ...
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Poland
Poland, officially the Republic of Poland, is a country in Central Europe. It is divided into 16 administrative provinces called voivodeships, covering an area of . Poland has a population of over 38 million and is the fifth-most populous member state of the European Union. Warsaw is the nation's capital and largest metropolis. Other major cities include Kraków, Wrocław, Łódź, Poznań, Gdańsk, and Szczecin. Poland has a temperate transitional climate and its territory traverses the Central European Plain, extending from Baltic Sea in the north to Sudeten and Carpathian Mountains in the south. The longest Polish river is the Vistula, and Poland's highest point is Mount Rysy, situated in the Tatra mountain range of the Carpathians. The country is bordered by Lithuania and Russia to the northeast, Belarus and Ukraine to the east, Slovakia and the Czech Republic to the south, and Germany to the west. It also shares maritime boundaries with Denmark and Sweden. ...
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Augmentation (psychiatry)
Augmentation, in the context of the pharmacological management of psychiatry, refers to the combination of two or more drugs to achieve better treatment results. Examples include: *Prescribing an atypical antipsychotic when someone is already taking a selective serotonin reuptake inhibitor for the treatment of depression. *Prescribing estrogen for someone already being treated with antipsychotics for the management of schizophrenia. *Giving an adenosine A2A receptor antagonist on top of existing treatment for Parkinson's disease. In pharmacology, the term is occasionally used to describe treatments that increase (augment) the concentration of some substance in the body. This might be done when someone is deficient in a hormone, enzyme, or other endogenous substance. For example: *Use of DDCIs in addition to L-DOPA, to reduce conversion of L-DOPA outside the brain. *To give α1 antitrypsin to someone with alpha 1-antitrypsin deficiency Alpha-1 antitrypsin deficiency (A1AD or A ...
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Dimethyltryptamine
''N'',''N''-Dimethyltryptamine (DMT or ''N'',''N''-DMT, SPL026) is a substituted tryptamine that occurs in many plants and animals, including human beings, and which is both a derivative and a structural analog of tryptamine. It is used as a psychedelic drug and prepared by various cultures for ritual purposes as an entheogen. DMT has a rapid onset, intense effects, and a relatively short duration of action. For those reasons, DMT was known as the "business trip" during the 1960s in the United States, as a user could access the full depth of a psychedelic experience in considerably less time than with other substances such as LSD or psilocybin mushrooms. DMT can be inhaled, ingested, or injected and its effects depend on the dose, as well as the mode of administration. When inhaled or injected, the effects last a short period of time: about five to 15 minutes. Effects can last three hours or more when orally ingested along with a monoamine oxidase inhibitor (MAOI), such as ...
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Augmentation (psychiatry)
Augmentation, in the context of the pharmacological management of psychiatry, refers to the combination of two or more drugs to achieve better treatment results. Examples include: *Prescribing an atypical antipsychotic when someone is already taking a selective serotonin reuptake inhibitor for the treatment of depression. *Prescribing estrogen for someone already being treated with antipsychotics for the management of schizophrenia. *Giving an adenosine A2A receptor antagonist on top of existing treatment for Parkinson's disease. In pharmacology, the term is occasionally used to describe treatments that increase (augment) the concentration of some substance in the body. This might be done when someone is deficient in a hormone, enzyme, or other endogenous substance. For example: *Use of DDCIs in addition to L-DOPA, to reduce conversion of L-DOPA outside the brain. *To give α1 antitrypsin to someone with alpha 1-antitrypsin deficiency Alpha-1 antitrypsin deficiency (A1AD or A ...
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Monoamine Oxidase B
Monoamine oxidase B, also known as MAOB, is an enzyme that in humans is encoded by the ''MAOB'' gene. The protein encoded by this gene belongs to the flavin monoamine oxidase family. It is an enzyme located in the outer mitochondrial membrane. It catalyzes the oxidative deamination of biogenic and xenobiotic amines and plays an important role in the catabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues (such as dopamine). This protein preferentially degrades benzylamine and phenethylamine. Similarly to monoamine oxidase A (MAOA), it also degrades dopamine hough some new research contradicts this, suggesting that MAOB does ''not'' directly degrade dopamine, but is responsible for GABA synthesis Structure Monoamine oxidase B has a hydrophobic bipartite elongated cavity that (for the "open" conformation) occupies a combined volume close to 700 Å3. hMAO-A has a single cavity that exhibits a rounder shape and is larger in volume t ...
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Monoamine Oxidase A
Monoamine oxidase A, also known as MAO-A, is an enzyme that in humans is encoded by the ''MAOA'' gene. This gene is one of two neighboring gene family members that encode mitochondrial enzymes which catalyze the oxidative deamination of amines, such as dopamine, norepinephrine, and serotonin. A mutation of this gene results in Brunner syndrome. This gene has also been associated with a variety of other psychiatric disorders, including antisocial behavior. Alternatively spliced transcript variants encoding multiple isoforms have been observed. Structures Gene Monoamine oxidase A, also known as MAO-A, is an enzyme that in humans is encoded by the ''MAOA'' gene. The promoter of ''MAOA'' contains conserved binding sites for Sp1, GATA2, and TBP. This gene is adjacent to a related gene (''MAOB'') on the opposite strand of the X chromosome. In humans, there is a 30-base repeat sequence repeated several different numbers of times in the promoter region of MAO-A. There are 2R (tw ...
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Functional Selectivity
Functional selectivity (or “agonist trafficking”, “biased agonism”, “biased signaling”, "ligand bias" and “differential engagement”) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the endogenous hormone or peptide) at the same receptor. Functional selectivity can be present when a receptor has several possible signal transduction pathways. To which degree each pathway is activated thus depends on which ligand binds to the receptor. Functional selectivity, or biased signaling, is most extensively characterized at G protein coupled receptors (GPCRs). A number of biased agonists, such as those at muscarinic M2 receptors tested as analgesics or antiproliferative drugs, or those at opioid receptors that mediate pain, show potential at various receptor families to increase beneficial properties while reducing side effects. For example, pre-clinical studies with G protein biased agonists at the μ-opioid re ...
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Drug Action
The action of drugs on the human body (or any other organism's body) is called pharmacodynamics, and the body's response to drugs is called pharmacokinetics. The drugs that enter an individual tend to stimulate certain receptors, ion channels, act on enzymes or transport proteins. As a result, they cause the human body to react in a specific way. Based on drug action on receptors, there are 2 different types of drugs: *Agonists – they stimulate and activate the receptors *Antagonists – they disable the agonists from stimulating the receptors Once the receptors are activated, they either trigger a particular response directly on the body, or they trigger the release of hormones and/or other endogenous drugs in the body to stimulate a particular response. Short note on receptors Drugs interact with receptors by bonding at specific binding sites. Most receptors are made up of proteins, and the drugs can therefore interact with the amino acids to change the conformation of the ...
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Time
Time is the continued sequence of existence and events that occurs in an apparently irreversible succession from the past, through the present, into the future. It is a component quantity of various measurements used to sequence events, to compare the duration of events or the intervals between them, and to quantify rates of change of quantities in material reality or in the conscious experience. Time is often referred to as a fourth dimension, along with three spatial dimensions. Time has long been an important subject of study in religion, philosophy, and science, but defining it in a manner applicable to all fields without circularity has consistently eluded scholars. Nevertheless, diverse fields such as business, industry, sports, the sciences, and the performing arts all incorporate some notion of time into their respective measuring systems. 108 pages. Time in physics is operationally defined as "what a clock reads". The physical nature of time is addre ...
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Monoamine Oxidase Inhibitor
Monoamine oxidase inhibitors (MAOIs) are a class of drugs that inhibit the activity of one or both monoamine oxidase enzymes: monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B). They are best known as effective antidepressants, especially for treatment-resistant depression and atypical depression. They are also used to treat panic disorder, social anxiety disorder, Parkinson's disease, and several other disorders. Reversible inhibitors of monoamine oxidase A (RIMAs) are a subclass of MAOIs that selectively and reversibly inhibit the MAO-A enzyme. RIMAs are used clinically in the treatment of depression and dysthymia. Due to their reversibility, they are safer in single-drug overdose than the older, irreversible MAOIs, and weaker in increasing the monoamines important in depressive disorder. RIMAs have not gained widespread market share in the United States. Medical uses MAOIs have been found to be effective in the treatment of panic disorder with agoraphobia ...
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Dose (biochemistry)
A dose is a measured quantity of a medicine, nutrient, or pathogen which is delivered as a unit. The greater the quantity delivered, the larger the dose. Doses are most commonly measured for compounds in medicine. The term is usually applied to the quantity of a drug or other agent administered for therapeutic purposes, but may be used to describe any case where a substance is introduced to the body. In nutrition, the term is usually applied to how much of a specific nutrient is in a person's diet or in a particular food, meal, or dietary supplement. For bacterial or viral agents, dose typically refers to the amount of the pathogen required to infect a host. For information on dosage of toxic substances, see Toxicology. For information on excessive intake of pharmaceutical agents, see Drug overdose. In clinical pharmacology, dose refers to dosage or amount of dose administered to a person, whereas exposure means the time-dependent concentration (often in the circulatory blood ...
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