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DOPR
2,5-Dimethoxy-4-propylamphetamine (DOPR) is a psychedelic drug of the phenethylamine, amphetamine, and DOx families. It was first synthesized by Alexander Shulgin, and was described in his book ''PiHKAL'' (''Phenethylamines i Have Known And Loved''). Very little data exists about the pharmacological properties, metabolism, and toxicity of DOPR. Use and effects According to Alexander Shulgin in ''PiHKAL'', the dosage of DOPR is 2.5 to 5mg and its duration is 20 to 30hours. He described DOPR as a "heavy duty psychedelic", complete with alterations of the thought process and visual distortion. Pharmacology Pharmacodynamics DOPR acts as an agonist of the serotonin 5-HT2 receptors, including of the serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors. It has very weak affinity for the serotonin 5-HT1 receptor. It produces the head-twitch response (HTR), a behavioral proxy of psychedelic effects, in rodents. As with many other psychedelics, DOPR shows an inverted U-shaped dose– ...
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Pro-motivational Agent
A motivation-enhancing drug, also known as a pro-motivational drug, is a drug which increases motivation. Drugs enhancing motivation can be used in the treatment of motivational deficits, for instance in depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD). They can also be used in the treatment of disorders of diminished motivation (DDMs), including apathy, abulia, and akinetic mutism, disorders that can be caused by conditions like stroke, traumatic brain injury (TBI), and neurodegenerative diseases. Motivation-enhancing drugs are used non-medically by healthy people to increase motivation and productivity as well, for instance in educational contexts. There are limited clinical data on medications in treating motivational deficits and disorders. In any case, drugs used for pro-motivational purposes are generally dopaminergic agents, for instance dopamine reuptake inhibitors (DRIs) like methylphenidate and modafinil, dopamine releasing agents (DRA ...
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2,5-dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine (DOET) is a psychedelic drug of the phenethylamine, amphetamine, and DOx families. It is closely related to DOM and is a synthetic analogue of the naturally occurring phenethylamine psychedelic mescaline. The drug acts as a selective agonist of the serotonin 5-HT2 receptors, including of the serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptors. DOET was first discovered by Alexander Shulgin in the 1960s. It was clinically studied at low and sub-hallucinogenic doses for potential use as a pharmaceutical drug acting as a " psychic energizer" by Dow Chemical Company in the 1960s. However, its development was terminated after DOM emerged as a street drug and caused a public health crisis in San Francisco in 1967. Nonetheless, DOET's effects at low doses were extensively characterized in small clinical trials. The psychedelic effects of DOET at higher doses were subsequently described by Shulgin in his book PiHKAL in 1991. DOET is taken by ...
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Substituted Amphetamine
Substituted amphetamines, or simply amphetamines, are a chemical class, class of compounds based upon the amphetamine structure; it includes all derivative (chemistry), derivative compounds which are formed by replacing, or substitution reaction, substituting, one or more hydrogen atoms in the amphetamine core structure with substituents. The compounds in this class span a variety of pharmacological subclasses, including stimulants, Empathogen-entactogen, empathogens, and hallucinogens, among others. Examples of substituted amphetamines are amphetamine (itself), methamphetamine, ephedrine, cathinone, phentermine, mephentermine, tranylcypromine, bupropion, methoxyphenamine, selegiline, amfepramone, amfepramone (diethylpropion), pyrovalerone, MDMA (ecstasy), and 2,5-dimethoxy-4-methylamphetamine, DOM (STP). Some of amphetamine's substituted Derivative (chemistry), derivatives occur in nature, for example in the leaves of ''Ephedra (genus), Ephedra'' and khat plants. Amphetamine w ...
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PiHKAL
''PiHKAL: A Chemical Love Story'' is a book by Alexander Shulgin and Ann Shulgin published in 1991. The subject of the work is Psychoactive drug, psychoactive phenethylamine Derivative (chemistry), chemical derivatives, notably those that act as psychedelic drug, psychedelics and/or empathogen-entactogens. The main title, PiHKAL, is an acronym that stands for "Phenethylamines I Have Known and Loved". The book is arranged into two parts, the first part being a fictionalized autobiography of the couple and the second part describing 179 different psychedelic compounds (most of which Shulgin discovered himself), including detailed synthesis instructions, bioassays, dosages, and other commentary. The second part was made freely available by Shulgin on Erowid while the first part is available only in the printed text. While the reactions described are beyond the ability of people with a basic chemistry education, some tend to emphasize techniques that do not require difficult-to-ob ...
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Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ...
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5-HT2B Receptor
5-Hydroxytryptamine receptor 2B (5-HT2B) also known as serotonin receptor 2B is a protein that in humans is encoded by the ''HTR2B'' gene. 5-HT2B is a member of the 5-HT2 receptor, 5-HT2 receptor family that binds the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). Like all 5-HT2 receptors, the 5-HT2B receptor is Gq protein, Gq/G11-protein coupled, leading to downstream activation of phospholipase C. Tissue distribution and function First discovered in the stomach of rats, 5-HT2B was challenging to characterize initially because of its structural similarity to the other 5-HT2 receptors, particularly 5-HT2C. The 5-HT2 receptors (of which the 5-HT2B receptor is a subtype) mediate many of the central and peripheral physiologic functions of serotonin. Cardiovascular effects include contraction of blood vessels and shape changes in platelets; central nervous system (CNS) effects include neuronal sensitization to tactile stimuli and mediation of some of the effects of halluci ...
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Structural Analog
A structural analog, also known as a chemical analog or simply an analog, is a chemical compound, compound having a chemical structure, structure similar to that of another compound, but differing from it in respect to a certain component. It can differ in one or more atoms, functional groups, or substructures, which are replaced with other atoms, groups, or substructures. A structural analog can be imagined to be formed, at least theoretically, from the other compound. Structural analogs are often isoelectronicity, isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily functional analog (chemistry), functional analogs and can have very different physical, chemical, biochemical, or pharmacological properties. In drug discovery, either a large series of structural analogs of an initial lead compound are created and tested as part of a structure–activity relationship study or a database is virtual screening, screened for structural analogs of a ...
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Microdosing
Microdosing, or micro-dosing, involves the administration of sub-therapeutic doses of drugs to study their effects in humans, aiming to gather preliminary data on safety, pharmacokinetics, and potential therapeutic benefits without producing significant physiological effects. This is called a " Phase 0 study" and is usually conducted before clinical Phase I to predict whether a drug is viable for the next phase of testing. Human microdosing aims to reduce the resources spent on non-viable drugs and the amount of testing done on animals. Less commonly, the term "microdosing" can be used to refer to precise dispensing of small amounts of a drug substance (, a powder API) for a drug product (, a capsule) and, when the drug substance also happens to be liquid, this can potentially overlap with the term microdispensing . Techniques The basic approach is to label a candidate drug using the radio isotope carbon-14, then administer the compound to human volunteers at levels typi ...
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Hyperlocomotion
Locomotor activity is a measure of animal behavior which is employed in scientific research. Hyperlocomotion, also known as locomotor hyperactivity, hyperactivity, or increased locomotor activity, is an effect of certain drugs in animals in which locomotor activity (locomotion) is increased. It is induced by certain drugs like psychostimulants and NMDA receptor antagonists and is reversed by certain other drugs like antipsychotics and certain antidepressants. Stimulation of locomotor activity is thought to be mediated by increased signaling in the nucleus accumbens, a major brain area involved in behavioral activation and motivated behavior. Hypolocomotion, also known as locomotor hypoactivity, hypoactivity, and decreased locomotor activity, is an effect of certain drugs in animals in which locomotor activity is decreased. It is a characteristic effect of many sedative agents and general anesthetics. Antipsychotics, which are dopamine receptor antagonists, and many serotonerg ...
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Inverted U-shaped Curve
In mathematics, a parabola is a plane curve which is mirror-symmetrical and is approximately U-shaped. It fits several superficially different mathematical descriptions, which can all be proved to define exactly the same curves. One description of a parabola involves a point (the focus) and a line (the directrix). The focus does not lie on the directrix. The parabola is the locus of points in that plane that are equidistant from the directrix and the focus. Another description of a parabola is as a conic section, created from the intersection of a right circular conical surface and a plane parallel to another plane that is tangential to the conical surface. The graph of a quadratic function y=ax^2+bx+ c (with a\neq 0 ) is a parabola with its axis parallel to the -axis. Conversely, every such parabola is the graph of a quadratic function. The line perpendicular to the directrix and passing through the focus (that is, the line that splits the parabola through the middle) ...
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