Alpha-Methylserotonin
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Alpha-Methylserotonin
α-Methylserotonin (αMS), also known as α-methyl-5-hydroxytryptamine (α-methyl-5-HT) or 5-hydroxy-α-methyltryptamine (5-HO-αMT), is a tryptamine derivative closely related to the neurotransmitter serotonin (5-HT). It acts as a non- selective serotonin receptor agonist and has been used extensively in scientific research to study the function of the serotonin system. Unlike serotonin, αMS is not metabolized by monoamine oxidase on account of the α-methyl substituent blocking the enzyme's access to the amine. As a result, it has a much longer half-life in comparison. Similarly to serotonin however, αMS poorly crosses the blood-brain-barrier due to its free hydroxyl group, and thus has only weak or no central effects when administered peripherally. α-Methyltryptophan (αMTP) is a prodrug to αMS which does cross the blood-brain-barrier and thus efficiently delivers αMS into the central nervous system. As a result, αMTP acts as an orally bioavailable false or substit ...
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Federal Analogue Act
The Federal Analogue Act, , is a section of the United States Controlled Substances Act passed in 1986 which allows any chemical "substantially similar" to a controlled substance listed in Schedule I or II to be treated as if it were listed in Schedule I, but only if intended for human consumption. These similar substances are often called designer drugs. The law's constitutionality has been questioned by now Supreme Court Justice Neil Gorsuch; its broad reach has been used to successfully prosecute possession of chemicals openly sold as dietary supplements and naturally contained in foods such as chocolate. Definition (32) *(A) Except as provided in subparagraph (C), the term ''controlled substance analogue'' means a substance - **(i) the chemical structure of which is substantially similar to the chemical structure of a controlled substance in schedule I or II; **(ii) which has a stimulant, depressant, or hallucinogenic effect on the central nervous system that is substantial ...
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Hydroxyl
In chemistry, a hydroxy or hydroxyl group is a functional group with the chemical formula and composed of one oxygen atom covalently bonded to one hydrogen atom. In organic chemistry, alcohols and carboxylic acids contain one or more hydroxy groups. Both the negatively charged anion , called hydroxide, and the neutral radical , known as the hydroxyl radical, consist of an unbonded hydroxy group. According to IUPAC definitions, the term ''hydroxyl'' refers to the hydroxyl radical () only, while the functional group is called a ''hydroxy group''. Properties Water, alcohols, carboxylic acids, and many other hydroxy-containing compounds can be readily deprotonated due to a large difference between the electronegativity of oxygen (3.5) and that of hydrogen (2.1). Hydroxy-containing compounds engage in intermolecular hydrogen bonding increasing the electrostatic attraction between molecules and thus to higher boiling and melting points than found for compounds that lack this f ...
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Florida
Florida is a state located in the Southeastern region of the United States. Florida is bordered to the west by the Gulf of Mexico, to the northwest by Alabama, to the north by Georgia, to the east by the Bahamas and Atlantic Ocean, and to the south by the Straits of Florida and Cuba; it is the only state that borders both the Gulf of Mexico and the Atlantic Ocean. Spanning , Florida ranks 22nd in area among the 50 states, and with a population of over 21 million, it is the third-most populous. The state capital is Tallahassee, and the most populous city is Jacksonville. The Miami metropolitan area, with a population of almost 6.2 million, is the most populous urban area in Florida and the ninth-most populous in the United States; other urban conurbations with over one million people are Tampa Bay, Orlando, and Jacksonville. Various Native American groups have inhabited Florida for at least 14,000 years. In 1513, Spanish explorer Juan Ponce de León became the first k ...
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Controlled Substance
A controlled substance is generally a drug or chemical whose manufacture, possession and use is regulated by a government, such as illicitly used drugs or prescription medications that are designated by law. Some treaties, notably the Single Convention on Narcotic Drugs, the Convention on Psychotropic Substances, and the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances, provide internationally agreed-upon "schedules" of controlled substances, which have been incorporated into national laws; however, national laws usually significantly expand on these international conventions. Some precursor chemicals used for the production of illegal drugs are also controlled substances in many countries, even though they may lack the pharmacological effects of the drugs themselves. Substances are classified according to schedules and consist primarily of potentially psychoactive substances and anabolic steroids. The controlled substances do not ...
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Federal Analog Act
The Federal Analogue Act, , is a section of the United States Controlled Substances Act passed in 1986 which allows any chemical "substantially similar" to a controlled substance listed in Controlled Substances Act#Schedule I controlled substances, Schedule I or Controlled Substances Act#Schedule II controlled substances, II to be treated as if it were listed in Schedule I, but only if intended for human consumption. These similar substances are often called designer drugs. The law's constitutionality has been questioned by now Supreme Court Justice Neil Gorsuch; its broad reach has been used to successfully prosecute possession of chemicals openly sold as dietary supplements and naturally contained in foods such as chocolate. Definition (32) *(A) Except as provided in subparagraph (C), the term ''controlled substance analogue'' means a substance - **(i) the chemical structure of which is substantially similar to the chemical structure of a controlled substance in schedule I or I ...
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Structural Analogue
A structural analog (analogue in modern traditional English; Commonwealth English), also known as a chemical analog or simply an analog, is a compound having a 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 isoelectronic. Despite a high chemical similarity, structural analogs are not necessarily 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 screened for structural analogs of a lead compound. Chemical analogues of ille ...
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False Neurotransmitter
A false neurotransmitter is a chemical compound which closely imitates the action of a neurotransmitter in the nervous system. Examples include 5-MeO-αMT (mimicking serotonin) and α-methyldopa. These chemicals can be accumulated by a neuron or secretory cell, are then packaged in secretory / synaptic vesicles, and then released with other neurotransmitters when an action potential provides the necessary stimulus for release. The concept of a false transmitter is credited to Irwin Kopin of the National Institute of Neurological Disorders and Stroke who determined that the drug tyramine increased blood pressure by being loaded and then released from secretory vesicles of the adrenal chromaffin cells. Tyramine can also be converted into octopamine by the dopamine-beta-hydroxylase (DBH) which itself acts as a false transmitter by displacing noradrenaline from its vesicle but not activating the postsynaptic alpha adrenoreceptor. There is growing evidence that a large number of well ...
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Bioavailability
In pharmacology, bioavailability is a subcategory of absorption and is the fraction (%) of an administered drug that reaches the systemic circulation. By definition, when a medication is administered intravenously, its bioavailability is 100%. However, when a medication is administered via routes other than intravenous, its bioavailability is generally lower than that of intravenous due to intestinal endothelium absorption and first-pass metabolism. Thereby, mathematically, bioavailability equals the ratio of comparing the area under the plasma drug concentration curve versus time (AUC) for the extravascular formulation to the AUC for the intravascular formulation. AUC is used because AUC is proportional to the dose that has entered the systemic circulation. Bioavailability of a drug is an average value; to take population variability into account, deviation range is shown as ±. To ensure that the drug taker who has poor absorption is dosed appropriately, the bottom value o ...
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Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as 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 willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ...
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Prodrug
A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted (ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects. History Many herbal extracts historically used in medicine contain glycosides (sugar derivatives) of the active agent, which are hydrolyzed in the intestines to release the active and more bioavailable aglycone. For example, salicin is a β-D-glucopyranosid ...
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