Norfenefrine
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Norfenefrine
Norfenefrine (INN; also known as ''meta''-octopamine, 3-octopamine, and 3,β-dihydroxyphenethylamine) is an adrenergic agent used as a sympathomimetic drug which is marketed in Europe, Japan, and Mexico. Along with its structural isomer ''p''-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Some brand names for it include Coritat, Energona, Hypolind, and Novadral. See also * ''m''-Tyramine * Phenylephrine * Metaraminol * Ciclafrine Ciclafrine (INN) is a sympathomimetic phenethylamine and antihypertensive that was never marketed. Synthesis Ciclafrine can be prepared by the reaction of norfenefrine with cycloheptanone Cycloheptanone, (CH2)6CO, is a cyclic ketone also referr ... References Alpha-adrenergic agonists Cardiac stimulants Norepinephrine-dopamine releasing agents Neurotransmitters Phenols Phenylethanolamines TAAR1 agonists Trace amines {{ ...
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Hydrochloride
In chemistry, a hydrochloride is an acid salt resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (e.g. an amine). An alternative name is chlorhydrate, which comes from French. An archaic alternative name is muriate, derived from hydrochloric acid's ancient name: muriatic acid. Uses Converting amines into their hydrochlorides is a common way to improve their water solubility, which can be desirable for substances used in medications. The European Pharmacopoeia lists more than 200 hydrochlorides as active ingredients in medications. These hydrochlorides, compared to free bases, may more readily dissolve in the gastrointestinal tract and be absorbed into the bloodstream more quickly. Additionally, many hydrochlorides of amines have a longer shelf-life than their respective free bases. Amine hydrochlorides represent latent forms of a more reactive free base. In this regard, formation of an amine hydrochloride confers protection. This eff ...
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Neurotransmitter
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell. Neurotransmitters are released from synaptic vesicles into the synaptic cleft where they are able to interact with neurotransmitter receptors on the target cell. The neurotransmitter's effect on the target cell is determined by the receptor it binds. Many neurotransmitters are synthesized from simple and plentiful precursors such as amino acids, which are readily available and often require a small number of biosynthetic steps for conversion. Neurotransmitters are essential to the function of complex neural systems. The exact number of unique neurotransmitters in humans is unknown, but more than 100 have been identified. Common neurotransmitters include glutamate, GABA, acetylcholine, glycine and norepinephrine. Mechanism and cycle Synthes ...
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Phenols
In organic chemistry, phenols, sometimes called phenolics, are a class of chemical compounds consisting of one or more hydroxyl groups (— O H) bonded directly to an aromatic hydrocarbon group. The simplest is phenol, . Phenolic compounds are classified as simple phenols or polyphenols based on the number of phenol units in the molecule. Phenols are both synthesized industrially and produced by plants and microorganisms. Properties Acidity Phenols are more acidic than typical alcohols. The acidity of the hydroxyl group in phenols is commonly intermediate between that of aliphatic alcohols and carboxylic acids (their pKa is usually between 10 and 12). Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book). Condensation with aldehydes and ketones Phenols are susceptible to Electrophilic aromatic substitutions. Condensation with formald ...
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Neurotransmitters
A neurotransmitter is a signaling molecule secreted by a neuron to affect another cell across a synapse. The cell receiving the signal, any main body part or target cell, may be another neuron, but could also be a gland or muscle cell. Neurotransmitters are released from synaptic vesicles into the synaptic cleft where they are able to interact with neurotransmitter receptors on the target cell. The neurotransmitter's effect on the target cell is determined by the receptor it binds. Many neurotransmitters are synthesized from simple and plentiful precursors such as amino acids, which are readily available and often require a small number of biosynthetic steps for conversion. Neurotransmitters are essential to the function of complex neural systems. The exact number of unique neurotransmitters in humans is unknown, but more than 100 have been identified. Common neurotransmitters include glutamate, GABA, acetylcholine, glycine and norepinephrine. Mechanism and cycle Synthe ...
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Cardiac Stimulants
The heart is a muscular organ in most animals. This organ pumps blood through the blood vessels of the circulatory system. The pumped blood carries oxygen and nutrients to the body, while carrying metabolic waste such as carbon dioxide to the lungs. In humans, the heart is approximately the size of a closed fist and is located between the lungs, in the middle compartment of the chest. In humans, other mammals, and birds, the heart is divided into four chambers: upper left and right atria and lower left and right ventricles. Commonly the right atrium and ventricle are referred together as the right heart and their left counterparts as the left heart. Fish, in contrast, have two chambers, an atrium and a ventricle, while most reptiles have three chambers. In a healthy heart blood flows one way through the heart due to heart valves, which prevent backflow. The heart is enclosed in a protective sac, the pericardium, which also contains a small amount of fluid. The wall of th ...
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Alpha-adrenergic Agonists
The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers, beta-2 (β2) agonists and alpha-2 (α2) agonists, which are used to treat high blood pressure and asthma, for example. Many cells have these receptors, and the binding of a catecholamine to the receptor will generally stimulate the sympathetic nervous system (SNS). The SNS is responsible for the fight-or-flight response, which is triggered by experiences such as exercise or fear-causing situations. This response dilates pupils, increases heart rate, mobilizes energy, and diverts blood flow from non-essential organs to skeletal muscle. These effects together tend to increase physical performance momentarily. History By the turn of the 19th century, it was agreed that the stimulation of sympathetic nerves could cause different ...
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Ciclafrine
Ciclafrine (INN) is a sympathomimetic phenethylamine and antihypertensive that was never marketed. Synthesis Ciclafrine can be prepared by the reaction of norfenefrine with cycloheptanone Cycloheptanone, (CH2)6CO, is a cyclic ketone also referred to as suberone. It is a colourless volatile liquid. Cycloheptanone is used as a precursor for the synthesis of pharmaceuticals. Synthesis In 1836, French chemist Jean-Baptiste Boussinga .... : References Antihypertensive agents Phenylethanolamine ethers Oxazolidines Spiro compounds Abandoned drugs {{antihypertensive-stub ...
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Metaraminol
Metaraminol, previously sold under the brand name Aramine among others and also known as metaradrine, is a stereoisomer of ''meta''-hydroxynorephedrine (3,β-dihydroxyamphetamine), is a potent sympathomimetic amine used in the prevention and treatment of hypotension, particularly as a complication of anesthesia. It is an α1-adrenergic receptor agonist with some β effect. It is currently sold in its generic form by Slayback Pharma. Pharmacology and use as a vasopressor Metaraminol is given intravenously as either a bolus (often 0.5-1mg doses) or as an infusion, usually via peripheral intravenous access. Metaraminol is commonly available as 10mg in 1mL, that requires dilution prior to administration (often made up to a 0.5mg/mL solution), however pre-prepared syringes of metaraminol for bolus use for hypotension are also commonly available. Pharmacodynamics The dominant mechanism for the vasopressor action of metaraminol is indirect, with metaraminol displacing noradrena ...
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Phenylephrine
Phenylephrine is a medication primarily used as a decongestant, to dilate the pupil, to increase blood pressure, and to relieve hemorrhoids. In the United States, it was previously used orally as an over-the-counter decongestant to relieve nasal congestion due to sinusitis, but this use was discontinued in 2007. As of 2022, its use as a nasal decongestant in other applications still persists. Phenylephrine can be taken by mouth, as a nasal spray, given by injection into a vein or muscle, or applied to the skin. Common side effects when taken by mouth or injected include nausea, vomiting, headache, and anxiety. Use on hemorrhoids is generally well tolerated. Severe side effects may include a slow heart rate, intestinal ischemia, chest pain, kidney failure, and tissue death at the site of injection. It is unclear if use during pregnancy or breastfeeding is safe. Phenylephrine is a selective α1-adrenergic receptor agonist which results in the constriction of both arteries and ...
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Meta-Tyramine
''meta''-Tyramine, also known as ''m''-tyramine and 3-tyramine, is an endogenous trace amine neuromodulator and a structural analog of phenethylamine. It is a positional isomer of ''para''-tyramine, and similarly to it, has effects on the adrenergic and dopaminergic systems. ''meta''-Tyramine is produced in humans via aromatic amino acid decarboxylase-mediated metabolism of ''meta''-tyrosine. meta-Tyramine can be metabolized into dopamine via peripheral or brain CYP2D6 enzyme Enzymes () are proteins that act as biological catalysts by accelerating chemical reactions. The molecules upon which enzymes may act are called substrates, and the enzyme converts the substrates into different molecules known as products ...s in humans. See also * ''para''-Tyramine * 3-Methoxytyramine References Phenethylamines Phenols TAAR1 agonists Trace amines Norepinephrine-dopamine releasing agents {{nervous-system-drug-stub ...
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