Etilefrine Pivalate
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Etilefrine Pivalate
Etilefrine pivalate ; developmental code name K-30052) is a sympathomimetic agent which was never marketed. It is the 3- pivalate ester of etilefrine (ethylnorphenylephrine) and has much greater lipophilicity than etilefrine. Some related compounds include pivenfrine (phenylephrine pivalate) and dipivefrine Dipivefrine, or dipivefrin, also known as epinephrine pivalate and sold under the brand name Propine among others, is a sympathomimetic medication which is used in the treatment of open-angle glaucoma.Dipivefrin . It is available as a 0.1% o ... (epinephrine dipivalate), which were developed as mydriatic agents. References Alpha-1 adrenergic receptor agonists Alpha-2 adrenergic receptor agonists Beta-adrenergic agonists Phenylethanolamines Sympathomimetics {{Cardiovascular-drug-stub ...
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Pivalate
Pivalic acid is a carboxylic acid with a molecular formula of (CH3)3CCO2H. This colourless, odoriferous organic compound is solid at room temperature. Two abbreviations for pivalic acid are ''t''-BuC(O)OH and PivOH. The pivalyl or pivaloyl group is abbreviated ''t''-BuC(O). Pivalic acid is an isomer of valeric acid, the other two isomers of it are 2-methylbutanoic acid and 3-methylbutanoic acid. Preparation Pivalic acid is prepared on a commercial scale by hydrocarboxylation of isobutene via the Koch reaction: :(CH3)2C=CH2 + CO + H2O → (CH3)3CCO2H Such reactions require an acid catalyst such as hydrogen fluoride. ''tert''-Butyl alcohol and isobutyl alcohol can also be used in place of isobutene. Globally, several million kilograms are produced annually. Pivalic acid is also economically recovered as a byproduct from the production of semisynthetic penicillins like ampicillin and amoxycillin. It was originally prepared by the oxidation of pinacolone with chromic acid: : A ...
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Ester
In chemistry, an ester is a compound derived from an acid (either organic or inorganic) in which the hydrogen atom (H) of at least one acidic hydroxyl group () of that acid is replaced by an organyl group (R). These compounds contain a distinctive functional group. Analogues derived from oxygen replaced by other chalcogens belong to the ester category as well. According to some authors, organyl derivatives of acidic hydrogen of other acids are esters as well (e.g. amides), but not according to the IUPAC. Glycerides are fatty acid esters of glycerol; they are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils. Lactones are cyclic carboxylic esters; naturally occurring lactones are mainly 5- and 6-membered ring lactones. Lactones contribute to the aroma of fruits, butter, cheese, vegetables like celery and other foods. Esters can be formed from oxoacids (e.g. esters of acetic acid, carbonic acid ...
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Etilefrine
Etilefrine, sold under the brand name Effortil among others, is a sympathomimetic medication used as an antihypotensive agent to treat orthostatic hypotension. It is usually used oral administration, by mouth, but is also available as an injection (medicine), injectable. Side effects of etilefrine include nausea, tremors, and palpitations, among others. Etilefrine is an agonist of the alpha-adrenergic receptor, α- and β-adrenergic receptors. It is a substituted phenethylamine and is related to epinephrine (medication), epinephrine, phenylephrine, and norfenefrine. Etilefrine was first described and introduced for medical use by 1949. Medical uses Etilefrine is used to treat orthostatic hypotension and as a nasal decongestant. It has also been used off-label use, off-label to treat priapism. Side effects Side effects of etilefrine include nausea, tremors, and palpitations, among others. Pharmacology Pharmacodynamics Etilefrine is an agonist of the alpha-1 adrenergic recept ...
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Lipophilicity
Lipophilicity (from Greek λίπος "fat" and φίλος "friendly") is the ability of a chemical compound to dissolve in fats, oils, lipids, and non-polar solvents such as hexane or toluene. Such compounds are called lipophilic (translated as "fat-loving" or "fat-liking"). Such non-polar solvents are themselves lipophilic, and the adage "like dissolves like" generally holds true. Thus lipophilic substances tend to dissolve in other lipophilic substances, whereas hydrophilic ("water-loving") substances tend to dissolve in water and other hydrophilic substances. Lipophilicity, hydrophobicity, and non-polarity may describe the same tendency towards participation in the London dispersion force, as the terms are often used interchangeably. However, the terms "lipophilic" and "hydrophobic" are not synonymous, as can be seen with silicones and fluorocarbons, which are hydrophobic but not lipophilic. __TOC__ Surfactants Hydrocarbon-based surfactants are compounds that are amph ...
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Chemical Compound
A chemical compound is a chemical substance composed of many identical molecules (or molecular entities) containing atoms from more than one chemical element held together by chemical bonds. A molecule consisting of atoms of only one element is therefore not a compound. A compound can be transformed into a different substance by a chemical reaction, which may involve interactions with other substances. In this process, bonds between atoms may be broken or new bonds formed or both. There are four major types of compounds, distinguished by how the constituent atoms are bonded together. Molecular compounds are held together by covalent bonds; ionic compounds are held together by ionic bonds; intermetallic compounds are held together by metallic bonds; coordination complexes are held together by coordinate covalent bonds. Non-stoichiometric compounds form a disputed marginal case. A chemical formula specifies the number of atoms of each element in a compound molecule, usin ...
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Pivenfrine
Pivenfrine (), also known as pivalylphenylephrine or phenylephrine pivalate, is a sympathomimetic and mydriatic agent which was never marketed. It is the 3- pivalyl ester of phenylephrine. Pivenfrine has much greater lipophilicity than phenylephrine. Higher lipophilicity is known to greatly improve corneal permeability, as in dipivefrine (epinephrine dipivalate). Another related compound Compound may refer to: Architecture and built environments * Compound (enclosure), a cluster of buildings having a shared purpose, usually inside a fence or wall ** Compound (fortification), a version of the above fortified with defensive struc ... is etilefrine pivalate (ethylnorphenylephrine pivalate). References Abandoned drugs Alpha-1 adrenergic receptor agonists Ophthalmology drugs Phenylethanolamines Pivalate esters Prodrugs Sympathomimetics {{Cardiovascular-drug-stub ...
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Dipivefrine
Dipivefrine, or dipivefrin, also known as epinephrine pivalate and sold under the brand name Propine among others, is a sympathomimetic medication which is used in the treatment of open-angle glaucoma.Dipivefrin . It is available as a 0.1% ophthalmic solution (eye drop). Side effects of dipivefrine include local eye reactions among others. Dipivefrine is a prodrug of epinephrine (adrenaline) and hence acts as a non-selective adrenergic receptor agonist. It is a substituted phenethylamine and catecholamine and is an ester of epinephrine with much greater fat solubility. Dipivefrine was first described by 1975. It is widely marketed throughout the world. However, it is no longer available in the United States. Medical uses Dipivefrine is used in the treatment of open-angle glaucoma. Contraindications Use in narrow-angle glaucoma may be dangerous because it could make the eye susceptible to an attack of angle closure, causing an increase in pressure and pain and possibly ...
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Mydriatic Agent
Mydriasis is the dilation of the pupil, usually having a non-physiological cause, or sometimes a physiological pupillary response. Non-physiological causes of mydriasis include disease, trauma, or the use of certain types of drugs. It may also be of unknown cause. Normally, as part of the pupillary light reflex, the pupil dilates in the dark and constricts in the light to respectively improve vividity at night and to protect the retina from sunlight damage during the day. A ''mydriatic'' pupil will remain excessively large even in a bright environment. The excitation of the radial fibres of the iris which increases the pupillary aperture is referred to as a mydriasis. More generally, mydriasis also refers to the natural dilation of pupils, for instance in low light conditions or under sympathetic stimulation. Mydriasis is frequently induced by drugs for certain ophthalmic examinations and procedures, particularly those requiring visual access to the retina. Fixed, unilateral m ...
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Alpha-1 Adrenergic Receptor Agonists
Alpha 1 or Alpha-1 may refer to: *Alpha-1 adrenergic receptor, a G protein-coupled receptor *Alpha-1 antitrypsin, a protein **Alpha-1 antitrypsin deficiency, a genetic disorder *Alpha-1-fetoprotein or Alpha-fetoprotein, a protein *Alpha-One, a fictional spacecraft in ''Buzz Lightyear of Star Command: The Adventure Begins'' *Alpha 1 (Robert Silverberg anthology), ''Alpha 1'' (Robert Silverberg anthology), a 1970 book *Alpha-1 Wrestling, a professional wrestling promotion See also

* * *A1 (other) *Alpha (other) *AMY1A or Alpha-1A or, an enzyme found in humans and other mammals *List of A1 genes, proteins or receptors {{disambiguation ...
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Alpha-2 Adrenergic Receptor Agonists
Alpha-adrenergic agonists are a class of sympathomimetic agents that selectively stimulates alpha adrenergic receptors. The alpha-adrenergic receptor has two subclasses α1 and α2. Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity. The activation of α1 stimulates the membrane bound enzyme phospholipase C, and activation of α2 inhibits the enzyme adenylate cyclase. Inactivation of adenylate cyclase in turn leads to the inactivation of the secondary messenger cyclic adenosine monophosphate and induces smooth muscle and blood vessel constriction. Classes Although complete selectivity between receptor agonism is rarely achieved, some agents have partial selectivity. NB: the inclusion of a drug in each cat ...
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Beta-adrenergic Agonists
Beta adrenergic agonists or beta agonists are medications that relax muscles of the airways, causing widening of the airways and resulting in easier breathing. They are a class of sympathomimetic agents, each acting upon the Adrenergic receptor#β receptors, beta adrenoceptors. In general, pure beta-adrenergic agonists have the opposite function of beta blockers: beta-adrenoreceptor agonist ligands mimic the actions of both epinephrine- and norepinephrine- signaling, in the heart and lungs, and in smooth muscle tissue; epinephrine expresses the higher affinity. The activation of β1, β2 and β3 activates the enzyme, Adenylyl cyclase, adenylate cyclase. This, in turn, leads to the activation of the secondary messenger cyclic adenosine monophosphate (cAMP); cAMP then activates protein kinase A (PKA) which phosphorylates target proteins, ultimately inducing smooth muscle relaxation and contraction of the cardiac tissue. Function Activation of β1 receptors induces positive inot ...
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