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Alpha-2 Blocker
Alpha-2 blockers (or α2 blockers) are a subset of the alpha blocker class of drugs and are antagonists to the α2 adrenergic receptor. They are mainly used in research, having found limited clinical application in human medicine. Alpha-2 blockers increase noradrenaline release. Uses Yohimbine, historically used as an aphrodisiac, is sometimes used in veterinary medicine (although now largely replaced by atipamezole) for reversing the effects of α2s such as medetomidine that are used as sedatives during surgery. The tetracyclic antidepressants mianserin and mirtazapine are α2 blockers, although their efficacy as antidepressants may come from their activity at other receptor sites. Mechanistically, α2 blockers increase adrenergic, dopaminergic and serotonergic neurotransmitters and induce insulin secretion, decreasing blood sugar levels. Withdrawal from α2 blockers can be difficult or dangerous as the global downregulation of neurotransmitters may cause symptoms of d ...
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Alpha Blocker
Alpha (uppercase , lowercase ; grc, ἄλφα, ''álpha'', or ell, άλφα, álfa) is the first letter of the Greek alphabet. In the system of Greek numerals, it has a value of one. Alpha is derived from the Phoenician letter aleph , which is the West Semitic word for " ox". Letters that arose from alpha include the Latin letter A and the Cyrillic letter А. Uses Greek In Ancient Greek, alpha was pronounced and could be either phonemically long ( ː or short ( . Where there is ambiguity, long and short alpha are sometimes written with a macron and breve today: Ᾱᾱ, Ᾰᾰ. * ὥρα = ὥρᾱ ''hōrā'' "a time" * γλῶσσα = γλῶσσᾰ ''glôssa'' "tongue" In Modern Greek, vowel length has been lost, and all instances of alpha simply represent the open front unrounded vowel . In the polytonic orthography of Greek, alpha, like other vowel letters, can occur with several diacritic marks: any of three accent symbols (), and either of two breathing ma ...
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Adrenergic
Adrenergic means "working on adrenaline (epinephrine) or noradrenaline (norepinephrine)" (or on their receptors). When not further qualified, it is usually used in the sense of enhancing or mimicking the effects of epinephrine and norepinephrine in the body. * Adrenergic nervous system, a part of the autonomic nervous system that uses epinephrine or norepinephrine as its neurotransmitter Regarding proteins: * Adrenergic receptor, a receptor type for epinephrine and norepinephrine; subtypes include α1, α2, β1, β2, and β3 receptors * Adrenergic transporter (norepinephrine transporter), a protein transporting norepinephrine from the synaptic cleft into nerve cells Regarding pharmaceutical drugs: * Adrenergic receptor agonist, a type of drug activating one or more subtypes of adrenergic receptors ** This includes drugs regulating blood pressure and antiasthmatic drugs. * Adrenergic receptor antagonist, a type of drug blocking one or more subtypes of adrenergic receptors ** ...
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Rauwolscine
Rauwolscine, also known as isoyohimbine, α-yohimbine, and corynanthidine, is an alkaloid found in various species within the genera ''Rauvolfia'' and ''Corynanthe'' (including ''Pausinystalia''). It is a stereoisomer of yohimbine. Rauwolscine is a central nervous system stimulant, a local anesthetic and a vague aphrodisiac. Rauwolscine acts predominantly as a α2-adrenergic receptor antagonist. It has also been shown to function as a 5-HT1A receptor partial agonist and 5-HT2A and 5-HT2B receptor antagonist. See also * Ajmalicine * Corynanthine * Spegatrine * Yohimbine Yohimbine (), also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe''; also from the bark of the unrelated South American tree ''Aspidosperma quebracho-blanco''. Yohimbine is an α2 ... References {{Serotonergics Indoloquinolizines Tryptamine alkaloids Quinolizidine alkaloids Alkaloids found in Rauvolfia Alpha-2 blockers 5-HT1A ag ...
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Yohimbine
Yohimbine (), also known as quebrachine, is an indole alkaloid derived from the bark of the African tree '' Pausinystalia johimbe''; also from the bark of the unrelated South American tree ''Aspidosperma quebracho-blanco''. Yohimbine is an α2-adrenergic receptor antagonist, and has been used in a variety of research projects. It is a veterinary drug used to reverse sedation in dogs and deer. While yohimbine behaves as an aphrodisiac in some mammals, it does not do so in humans. It has been prescribed as a treatment for erectile dysfunction, although its reported clinical benefits were modest and it has largely been superseded by the PDE5 inhibitor class of drugs. Substances that have purported to be extracts from the yohimbe tree have been marketed as dietary supplements for various purposes, but they contain highly variable amounts of yohimbine, if any; no published scientific evidence supports their efficacy. Uses Yohimbine is a drug used in veterinary medicine to reverse t ...
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Idazoxan
Idazoxan ( INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor. Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia. Alzheimer's research Mice treated with idazoxan, which blocks the α2A receptor which regulates norepinephrine, behaved similarly to control animals despite still having amyloid-beta plaques in the brain, as a proof-of-concept experiment that dramatically reduced Alzheimer's pathology and symptoms in two mouse models, potentially offering an immediate treat ...
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Efaroxan
Efaroxan is an α2-adrenergic receptor antagonist and antagonist of the imidazoline receptor. Synthesis The Darzens reaction between 2-fluorobenzaldehyde 7848-46-1(1) and Ethyl 2-bromobutyrate 33-68-6(2) gives ethyl 2-ethyl-3-(2-fluorophenyl)oxirane-2-carboxylateCID:100942311(3). A catalytic hydrogenation over Pd/C would give ethyl 2- 2-fluorophenyl)methyl2-hydroxybutanoateCID:77591056(4). Saponification of the ester then gives 2- 2-Fluorophenyl)methyl2-hydroxybutanoic acidCID:53869347(5). Treatment with 2 molar equivalents of sodium hydride apparently gives 2-Ethyl-2,3-dihydrobenzofuran-2-carboxylic acid 11080-50-3(6). Treatment of the carboxylic acid with thionyl chloride then gives the acid chloride and subsequent treatment of this with ethylenediamine in the presence of trimethylaluminium completed the synthesis of ' (8). See also * Fluparoxan * Idazoxan Idazoxan ( INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic recepto ...
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Microcirculation
The microcirculation is the circulation of the blood in the smallest blood vessels, the microvessels of the microvasculature present within organ tissues. The microvessels include terminal arterioles, metarterioles, capillaries, and venules. Arterioles carry oxygenated blood to the capillaries, and blood flows out of the capillaries through venules into veins. In addition to these blood vessels, the microcirculation also includes lymphatic capillaries and collecting ducts. The main functions of the microcirculation are the delivery of oxygen and nutrients and the removal of carbon dioxide (CO2). It also serves to regulate blood flow and tissue perfusion thereby affecting blood pressure and responses to inflammation which can include edema (swelling). Most vessels of the microcirculation are lined by flattened cells of the endothelium and many of them are surrounded by contractile cells called pericytes. The endothelium provides a smooth surface for the flow of blood and regu ...
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Insulin
Insulin (, from Latin ''insula'', 'island') is a peptide hormone produced by beta cells of the pancreatic islets encoded in humans by the ''INS'' gene. It is considered to be the main anabolic hormone of the body. It regulates the metabolism of carbohydrates, fats and protein by promoting the absorption of glucose from the blood into liver, fat and skeletal muscle cells. In these tissues the absorbed glucose is converted into either glycogen via glycogenesis or fats (triglycerides) via lipogenesis, or, in the case of the liver, into both. Glucose production and secretion by the liver is strongly inhibited by high concentrations of insulin in the blood. Circulating insulin also affects the synthesis of proteins in a wide variety of tissues. It is therefore an anabolic hormone, promoting the conversion of small molecules in the blood into large molecules inside the cells. Low insulin levels in the blood have the opposite effect by promoting widespread catabolism, especial ...
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Serotonergic
Serotonergic () or serotoninergic () means "pertaining to or affecting serotonin". Serotonin is a neurotransmitter. A synapse is serotonergic if it uses serotonin as its neurotransmitter. A serotonergic neuron ''produces'' serotonin. A substance is serotonergic if it produces its effects via interactions with the serotonin system, such as by stimulating or blocking neurotransmission. A serotonergic or serotoninergic agent is any chemical that modifies the effects of serotonin in the body. Some different types of serotonergics drugs include the following: * Serotonin receptor agonists and antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, ri ...s * Serotonin reuptake inhibitors * Serotonin releasing agents See also References Parasympathetic nervous system Neurochemi ...
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Dopaminergic
Dopaminergic means "related to dopamine" (literally, "working on dopamine"), dopamine being a common neurotransmitter. Dopaminergic substances or actions increase dopamine-related activity in the brain. Dopaminergic brain pathways facilitate dopamine-related activity. For example, certain proteins such as the dopamine transporter (DAT), vesicular monoamine transporter 2 (VMAT2), and dopamine receptors can be classified as dopaminergic, and neurons that synthesize or contain dopamine and synapses with dopamine receptors in them may also be labeled as ''dopaminergic''. Enzymes that regulate the biosynthesis or metabolism of dopamine such as aromatic L-amino acid decarboxylase or DOPA decarboxylase, monoamine oxidase (MAO), and catechol ''O''-methyl transferase (COMT) may be referred to as ''dopaminergic'' as well. Also, any endogenous or exogenous chemical substance that acts to affect dopamine receptors or dopamine release through indirect actions (for example, on neurons ...
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Mirtazapine
Mirtazapine, sold under the brand name Remeron amongst others, is an Atypical antidepressant, atypical antidepressant, and as such is used primarily to treat Depression (mood), depression. Its effects may take up to four weeks, but can also manifest as early as one to two weeks. It is often used in cases of depression complicated by anxiety or insomnia. The effectiveness of mirtazapine is comparable to other commonly prescribed antidepressants. It is taken oral administration, by mouth. Common side effects include somnolence, sleepiness, vertigo, dizziness, hyperphagia, increased appetite and weight gain. Serious side effects may include mania, neutropenia, low white blood cell count, and increased suicide among children. Drug withdrawal, Withdrawal symptoms may occur with stopping. It is not recommended together with a monoamine oxidase inhibitor, although evidence supporting the danger of this combination has been refuted. It is unclear if use during pregnancy is safe. How i ...
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Receptor Antagonist
A receptor antagonist is a type of receptor ligand or drug that blocks or dampens a biological response by binding to and blocking a receptor rather than activating it like an agonist. Antagonist drugs interfere in the natural operation of receptor proteins.Pharmacology Guide: In vitro pharmacology: concentration-response curves
" '' GlaxoWellcome.'' Retrieved on December 6, 2007.
They are sometimes called blockers; examples include alpha blockers, beta blocker
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