Perathiepin
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Perathiepin
Perathiepin is a neuroleptic drug of the tricyclic family which was developed in the 1960s but was never marketed. In animal studies it was found to possess central depressant, antihistamine, antiserotonergic, and analgesic effects. See also * Clorotepine * Metitepine Metitepine (; developmental code names Ro 8-6837 (maleate), VUFB-6276 ( mesylate)), also known as methiothepin, is a drug described as a " psychotropic agent" of the tricyclic group which was never marketed. It acts as a non-selective antagonist ... References {{Tricyclics Antipsychotics Dibenzothiepines Diphenylethylpiperazines ...
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Metitepine
Metitepine (; developmental code names Ro 8-6837 (maleate), VUFB-6276 (mesylate)), also known as methiothepin, is a drug described as a "psychotropic agent" of the tricyclic compound, tricyclic group which was never marketed. It acts as a binding selectivity, non-selective receptor antagonist, antagonist of serotonin receptor, serotonin, dopamine receptor, dopamine, and adrenergic receptors and has antipsychotic properties. Synthesis The reduction of 2-(4-methylsulfanylphenyl)sulfanylbenzoic acidCID:2733664(1) gives [2-(4-methylsulfanylphenyl)sulfanylphenyl]methanolCID:12853582(2). Halogenating with thionyl chloride gives 1-(chloromethyl)-2-(4-methylsulfanylphenyl)sulfanylbenzeneCID:12853583(3). FGI with cyanide gives 2-[2-(4-methylsulfanylphenyl)sulfanylphenyl]acetonitrileCID:12853584(4). Alkali hydrolysis of the nitrile to 2-[2-(4-methylsulfanylphenyl)sulfanylphenyl]acetic acidCID:12383832(5). PPA cyclization to 3-methylsulfanyl-6H-benzo[b][1]benzothiepin-5-oneCID:827052(6). T ...
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Clorotepine
Clorotepine (; brand names Clotepin, Clopiben), also known as octoclothepin or octoclothepine, is an antipsychotic of the tricyclic group which was derived from perathiepin in 1965 and marketed in the Czech Republic by Spofa in or around 1971 for the treatment of schizophrenic psychosis. Clorotepine is known to have high affinity for the dopamine D1, D2, D3, and D4 receptors, the serotonin 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, and 5-HT7 receptors, the α1A-, α1B-, and α1D-adrenergic receptors, and the histamine H1 receptors, where it has been it has been confirmed to act as an antagonist (or inverse agonist) at most sites (and likely is as such at all of them based on structure–activity relationships), and it also blocks the reuptake of norepinephrine via inhibition of the norepinephrine transporter. Due to its very potent activity at the D2 receptor, along with tefludazine, clorotepine was used as the basis for developing a 3-dimensional (3D) pharmacophore fo ...
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Neuroleptic
Antipsychotics, also known as neuroleptics, are a class of psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder. Prior research has shown that use of any antipsychotic is associated with smaller brain tissue volumes, including white matter reduction and that this brain shrinkage is dose dependent and time dependent. A more recent controlled trial suggests that second generation antipsychotics combined with intensive psychosocial therapy may potentially prevent pallidal brain volume loss in first episode psychosis. The use of antipsychotics may result in many unwanted side effects such as involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. Long-term use can produce adverse effects such ...
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Drug
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insufflation (medicine), inhalation, drug injection, injection, smoking, ingestion, absorption (skin), absorption via a dermal patch, patch on the skin, suppository, or sublingual administration, dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to pharmacotherapy, treat, cure, preventive healthcare, prevent, or medical diagnosis, diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used ...
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Tricyclic
Tricyclics are chemical compounds that contain three interconnected rings of atoms. Many compounds have a tricyclic structure, but in pharmacology, the term has traditionally been reserved to describe heterocyclic drugs. Among these are antidepressants, antipsychotics, anticonvulsants, and antihistamines (as antiallergens, anti-motion sickness drugs, antipruritics, and hypnotics/sedatives) of the dibenzazepine, dibenzocycloheptene, dibenzothiazepine, dibenzothiepin, phenothiazine, and thioxanthene chemical classes, and others. History * Promethazine and other first generation antihistamines with a tricyclic structure were discovered in the 1940s. * Chlorpromazine, derived from promethazine originally as a sedative, was found to have neuroleptic properties in the early 1950s, and was the first typical antipsychotic. * Imipramine, originally investigated as an antipsychotic, was discovered in the early 1950s, and was the first tricyclic antidepressant. * Carbamazepine was disco ...
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Central Depressant
A depressant, or central depressant, is a drug that lowers neurotransmission levels, which is to depress or reduce arousal or stimulation, in various areas of the brain. Depressants are also colloquially referred to as downers as they lower the level of arousal when taken. Stimulants or "uppers" increase mental or physical function, hence the opposite drug class of depressants is stimulants, not antidepressants. Depressants are widely used throughout the world as prescription medicines and as illicit substances. Alcohol is a very prominent depressant. Alcohol can be and is more likely to be a large problem among teenagers and young adults. When depressants are used, effects often include ataxia, anxiolysis, pain relief, sedation or somnolence, and cognitive or memory impairment, as well as in some instances, euphoria, dissociation, muscle relaxation, lowered blood pressure or heart rate, respiratory depression, and anticonvulsant effects. Depressants also act to produce anesthesi ...
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Antihistamine
Antihistamines are drugs which treat allergic rhinitis, common cold, influenza, and other allergies. Typically, people take antihistamines as an inexpensive, generic (not patented) drug that can be bought without a prescription and provides relief from nasal congestion, sneezing A sneeze (also known as sternutation) is a semi-autonomous, convulsive expulsion of air from the lungs through the nose and mouth, usually caused by foreign particles irritating the nasal mucosa. A sneeze expels air forcibly from the mouth and ..., or hives caused by pollen, dust mites, or animal allergy with few side effects. Antihistamines are usually for short-term treatment. Chronic allergies increase the risk of health problems which antihistamines might not treat, including asthma, sinusitis, and lower respiratory tract infection. Consultation of a medical professional is recommended for those who intend to take antihistamines for longer-term use. Although people typically use the word "anti ...
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Antiserotonergic
A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action at serotonin (5-HT) receptors. Types 5-HT2A antagonists Antagonists of the 5-HT2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists). They include, but are not limited to: * Cyproheptadine blocks 5-HT2A, H1 and is a mild anticholinergic. * Methysergide is a 5-HT2A antagonist and nonselective 5-HT1 receptor blocker. It causes retroperitoneal fibrosis and mediastinal fibrosis. * Quetiapine blocks 5-HT2A, 5-HT1A, dopamine receptors D1 and D2, histamine receptor H1, and A1 adrenoreceptors. 5-HT2A/2C antagonists * Ketanserin Antihypertensive. Blocks 5-HT2A, 5-HT2C and Alpha 1 (A1) adrenoreceptors. * Risperidone antipsychotic * Trazodone 5-HT3 antagonists Another subclass consists of drugs selectively acting at the 5-HT3 receptors, and thus are known as 5-HT3 antagonists. They are efficacious i ...
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Analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing ...
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Pharmacodynamics
Pharmacodynamics (PD) is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms (for example, infection). Pharmacodynamics and pharmacokinetics are the main branches of pharmacology, being itself a topic of biology interested in the study of the interactions between both endogenous and exogenous chemical substances with living organisms. In particular, pharmacodynamics is the study of how a drug affects an organism, whereas pharmacokinetics is the study of how the organism affects the drug. Both together influence dosing, benefit, and adverse effects. Pharmacodynamics is sometimes abbreviated as PD and pharmacokinetics as PK, especially in combined reference (for example, when speaking of PK/PD models). Pharmacodynamics places particular emphasis on dose–response relationships, that is, the relationships between d ...
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Antipsychotics
Antipsychotics, also known as neuroleptics, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder. Prior research has shown that use of any antipsychotic is associated with smaller brain tissue volumes, including white matter reduction and that this brain shrinkage is dose dependent and time dependent. A more recent controlled trial suggests that second generation antipsychotics combined with intensive psychosocial therapy may potentially prevent pallidal brain volume loss in first episode psychosis. The use of antipsychotics may result in many unwanted side effects such as Extrapyramidal symptoms, involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. ...
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