Pyridinylpiperazine
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Pyridinylpiperazine
1-(2-Pyridinyl)piperazine is a chemical compound and piperazine derivative. Some derivatives of this substance are known to act as potent and selective α2-adrenergic receptor antagonists, such as 1-(3-fluoro-2-pyridinyl)piperazine. A few pyridinylpiperazine derivatives are drugs, including: * ABT-724 AR234960* Azaperol 804-05-9* Azaperone — antipsychotic * Atevirdine — antiretroviral BRN 0563047 9215-20-2"''Stimulating dopaminerginic activity''": Journal Ref (Cmp XVIII): * CP-226,269 * Delavirdine — antiretroviral * Mirtazapine — antidepressant MLS1547 15698-36-3Revenast 5673-87-6UMB38ref> XH-148 See also * Diphenylmethylpiperazine * Benzylpiperazine * Phenylpiperazine 1-Phenylpiperazine is a simple chemical compound featuring a phenyl group bound to a piperazine ring. The suffix ‘-piprazole’ is sometimes used in the names of drugs to indicate they belong to this class. List phenylpiperazine derivativesAlpe ... * Pyrimidinylpiperazine References P ...
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Azaperone
Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine. It is uncommonly used in humans as an antipsychotic drug. Azaperone acts primarily as a dopamine antagonist (pharmacology), antagonist but also has some histamine, antihistaminic and choline, anticholinergic properties as seen with similar drugs such as haloperidol. Azaperone may cause hypotension and while it has minimal effects on respiration in pigs, high doses in humans can cause respiratory depression. Veterinary use The most common use for azaperone is in relatively small doses as a "serenic" (to reduce aggression) in farmed pigs, either to stop them fighting or to encourage sows to accept piglets. Higher doses are used for anesthesia in combination with other drugs such as xylazine, tiletamine and zolazepam. Azaperone is also used in combination with strong narcotics such as etorphine or carfentanil ...
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Piperazine
Piperazine () is an organic compound that consists of a six-membered ring containing two nitrogen atoms at opposite positions in the ring. Piperazine exists as small alkaline deliquescent crystals with a saline taste. The piperazines are a broad class of chemical compounds, many with important pharmacological properties, which contain a core piperazine functional group. Origin and naming Piperazines were originally named because of their chemical similarity with piperidine, part of the structure of piperine in the black pepper plant (''Piper nigrum''). The -az- infix added to "piperazine" refers to the extra nitrogen atom, compared to piperidine. It is important to note, however, that piperazines are ''not'' derived from plants in the '' Piper'' genus. Chemistry Piperazine is freely soluble in water and ethylene glycol, but insoluble in diethyl ether. It is a weak base with two pKb of 5.35 and 9.73 at 25 °C.; the pH of a 10% aqueous solution of piperazine is 10.8–11.8. Pi ...
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Pyrimidinylpiperazine
1-(2-Pyrimidinyl)piperazine (1-PP, 1-PmP) is a chemical compound and piperazine derivative. It is known to act as an antagonist of the α2-adrenergic receptor (Ki = 7.3–40 nM) and, to a much lesser extent, as a partial agonist of the 5-HT1A receptor (Ki = 414 nM; Emax = 54%). It has negligible affinity for the dopamine D2, D3, and D4 receptors (Ki > 10,000 nM) and does not appear to have significant affinity for the α1-adrenergic receptors. Its crystal structure has been determined. Derivatives A number of pyrimidinylpiperazine derivatives are drugs, including: * Buspirone - anxiolytic * Dasatinib - anticancer agent * Eptapirone - anxiolytic * Gepirone - anxiolytic * Ipsapirone - anxiolytic * Piribedil - antiparkinsonian agent * Revospirone - anxiolytic * Tandospirone - anxiolytic * Tirilazad - neuroprotective agent * Umespirone - anxiolytic * Zalospirone - anxiolytic The anxiolytics are also classified as azapirones due to the azaspirodecanedione moie ...
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Phenylpiperazine
1-Phenylpiperazine is a simple chemical compound featuring a phenyl group bound to a piperazine ring. The suffix ‘-piprazole’ is sometimes used in the names of drugs to indicate they belong to this class. List phenylpiperazine derivativesAlpertine 7076-46-6br>BP 554 2900-57-0br>Butropipazone 354-61-2br>CAM89alluded to here: Centphenaquin 8459-16-6br>Centpropazine 1315-34-3 4675-77-9br>Clodoxopone 1923-34-7br>Dropropizine 7692-31-8br>FAUC-299 13972-96-2br>FAUC-312 62104-72-7br>LASSBio-579 91774-47-9br>LASSBio-581 91774-48-0br>LASSBio-632LASSBio-680LASSBio-724LASSBio-729

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Benzylpiperazine
Benzylpiperazine (BZP) is a recreational drug with euphoriant and stimulant properties. The effects produced by BZP are comparable to those produced by amphetamine. Adverse effects have been reported following its use including acute psychosis, renal toxicity and seizures. Deaths from piperazine derivatives are extremely rare, but there has been at least one death apparently due to BZP alone. Its sale is banned in several countries, including Australia, Canada, New Zealand, the United States, the Republic of Ireland, the United Kingdom, Bulgaria, Romania and other parts of Europe. History Development history BZP was first synthesized by Burroughs Wellcome & Company in 1944. It is often claimed that it was originally synthesized as a potential antihelminthic (anti-parasitic) agent for use in farm animals, but its synthesis is thought to pre-date their interest in piperazines as anthelmintics. Even so, the majority of the early work with the piperazines were investigations i ...
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Diphenylmethylpiperazine
1-(Diphenylmethyl)piperazine, also known as benzhydrylpiperazine, is a chemical compound and piperazine derivative. It features a piperazine ring with a benzhydryl (diphenyl methyl) group bound to one of the nitrogen Nitrogen is the chemical element with the symbol N and atomic number 7. Nitrogen is a nonmetal and the lightest member of group 15 of the periodic table, often called the pnictogens. It is a common element in the universe, estimated at se ...s.Kaczor A, Matosiuk D. Non-peptide opioid receptor ligands - recent advances. Part I - agonists. Curr Med Chem. 2002 Sep;9(17):1567-89. Review. References Piperazines Diphenylmethylpiperazines Benzhydryl compounds {{organic-compound-stub ...
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Mirtazapine
Mirtazapine, sold under the brand name Remeron amongst others, is an atypical antidepressant, and as such is used primarily to treat 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 by mouth. Common side effects include sleepiness, dizziness, increased appetite and weight gain. Serious side effects may include mania, low white blood cell count, and increased suicide among children. 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 it works is not clear, but it may involve blocking certain adrenergic and serotonin receptors. Chemically, it is a tetracyclic ...
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Delavirdine
Delavirdine (DLV) (brand name Rescriptor) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) marketed by ViiV Healthcare. It is used as part of highly active antiretroviral therapy (HAART) for the treatment of human immunodeficiency virus (HIV) type 1. It is presented as the mesylate. The recommended dosage is 400 mg, three times a day. Although delavirdine was approved by the U.S. Food and Drug Administration in 1997, its efficacy is lower than other NNRTIs, especially efavirenz, and it also has an inconvenient schedule. These factors have led the U.S. DHHS not to recommend its use as part of initial therapy.DHHS panel. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents (May 4, 2006). (Available for download froAIDSInfo) The risk of cross-resistance across the NNRTI class, as well as its complex set of drug interactions, make the place of delavirdine in second-line and salvage therapy unclear, and it is currently rarely used. ...
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CP-226,269
CP-226,269 is a drug which acts as a dopamine agonist selective for the D4 subtype, which is used for researching the role of D4 receptors in the brain. Synthesis The piperazine used has dual use in the synthesis of ABT-724, ABT-670, Azaperone, MLS 1547 15698-36-3 Revenast 5673-87-6 UMB38 & XH-148. Weinreb ketone synthesis between 5-Fluoroindole-2-Carboxylic acid 99-76-8(1) and N,O-Dimethylhydroxylamine Fb: 117-97-1Hcl: 638-79-5(2) gives the Weinreb–Nahm amide, 5-Fluoro-N-Methoxy-N-Methyl-Indole-2-CarboxamideCID:23003585(3). This intermediate is further reduced giving 5-Fluoro-Indole-2-Carbaldehyde 20943-23-7(4). Reductive amination Reductive amination (also known as reductive alkylation) is a form of amination that involves the conversion of a carbonyl group to an amine via an intermediate imine. The carbonyl group is most commonly a ketone or an aldehyde. It is considered ... with 1-(2-Pyridyl)Piperazine 4803-66-2(5) completed the synthesis CP-226,269 (6). ...
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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 and/or new bonds formed. 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, using the s ...
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Atevirdine
Ateviridine is a non-nucleoside reverse transcriptase inhibitor that has been studied for the treatment of HIV. Synthesis Preparation of the pyridylpiperazine moiety starts by aromatic displacement of chlorine from 2-chloro-3-nitropyridine by piperazine to give 3. The secondary amine is then protected as its BOC derivative by reaction with di-tert-butyl dicarbonate (Boc anhydride) to give 4. The nitro group is then reduced by catalytic hydrogenation. Reductive alkylation with acetaldehyde in the presence of lithium cyanoborohydride gives the corresponding N-ethyl derivative. The protecting group is then removed by reaction with TFA. Reaction of the resulting amine with the imidazolide derivative of 5-methoxy-3-indoleacetic acid produces the amide reverse transcriptase inhibitor, atevirdine. See also *Delavirdine Delavirdine (DLV) (brand name Rescriptor) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) marketed by ViiV Healthcare. It is used as part of highly act ...
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ABT-724
ABT-724 is a drug which acts as a dopamine agonist, and is selective for the D4 subtype. It was developed as a possible drug for the treatment of erectile dysfunction, although poor oral bioavailability means alternative drugs such as ABT-670 may be more likely to be developed commercially. Nonetheless, it continues to be used in scientific research into the function of the D4 receptor. See also * ABT-670 * Bremelanotide * Cabergoline * Flibanserin * Intrinsa * Melanotan II * Pramipexole * PF-219,061 * Tibolone Tibolone, sold under the brand name Livial among others, is a medication which is used in menopausal hormone therapy and in the treatment of postmenopausal osteoporosis and endometriosis. The medication is available alone and is not formulated ... * UK-414,495 References Dopamine agonists Piperazines 2-Pyridyl compounds Benzimidazoles {{genito-urinary-drug-stub ...
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