|
α2A-adrenergic
The alpha-2A adrenergic receptor (α2A adrenoceptor), also known as ADRA2A, is an α2-adrenergic receptor, and also denotes the human gene encoding it. Receptor α2-adrenergic receptors include 3 highly homologous subtypes: α2A, α2B, and α2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. Studies in mice revealed that both the α2A and α2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the α2A subtype inhibited transmitter release at high stimulation frequencies, whereas the α2C subtype modulated neurotransmission at lower levels of nerve activity. Gene This gene encodes α2A subtype and it contains no introns in either its coding or untranslated sequences. Ligands Agonists * 4-NEMD * Brimonidine * Clonidine * Detomidine * Dexmedetomidine * Guanfac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-2 Adrenergic Receptor
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi alpha subunit, Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-adrenergic, α2A-, α2B-adrenergic, α2B-, and α2C-adrenergic, α2C-adrenergic. Some species other than humans express a fourth α2D-adrenergic receptor as well. Catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) signal through the α2-adrenergic receptor in the central nervous system, central and peripheral nervous systems. Cellular localization The Alpha-2A adrenergic receptor, α2A adrenergic receptor is localised in the following central nervous system (CNS) structures: * Brainstem (especially the locus coeruleus as presynaptic & somatodendritic autoreceptor ) * Midbrain * Hypothalamus * Olfactory system * Hippocampus * Spinal cord * Cerebral cortex * Cerebellum * Septum Whereas the Alpha-2B adrenergic receptor, α2B adren ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lurasidone
Lurasidone, sold under the brand name Latuda among others, is an atypical antipsychotic medication used to treat schizophrenia and bipolar depression. It is taken by mouth. Common side effects include sedation, indigestion, nausea, and insomnia. At higher dosages, there is an increased risk for restlessness and movement problems. Serious side effects are valid for all atypical antipsychotics and may include the potentially permanent movement disorder tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, angioedema, and high blood sugar levels. Although lurasidone is less likely to cause high blood sugar levels in most patients, hyperosmolar hyperglycemic syndrome may occur. In older people with psychosis as a result of dementia, it may increase the risk of dying. Use during pregnancy is of unclear safety. Lurasidone was first approved for medical use in the United States in 2010. In 2013, it was approved in Canada and by the U.S. Fo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Myrcene
Myrcene, or β-myrcene, is a terpene, monoterpene. A colorless oil, it occurs widely in essential oils. It is produced mainly semi-synthetically from ''Myrcia'', from which it gets its name. It is an intermediate in the production of several fragrances. A less-common isomeric form, having one of the three alkene units in a different position, is α-myrcene. Production Myrcene is often produced commercially by the pyrolysis (400 °C) of β-pinene, which is obtained from turpentine. It is rarely obtained directly from plants. Plants biosynthesize myrcene via geranyl pyrophosphate (GPP), which isomerizes into linalool, linalyl pyrophosphate. An elimination reaction, releasing the pyrophosphate (OPP) and a proton, completes the conversion. Occurrence It could in principle be extracted from any number of plants, such as verbena or wild thyme, the leaves of which contain up to 40% by weight of myrcene. Many other plants contain myrcene, sometimes in substantial amounts. Some of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clozapine
Clozapine, sold under the brand name Clozaril among others, is a psychiatric medication and was the first atypical antipsychotic to be discovered. It is used primarily to treat people with schizophrenia and schizoaffective disorder who have had an inadequate response to two other antipsychotics, or who have been unable to tolerate other drugs due to extrapyramidal side effects. In the US, clozapine is also approved for use in people with recurrent suicidal behavior in people with schizophrenia or schizoaffective disorder. It is also used for the treatment of psychosis in Parkinson's disease. Clozapine is recommended by multiple international treatment guidelines, after resistance to two other antipsychotic medications, and is the only treatment likely to result in improvement if two (or one) other antipsychotic has not had a satisfactory effect. Long term follow-up studies from Finland show significant improvements in terms of overall mortality including from suicide and all ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
BRL-44408
BRL-44408 is a drug used in scientific research which acts as a selective antagonist for the α2A-adrenergic receptor. It has been suggested as having potential therapeutic application in the treatment of extrapyramidal side effects produced by some antipsychotic Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), p ... medications. References External links * Alpha-2 blockers Isoindolines Imidazolines {{antihypertensive-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Asenapine
Asenapine, sold under the brand name Saphris among others, is an atypical antipsychotic medication used to treat schizophrenia and acute mania associated with bipolar disorder as well as the medium to long-term management of bipolar disorder. It was chemically derived via altering the chemical structure of the tetracyclic (''atypical'') antidepressant, mianserin. It was initially approved in the United States in 2009 and approved as a generic medication in 2020. Medical uses Asenapine has been approved by the FDA for the acute treatment of adults with schizophrenia and acute treatment of manic or mixed episodes associated with bipolar I disorder with or without psychotic features in adults. In Australia asenapine's approved (and also listed on the PBS) indications include the following: * Schizophrenia * Treatment, for up to 6 months, of an episode of acute mania or mixed episodes associated with bipolar I disorder * Maintenance treatment, as monotherapy, of bipolar I diso ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gepirone
Gepirone, sold under the brand name Exxua, is a medication used for the treatment of major depressive disorder. It is taken orally. Side effects of gepirone include dizziness, nausea, insomnia, abdominal pain, and dyspepsia (indigestion). Gepirone acts as a partial agonist of the serotonin 5-HT1A receptor. An active metabolite of gepirone, 1-(2-pyrimidinyl)piperazine, is an α2-adrenergic receptor antagonist. Gepirone is a member of the azapirone group of compounds. Gepirone was synthesized by Bristol-Myers Squibb in 1986 and was developed and marketed by Fabre-Kramer Pharmaceuticals. It was approved for the treatment of major depressive disorder in the United States in September 2023. This came after the drug had been rejected by the Food and Drug Administration (FDA) three times over two decades due to insufficient evidence of effectiveness. Medical uses Gepirone is indicated for the treatment of major depressive disorder (MDD) in adults. Of 15 clinical trials of gepi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Buspirone
Buspirone, sold under the brand name Buspar among others, is an anxiolytic, a medication primarily used to treat anxiety disorders, particularly generalized anxiety disorder (GAD). It is a serotonin 5-HT1A receptor, 5-HT1A receptor partial agonist, increasing action at serotonin receptors in the brain. It is taken orally and takes two to six weeks to be fully effective. Common side effects of buspirone include nausea, headaches, dizziness, and difficulty concentrating. Serious side effects may include movement disorders, serotonin syndrome, and seizures. Its use in pregnancy appears to be safe but has not been well studied, and use during breastfeeding has not been well studied either. Buspirone was developed in 1968 and approved for medical use in the United States in 1986. It is available as a generic medication. In 2022, it was the 54th most commonly prescribed medication in the United States, with more than 12million prescriptions. Medical uses Anxiety Buspirone is used ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
1-PP
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 moiety in their stru ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 α2 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. Research Alzheimer’s disease Mice treated with idazoxan, which blocks the α2A-adrenergic receptor, 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 disease pathology and symptoms in two mouse models, potentially offering an immediate treatment ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atipamezole
Atipamezole , sold under the brand name Antisedan among others, is a synthetic α2 adrenergic receptor antagonist used for the reversal of the sedative and analgesic effects of dexmedetomidine and medetomidine in dogs. Its reversal effect works by competing with the sedative for α2-adrenergic receptors and displacing them. It is mainly used in veterinary medicine, and while it is only licensed for dogs and for intramuscular use, it has been used intravenously, as well as in cats and other animals (intravenous use in cats and dogs is not recommended due to the potential for cardiovascular collapse. This occurs due to profound hypotension caused by reversal of the alpha 1 effects while the reflex bradycardia is still in effect.). There is a low rate of side effects, largely due to atipamezole's high specificity for the α2-adrenergic receptor. Atipamezole has a very quick onset, usually waking an animal up within 5 to 10 minutes. It was originally released in 1996. It is availa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Xylazine
Xylazine is a structural analog of clonidine and an α2-adrenergic receptor, α2-adrenergic receptor agonist, sold under many trade names worldwide, most notably the Bayer brand name Rompun, as well as Anased, Sedazine and Chanazine. Xylazine is a common veterinary drug used for sedation, anesthesia, muscle relaxation, and analgesia in animals such as horses, cattle, and other mammals. In veterinary anesthesia, it is often used in combination with ketamine. Veterinarians also use xylazine as an emetic, especially in cats. Drug interactions vary with different animals. Xylazine has become a commonly substance abuse, abused street drug in the United States where it is known by the street name "tranq", particularly in the territory of Puerto Rico. The drug is being drug diversion, diverted from stocks for equine veterinarians as well as trafficked in bulk from China to be used as a cutting agent for heroin and fentanyl, causing necrotic skin wounds leading to serious infections an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
