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Fluprazine
Fluprazine (DU-27,716) is a drug of the phenylpiperazine class. It is a so-called serenic or antiaggressive agent. It is closely related to several other piperazines, including eltoprazine and batoprazine, and TFMPP, as well as more distantly to the azapirones such as buspirone. The pharmacology of fluprazine is unknown, but it is likely to act as an agonist at the 5-HT1A and 5-HT1B receptors like its sister compound eltoprazine. See also * 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 ... References {{Piperazines meta-Trifluoromethylphenylpiperazines Serotonin receptor agonists Ureas ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serenic
A serenic, or antiaggressive agent, is a type of drug which reduces the capacity for irritability and aggression. Examples The recreational drug MDMA ("ecstasy") and a variety of related drugs have been described as ''empathogen-entactogens'', or simply as ''entactogens''. These agents possess serenic and empathy-increasing properties in addition to their euphoriant effects, and have been associated with increased sociability, friendliness, and feelings of closeness to others as well as emotional empathy and prosocial behavior. The entactogenic effects of these drugs are thought to be related to their ability to temporarily increase the levels of certain brain chemicals, including serotonin, dopamine, and, particularly, oxytocin. Certain other serotonergic drugs, such as 5-HT1A receptor, 5-HT1A receptor agonists, also increase oxytocin levels and may possess serenic properties as well. The phenylpiperazine mixed 5-HT1A and 5-HT1B receptor, 5-HT1B receptor agonists eltoprazine, flup ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eltoprazine
Eltoprazine (developmental code name DU-28,853) is a serotonergic drug of the phenylpiperazine class which is described as a serenic or antiaggressive agent. It acts as an agonist of the serotonin 5-HT1A and 5-HT1B receptors and as an antagonist of the serotonin 5-HT2C receptor. The drug is closely related to fluprazine and batoprazine, which are similarly acting agents, and is also a known chemical precursor to S-15535 and lecozotan. Eltoprazine is or was under development for the treatment of aggression, attention deficit hyperactivity disorder (ADHD), cognition disorders, and drug-induced dyskinesia, but no recent development has been reported for these indications as of February 2022. It was also under development for the treatment of psychotic disorders, but development for this indication was discontinued. Eltoprazine was originated by Solvay Solvay may refer to: Companies and organizations * Solvay Brussels School of Economics and Management, Brussels, Belgium * So ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Batoprazine
Batoprazine is a drug of the phenylpiperazine class which has been described as a serenic or antiaggressive agent. It acts as a 5-HT1A receptor, 5-HT1A and 5-HT1B receptor, 5-HT1B receptor agonist. It is closely related to eltoprazine, fluprazine, and naphthylpiperazine, of which possess similar actions and effects. See also * Phenylpiperazine References {{Piperazines N-(2-methoxyphenyl)piperazines Serotonin receptor agonists Coumarin drugs ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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-632 [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Aggressive
Aggression is overt or covert, often harmful, social interaction with the intention of inflicting damage or other harm upon another individual; although it can be channeled into creative and practical outlets for some. It may occur either reactively or without provocation. In humans, aggression can be caused by various triggers, from frustration due to blocked goals to feeling disrespected. Human aggression can be classified into direct and indirect aggression; whilst the former is characterized by physical or verbal behavior intended to cause harm to someone, the latter is characterized by behavior intended to harm the social relations of an individual or group. In definitions commonly used in the social sciences and behavioral sciences, aggression is an action or response by an individual that delivers something unpleasant to another person. Some definitions include that the individual must intend to harm another person. In an interdisciplinary perspective, aggression is regar ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
TFMPP
3-Trifluoromethylphenylpiperazine (TFMPP) is a recreational drug of the piperazine chemical class. Usually in combination with benzylpiperazine (BZP) and other analogues, it is sold as an alternative to the illicit drug MDMA ("Ecstasy"). Pharmacology TFMPP has affinity for the 5-HT1A (Ki = 288 nM), 5-HT1B (Ki = 132 nM), 5-HT1D (Ki = 282 nM), 5-HT2A (Ki = 269 nM), and 5-HT2C (Ki = 62 nM) receptors, and functions as a full agonist at all sites except the 5-HT2A receptor, where it acts as a weak partial agonist or antagonist. Unlike the related piperazine compound ''meta''-chlorophenylpiperazine (mCPP), TFMPP has insignificant affinity for the 5-HT3 receptor (IC50 = 2,373 nM). TFMPP also binds to the SERT (EC50 = 121 nM) and evokes the release of serotonin. It has no effects on dopamine or norepinephrine reuptake or efflux. Use and effects TFMPP is rarely used by itself. In fact, TFMPP reduces locomotor activity and produces aversive ef ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azapirone
Azapirones are a class of drugs used as anxiolytics, antidepressants, and antipsychotics. They are commonly used as add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs). Medical uses Azapirones have shown benefit in general anxiety and augmenting SSRIs in social anxiety and depression. Evidence is not clear for panic disorder and functional gastrointestinal disorders. Tandospirone has also been used to augment antipsychotics in Japan as it improves cognitive and negative symptoms of schizophrenia. Buspirone is being investigated for this purpose as well. Gepirone was abandoned after FDA rejection. Side effects Side effects of azapirones may include dizziness, headaches, restlessness, nausea, and diarrhea. Azapirones have more tolerable adverse effects than many other available anxiolytics, such as benzodiazepines or SSRIs. Unlike benzodiazepines, azapirones lack abuse potential and are not addictive, do not cause cognitive/memor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Buspirone
Buspirone, sold under the brand name Buspar, among others, is a medication primarily used to treat anxiety disorders, particularly generalized anxiety disorder. Benefits support its short-term use. It is taken by mouth, and it may take up to four weeks to have an effect. Common side effects of buspirone include nausea, headaches, dizziness, and difficulty concentrating. Serious side effects may include hallucinations, serotonin syndrome, and seizures. Its use in pregnancy appears to be safe but has not been well studied, while use during breastfeeding has not been well studied. It is a serotonin 5-HT1A receptor agonist. Buspirone was first made in 1968 and approved for medical use in the United States in 1986. It is available as a generic medication. In 2020, it was the 55th most-commonly prescribed medication in the United States, with more than 12million prescriptions. Medical uses Anxiety Buspirone is used for the short-term and long-term treatment of anxiety disorders ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology From the Greek αγωνιστής (agōnistēs), contestant; champion; rival < αγων (agōn), contest, combat; exertion, struggle < αγω (agō), I lead, lead towards, conduct; drive Types of agonists can be activated by either endogenous agonists (such as |
5-HT1A
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptor, or 5-HT receptor, that binds serotonin, also known as 5-HT, a neurotransmitter. 5-HT1A is expressed in the brain, spleen, and neonatal kidney. It is a G protein-coupled receptor (GPCR), coupled to the Gi protein, and its activation in the brain mediates hyperpolarisation and reduction of firing rate of the postsynaptic neuron. In humans, the serotonin 1A receptor is encoded by the HTR1A gene. Distribution The 5-HT1A receptor is the most widespread of all the 5-HT receptors. In the central nervous system, 5-HT1A receptors exist in the cerebral cortex, hippocampus, septum, amygdala, and raphe nucleus in high densities, while low amounts also exist in the basal ganglia and thalamus. The 5-HT1A receptors in the raphe nucleus are largely somatodendritic autoreceptors, whereas those in other areas such as the hippocampus are postsynaptic receptors. Function Neuromodulation 5-HT1A receptor ag ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1B
5-hydroxytryptamine receptor 1B also known as the 5-HT1B receptor is a protein that in humans is encoded by the ''HTR1B'' gene. The 5-HT1B receptor is a 5-HT receptor subtype. Tissue distribution and function 5-HT1B receptors are widely distributed throughout the central nervous system with the highest concentrations found in the frontal cortex, basal ganglia, striatum, and the hippocampus. The function of the 5-HT1B receptor differs depending upon its location. In the frontal cortex, it is believed to act as a postsynaptic receptor inhibiting the release of dopamine. In the basal ganglia and the striatum, evidence suggests 5-HT signaling acts on an autoreceptor, inhibiting the release of serotonin and decreasing glutamatergic transmission by reducing miniature excitatory postsynaptic potential (mEPSP) frequency, respectively. In the hippocampus, a recent study has demonstrated that activation of postsynaptic 5-HT1B heteroreceptors produces a facilitation in excitatory synap ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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