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Mepiprazole
Mepiprazole (INN, BAN) (brand name Psigodal) is an anxiolytic drug of the phenylpiperazine group with additional antidepressant properties that is marketed in Spain. It acts as a 5-HT2A and α1-adrenergic receptor antagonist and inhibits the reuptake and induces the release of serotonin, dopamine, and norepinephrine to varying extents, and has been described as a serotonin antagonist and reuptake inhibitor (SARI). Controlled clinical trials of mepiprazole in patients with irritable bowel syndrome (IBS) were also carried out and suggested some benefits of the drug in relieving symptoms of IBS in some patients. Similarly to other phenylpiperazines like trazodone, nefazodone, and etoperidone, mepiprazole produces ''m''CPP as an active metabolite An active metabolite is an active form of a drug after it has been processed by the body. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which continues to produce eff ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tolpiprazole
Tolpiprazole (International Nonproprietary Name, INN, British Approved Name, BAN) (developmental code name H-4170) is an anxiolytic drug of the phenylpiperazine group that was never marketed. See also * Acaprazine * Enpiprazole * Lorpiprazole * Mepiprazole References {{Piperazines Anxiolytics Phenylpiperazines Pyrazoles ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lorpiprazole
Lorpiprazole (INN) (brand name Normarex) is a marketed anxiolytic drug of the phenylpiperazine group. It has been described as a serotonin antagonist and reuptake inhibitor (SARI) in the same group as trazodone, nefazodone, and etoperidone. See also * Acaprazine * Enpiprazole * Mepiprazole Mepiprazole (INN, BAN) (brand name Psigodal) is an anxiolytic drug of the phenylpiperazine group with additional antidepressant properties that is marketed in Spain. It acts as a 5-HT2A and α1-adrenergic receptor antagonist and inhibits th ... * Tolpiprazole References Antidepressants Anxiolytics meta-Trifluoromethylphenylpiperazines Pyrroles Serotonin receptor antagonists Triazoles Cyclopentanes {{Anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Enpiprazole
Enpiprazole (International Nonproprietary Name, INN, British Approved Name, BAN) is an anxiolytic drug of the phenylpiperazine group that was never marketed. It produces anxiolytic-like effects in animals, though these effects appear to be biphasic and may reverse at high doses. It is known to produce ortho-chlorophenylpiperazine, ''ortho''-chlorophenylpiperazine (oCPP) as a metabolite. See also * Acaprazine * Enciprazine * Lorpiprazole * Mepiprazole * Tolpiprazole References Anxiolytics Chloroarenes Phenylpiperazines Pyrazoles {{Anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acaprazine
Acaprazine (International Nonproprietary Name, INN) is an anxiolytic and "adrenergic antagonist, adrenolytic" drug of the phenylpiperazine group that was never marketed. See also * Enciprazine * Enpiprazole * Lorpiprazole * Mepiprazole * Tolpiprazole References External links * Acetamides Anilines Anxiolytics meta-Chlorophenylpiperazines Abandoned drugs Sedatives {{Anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Serotonin Antagonist And Reuptake Inhibitor
Serotonin antagonist and reuptake inhibitors (SARIs) are a class of drugs used mainly as antidepressants, but also as anxiolytics and hypnotics. They act by antagonizing serotonin receptors such as 5-HT2A and inhibiting the reuptake of serotonin, norepinephrine, and/or dopamine. Additionally, most also antagonize α1-adrenergic receptors. The majority of the currently marketed SARIs belong to the phenylpiperazine class of compounds. List of SARIs Marketed * Etoperidone (Axiomin, Etonin) * Lorpiprazole (Normarex) * Mepiprazole (Psigodal) * Nefazodone (Serzone, Nefadar) * Trazodone (Desyrel) Miscellaneous * Vilazodone (Viibryd) – a related drug but does not fit into this class as it does not function as a serotonin antagonist, acting solely as a 5-HT1A receptor partial agonist instead. * Vortioxetine (Trintellix) – another closely related drug, could technically be considered to be a member of this group, but both vilazodone and vortioxetine are instead generally labe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine
Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad'', "near", and '' ren'', "kidney") is more commonly used in the United Kingdom, whereas "norepinephrine" (from Ancient Greek ἐπῐ́ (''epí''), "upon", and νεφρός (''nephrós''), "kidney") is usually preferred in the United States. "Norepinephrine" is also the international nonproprietary name given to the drug. Regardless of which name is used for the substance itself, parts of the body that produce or are affected by it are referred to as noradrenergic. The general function of norepinephrine is to mobilize the brain and body for action. Norepinephrine release is lowest during sleep, rises during wakefulness, and reaches much higher levels during situations of stress or danger, in the so-called fight-or-flight response. In the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alpha-1 Blockers
Alpha 1 or Alpha-1 may refer to: *Alpha-1 adrenergic receptor, a G protein-coupled receptor *Alpha-1 antitrypsin, a protein **Alpha-1 antitrypsin deficiency, a genetic disorder *Alpha-1-fetoprotein or Alpha-fetoprotein, a protein *Alpha-One, a fictional spacecraft in '' Buzz Lightyear of Star Command: The Adventure Begins'' * ''Alpha 1'' (Robert Silverberg anthology), a 1970 book See also * * *Alpha (other) *AMY1A Alpha-amylase 1 is an enzyme that in humans is encoded by the ''AMY1A'' gene In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth' ... or Alpha-1A or, an enzyme found in humans and other mammals * List of A1 genes, proteins or receptors {{disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT2A Antagonists
The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled receptor (GPCR). The 5-HT2A receptor is a cell surface receptor, but has several intracellular locations. 5-HT is short for 5-hydroxy-tryptamine or serotonin. This is the main excitatory receptor subtype among the GPCRs for serotonin, although 5-HT2A may also have an inhibitory effect on certain areas such as the visual cortex and the orbitofrontal cortex. This receptor was first noted for its importance as a target of serotonergic psychedelic drugs such as LSD and psilocybin mushrooms. Later it came back to prominence because it was also found to be mediating, at least partly, the action of many antipsychotic drugs, especially the atypical ones. Downregulation of post-synaptic 5-HT2A receptor is an adaptive process provoked by chronic administration of selective serotonin reuptake inhibitors (SSRIs) and atypical antipsychotics. Suicidal and otherwise ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Active Metabolite
An active metabolite is an active form of a drug after it has been processed by the body. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which continues to produce effects in the body. Usually these effects are similar to those of the parent drug but weaker, although they can still be significant (see e.g. 11-hydroxy-THC, morphine-6-glucuronide). Certain drugs such as codeine and tramadol have metabolites (morphine and ''O''-desmethyltramadol respectively) that are stronger than the parent drug and in these cases the metabolite may be responsible for much of the therapeutic action of the parent drug. Sometimes, however, metabolites may produce toxic effects and patients must be monitored carefully to ensure they do not build up in the body. This is an issue with some well-known drugs, such as pethidine (meperidine) and dextropropoxyphene. Prodrugs Sometimes drugs are formulated in an inactive form that is designe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Meta-Chlorophenylpiperazine
''meta''-Chlorophenylpiperazine (mCPP) is a psychoactive drug of the phenylpiperazine class. It was initially developed in the late-1970s and used in scientific research before being sold as a designer drug in the mid-2000s. It has been detected in pills touted as legal alternatives to illicit stimulants in New Zealand and pills sold as " ecstasy" in Europe and the United States. Despite its advertisement as a recreational substance, mCPP is actually generally considered to be an unpleasant experience and is not desired by drug users. It lacks any reinforcing effects, but has "psychostimulant, anxiety-provoking, and hallucinogenic effects." It is also known to produce dysphoric, depressive, and anxiogenic effects in rodents and humans, and can induce panic attacks in individuals susceptible to them. It also worsens obsessive–compulsive symptoms in people with the disorder. mCPP is known to induce headaches in humans and has been used for testing potential antimigraine m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etoperidone
Etoperidone, associated with several brand names, is an atypical antidepressant which was developed in the 1970s and either is no longer marketed or was never marketed. It is a phenylpiperazine related to trazodone and nefazodone in chemical structure and is a serotonin antagonist and reuptake inhibitor (SARI) similarly to them. Medical uses Etoperidone was used or was intended for use as an antidepressant in the treatment of depression. Pharmacology Pharmacodynamics Etoperidone is as an antagonist of several receptors in the following order of potency: 5-HT2A receptor (36 nM) > α1-adrenergic receptor (38 nM) > 5-HT1A receptor (85 nM) (may be a partial agonist) > α2-adrenergic receptor (570 nM); it has only very weak or negligible affinity for blocking the following receptors: D2 receptor (2,300 nM) > H1 receptor (3,100 nM) > mACh receptors (>35,000 nM). In addition to its receptor blockade, etoperidone also has weak affinity for the monoamine transporters as well ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
