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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 moiet ... [...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] |
Tandospirone
Tandospirone (brand name Sediel) is an anxiolytic and antidepressant drug used in China and Japan, where it is marketed by Dainippon Sumitomo Pharma. It is a member of the azapirone class of drugs and is closely related to other azapirones like buspirone and gepirone. Medical uses Anxiety and depression Tandospirone is most commonly used as a treatment for anxiety and depressive disorders, such as generalised anxiety disorder and dysthymia respectively. For both indications it usually takes a couple of weeks for therapeutic effects to begin to be seen, although at higher doses more rapid anxiolytic responses have been seen. It has also been used successfully as a treatment for bruxism. Augmentation for depression Tandospirone can be used as an effective augmentation, especially when coupled with fluoxetine or clomipramine. Other uses Tandospirone has been tried successfully as an adjunctive treatment for cognitive symptoms in schizophrenic individuals. Side effects Com ... [...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] |
α2-adrenergic
The alpha-2 (α2) adrenergic receptor (or adrenoceptor) is a G protein-coupled receptor (GPCR) associated with the Gi heterotrimeric G-protein. It consists of three highly homologous subtypes, including α2A-, α2B-, and 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 and peripheral nervous systems. Cellular localization The α2A adrenergic receptor is localised in the following central nervous system (CNS) structures: * Brainstem (especially the locus coeruleus) * Midbrain * Hypothalamus * Hippocampus * Spinal cord * Cerebral cortex * Cerebellum * Septum Whereas the α2B adrenergic receptor is localised in the following CNS structures: * Olfactory system * Thalamus * Pyramidal layer of the hippocampus * Cerebellar Purkinje layer and the α2C adrenergic receptor is localised in the CNS ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Revospirone
Revospirone (Bay Vq 7813) is an azapirone drug which was patented as a veterinary tranquilizer but was never marketed. It acts as a selective 5-HT1A receptor partial agonist. Similarly to other azapirones such as buspirone, revospirone produces 1-(2-pyrimidinyl)piperazine (1-PP) as an active metabolite. As a result, it also acts as an α2-adrenergic receptor antagonist An antagonist is a character in a story who is presented as the chief foe of the protagonist. Etymology The English word antagonist comes from the Greek ἀνταγωνιστής – ''antagonistēs'', "opponent, competitor, villain, enemy, riv ... to an extent. References 5-HT1A agonists Azapirones Benzothiazoles Lactams Piperazines Pyrimidines Sultams {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eptapirone
Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone family. Its affinity for the 5-HT1A receptor was reported to be 4.8 nM (Ki) (or 8.33 (pKi)), and its intrinsic activity approximately equal to that of serotonin (i.e., 100%). Eptapirone and related high-efficacy 5-HT1A full and super agonists such as befiradol and F-15,599 were developed under the hypothesis that the maximum exploitable therapeutic benefits of 5-HT1A receptor agonists might not be able to be seen without the drugs employed possessing sufficiently high intrinsic activity at the receptor. As 5-HT1A receptor agonism, based on animal and other research, looked extremely promising for the treatment of depression from a theoretical perspective, this idea was developed as a potential explanation for the relatively modest clinical effectiveness seen with already available 5-HT1A receptor agonists like buspirone and tandospirone, which act merely as weak-to-moderat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Alnespirone
Alnespirone (S-20,499) is a selective 5-HT1A receptor full agonist of the azapirone chemical class. It has antidepressant and anxiolytic effects. See also * 8-OH-DPAT * 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 ... References Serotonin receptor agonists Imides Resorcinol ethers Amines Azapirones Chromanes Lactams Cyclopentanes Cyclic ethers 2-Phenoxyethanamines Propyl compounds {{anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Metabolite
In biochemistry, a metabolite is an intermediate or end product of metabolism. The term is usually used for small molecules. Metabolites have various functions, including fuel, structure, signaling, stimulatory and inhibitory effects on enzymes, catalytic activity of their own (usually as a cofactor to an enzyme), defense, and interactions with other organisms (e.g. pigments, odorants, and pheromones). A primary metabolite is directly involved in normal "growth", development, and reproduction. Ethylene exemplifies a primary metabolite produced large-scale by industrial microbiology. A secondary metabolite is not directly involved in those processes, but usually has an important ecological function. Examples include antibiotics and pigments such as resins and terpenes etc. Some antibiotics use primary metabolites as precursors, such as actinomycin, which is created from the primary metabolite tryptophan. Some sugars are metabolites, such as fructose or glucose, which are both p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Azaspirodecanedione
Azaspirodecanedione is a chemical compound. It is a component of the chemical structures of several of the azapirones. See also * Azapirone * Azaspirodecane * Glutarimide * Ketone In organic chemistry, a ketone is a functional group with the structure R–C(=O)–R', where R and R' can be a variety of carbon-containing substituents. Ketones contain a carbonyl group –C(=O)– (which contains a carbon-oxygen double bo ... * Spirodecanedione Azapirones Imides Cyclopentanes Spiro compounds {{organic-compound-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zalospirone
Zalospirone (WY-47,846) is a binding selectivity, selective 5-HT1A receptor, 5-HT1A partial agonist of the azapirone chemical class. It was found to be effective in the treatment of anxiety and major depressive disorder, depression in clinical trials, but a high proportion of subjects dropped out due to side effects and development was subsequently never completed. See also * Azapirone References Piperazines Aminopyrimidines Imides Azapirones Cyclobutenes {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Umespirone
Umespirone (KC-9172) is a drug of the azapirone class which possesses anxiolytic and antipsychotic properties. It behaves as a 5-HT1A receptor partial agonist (Ki = 15 nM), D2 receptor partial agonist (Ki = 23 nM), and α1-adrenoceptor receptor antagonist (Ki = 14 nM), and also has weak affinity for the sigma receptor (Ki = 558 nM). Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation, cognitive/memory impairment, catalepsy, and extrapyramidal symptoms. Synthesis The condensation between ethyl cyanoacetate (1) and acetone gives ethylisopropylidenecyanoacetate 59-58-0(2). This product is reacted with N-butylcyanoacetamide 9581-21-0(3) in sodium methoxide solution to give N-butyl-2,4-dicyano-3,3-dimethylglutarimideCID:10681941(4). The glutarimide is cyclized with phosphoric acid to yield 3-butyl-9,9-dimethyl-3,7-diazabicyclo .3.1onane-2,4,6,8-tetraone, https://pubchem.ncbi.nlm.nih.gov/compound/10825633 CID:10825633 (5). The reaction between ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
