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Enilospirone
Enilospirone (CERM-3,726) is a selective 5-HT1A receptor agonist of the azapirone class. See also * Azapirone Azapirones are a class of drugs used as anxiolytics, antidepressants, and antipsychotics. They are commonly used as Augmentation (psychiatry), add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs). List of ... References Further reading * 3-Chlorophenyl compounds Phenol ethers Lactams Azapirones {{anxiolytic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Binding Selectivity
In chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex. Binding selectivity describes how a ligand may bind more preferentially to one receptor than another. A selectivity coefficient is the equilibrium constant for the reaction of displacement by one ligand of another ligand in a complex with the substrate. Binding selectivity is of major importance in biochemistry and in chemical separation processes. Selectivity coefficient The concept of selectivity is used to quantify the extent to which one chemical substance, A, binds each of two other chemical substances, B and C. The simplest case is where the complexes formed have 1:1 stoichiometry. Then, the two interactions may be characterized by equilibrium constants and .The constant used here are ''association'' constants. ''Dissociation'' constants are used in some contexts. A dissociation constant is the reciprocal of an association constant. \begin \ce;& \quad ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
5-HT1A Receptor
The serotonin 1A receptor (or 5-HT1A receptor) is a subtype of serotonin receptors, or 5-HT receptors, 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 hyperpolarization 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 pellucidum, septum, amygdala, and Raphe nuclei, 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 Neur ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive." Types of agonists Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...[...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 Augmentation (psychiatry), add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs). List of azapirones The azapirones include the following agents: ; Anxiolytics * Alnespirone (S-20,499) * Binospirone (MDL-73,005) * BMY-7,378 (CAS number: ) * Buspirone (Buspar) * Enilospirone (CERM-3,726) * Eptapirone (F-11,440) * Gepirone (Exxua) * Ipsapirone (TVX-Q-7,821) * MJ-7378 (CAS number: ) * Revospirone (BAY-VQ-7,813) * Tandospirone (Sediel) * Zalospirone (WY-47,846) ; Antipsychotics * Perospirone (Lullan) * Tiospirone (BMY-13,859) * Umespirone (KC-9,172) ; others *SNAP-8719 (CAS number: )CID:14086451 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Chemical Class
Chemical classification systems attempt to classify elements or compounds according to certain chemical functional or structural properties. Whereas the structural properties are largely intrinsic, functional properties and the derived classifications depend to a certain degree on the type of chemical interaction partners on which the function is exerted. Sometimes other criteria like purely physical ones (e.g. molecular weight) or – on the other hand – functional properties above the chemical level are also used for building chemical taxonomies. Some systems mix the various levels, resulting in hierarchies where the domains are slightly confused, for example having structural and functional aspects end up on the same level. Whereas chemical function is closely dependent on chemical structure, the situation becomes more involved when e.g. pharmacological function is integrated, because the QSAR can usually not be directly computed from structural qualities. Physico-ch ... [...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 Augmentation (psychiatry), add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs). List of azapirones The azapirones include the following agents: ; Anxiolytics * Alnespirone (S-20,499) * Binospirone (MDL-73,005) * BMY-7,378 (CAS number: ) * Buspirone (Buspar) * Enilospirone (CERM-3,726) * Eptapirone (F-11,440) * Gepirone (Exxua) * Ipsapirone (TVX-Q-7,821) * MJ-7378 (CAS number: ) * Revospirone (BAY-VQ-7,813) * Tandospirone (Sediel) * Zalospirone (WY-47,846) ; Antipsychotics * Perospirone (Lullan) * Tiospirone (BMY-13,859) * Umespirone (KC-9,172) ; others *SNAP-8719 (CAS number: )CID:14086451 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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenol Ethers
Phenol (also known as carbolic acid, phenolic acid, or benzenol) is an aromatic organic compound with the molecular formula . It is a white crystalline solid that is volatile and can catch fire. The molecule consists of a phenyl group () bonded to a hydroxy group (). Mildly acidic, it requires careful handling because it can cause chemical burns. It is acutely toxic and is considered a health hazard. Phenol was first extracted from coal tar, but today is produced on a large scale (about 7 million tonnes a year) from petroleum-derived feedstocks. It is an important industrial commodity as a precursor to many materials and useful compounds, and is a liquid when manufactured. It is primarily used to synthesize plastics and related materials. Phenol and its chemical derivatives are essential for production of polycarbonates, epoxies, explosives such as picric acid, Bakelite, nylon, detergents, herbicides such as phenoxy herbicides, and numerous pharmaceutical drugs. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactams
A lactam is a cyclic amide, formally derived from an amino alkanoic acid through cyclization reactions. The term is a portmanteau of the words '' lactone'' + ''amide''. Nomenclature Greek prefixes in alphabetical order indicate ring size. This ring-size nomenclature stems from the fact that hydrolysis of an α-lactam gives an α-amino acid and that of a β-Lactam gives a β-amino acid, and so on. Synthesis General synthetic methods are used for the organic synthesis of lactams. Beckmann rearrangement Lactams form by the acid-catalyzed rearrangement of oximes in the Beckmann rearrangement. Schmidt reaction Lactams form from cyclic ketones and hydrazoic acid in the Schmidt reaction. Cyclohexanone with hydrazoic acid, forms ε - Caprolactum, which upon treatment with excess acid forms Cardiazole, a heart stimulant. Cyclization of amino acids Lactams can be formed from cyclisation of amino acids via the coupling between an amine and a carboxylic acid within the s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
