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Buspirone

Name: Buspirone
Description: An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam. (PubChem) Pharmacology: Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems. Mechanism of action: Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced. Drug type: Approved. Investigational. Small Molecule. Drug category: Anti-anxiety Agents. Anxiolytics sedatives and hypnotics. Serotonin Agonists
Synonym(s): Buspirona (INN-Spanish), Buspirone, Buspirone HCL, Buspironum (INN-Latin), Ansial, Ansiced, Anxiron, Axoren, Bespar, Buspar, Buspimen, Buspinol, Buspisal, Censpar, Lucelan, Narol, Travin, Wellbutrin XL
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB00490
Id: CHEBI: 3223
Related to: 5-hydroxytryptamine 1A receptor, D(2) dopamine receptor
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Bandrow, Ccdbuser, Nifbot2



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Commenttaken from DrugBank
CurationStatusuncurated  +
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB00490  +
DefinitionAn anxiolytic agent and a serotonin recept An anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam. (PubChem) Pharmacology: Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems. Mechanism of action: Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced. Drug type: Approved. Investigational. Small Molecule. Drug category: Anti-anxiety Agents. Anxiolytics sedatives and hypnotics. Serotonin Agonists edatives and hypnotics. Serotonin Agonists
Has roleDrug  +
IdCHEBI: 3223  +
LabelBuspirone  +
ModifiedDate14 April 2014  +
RelatedTo5-hydroxytryptamine 1A receptor  +, and D(2) dopamine receptor  +
SuperCategoryMolecular entity  +
SynonymBuspirona (INN-Spanish)  +, Buspirone  +, Buspirone HCL  +, Buspironum (INN-Latin)  +, Ansial  +, Ansiced  +, Anxiron  +, Axoren  +, Bespar  +, Buspar  +, Buspimen  +, Buspinol  +, Buspisal  +, Censpar  +, Lucelan  +, Narol  +, Travin  +, and Wellbutrin XL  +