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BUSPIRONE

IUPAC Name: 8-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione

Symbol: BU

Molecular Formula: C21H31N5O2

Molecular weight: 385.5 g/mol

CAS No: 36505-84-7

ATC Code: N05BE01

Drug Class: Antianxiety

General Properties:

Buspirone is an azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position. It has a role as an anxiolytic drug, a sedative, a serotonergic agonist and an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor. It is an azaspiro compound, a member of pyrimidines, a N-arylpiperazine, a N-alkylpiperazine, a member of piperidones and an organic heteropolycyclic compound. It is a conjugate base of a buspirone(1+).

Buspirone is a novel anxiolytic agent with a unique structure and a pharmacological profile. Belonging to the azaspirodecanedione drug class, buspirone is a serotonin 5-HT1A receptor agonist that is not chemically or pharmacologically related to benzodiazepines, barbiturates, and other sedative/anxiolytic drugs. Unlike many drugs used to treat anxiety, buspirone does not exhibit anticonvulsant, sedative, hypnotic, and muscle-relaxant properties. Due to these characteristics, buspirone been termed ‘anxioselective’. First synthesized in 1968 then patented in 1975, it is commonly marketed under the brand name Buspar®. Buspirone was first approved in 1986 by the FDA and has been used to treat anxiety disorders, such as generalized anxiety disorder (GAD), and relieve symptoms of anxiety. It has also been used as a second-line therapy for unipolar depression when the use of selective serotonin reuptake inhibitors (SSRIs) is deemed clinically inadequate or inappropriate. The potential use of buspirone in combination with [melatonin] in depression and cognitive impairment via promoting neurogenesis has also been investigated.

Buspirone is a psychoactive drug used for management of general anxiety disorders and alleviation of the symptoms of anxiety. Despite wide scale use, it is an infrequent cause of serum enzyme elevations and has not been linked to instances of clinically apparent liver injury with jaundice.

Indication:

Buspirone is primarily used to treat generalized anxiety disorder (GAD). It is an FDA-approved medicine for managing anxiety disorders or the short-term relief of anxiety symptoms. Off-labeled buspirone is used for the augmentation of unipolar depression.

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