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Buspirone. Buspirone, sold under the brand name Buspar, among others, is an anxiolytic, a medication primarily used to treat anxiety disorders, particularly generalized anxiety disorder (GAD). [10][11] It is a serotonin 5-HT 1A receptor partial agonist, increasing action at serotonin receptors in the brain. [3]
5-HT 1A receptor (as partial or full agonists) 5-HT 2A receptor (as inverse agonists) D 2 receptor (as antagonists or partial agonists) α 1-adrenergic receptor (as antagonists) α 2-adrenergic receptor (as antagonists) Actions at D 4, 5-HT 2C, 5-HT 7, and sigma receptors have also been shown for some azapirones. [33] [34] [35] [36]
5-HT 1A receptor agonists like buspirone [18] and flesinoxan [19] show efficacy in relieving anxiety [20] and depression. [21] Buspirone and tandospirone are currently approved for these indications in different parts of the world.
Azapirones such as buspirone, gepirone, and tandospirone are 5-HT 1A receptor partial agonists marketed primarily as anxiolytics, but also as antidepressants. The antidepressants vilazodone and vortioxetine are 5-HT 1A receptor partial agonists. Flibanserin, a drug used for female sexual dysfunction, is a 5-HT 1A receptor partial agonist
Its crystallographic structure in ribbon representation. 5-HT receptors, 5-hydroxytryptamine receptors, or serotonin receptors, are a group of G protein-coupled receptor and ligand-gated ion channels found in the central and peripheral nervous systems. [1][2][3] They mediate both excitatory and inhibitory neurotransmission.
Buspirone (Buspar) is a 5-HT 1A receptor agonist used to treated generalized anxiety disorder. [37] If an individual has only recently stopped taking benzodiazepines, buspirone will be less effective. [38]
Cerebrovascular accident (stroke); Myocardial infarction (heart attack); Cardiomyopathy; Congestive heart failure; Bradycardia; Dysphoria; Hallucinations; Feelings of ...
Buspirone appears to be successful in ... 20: 5.1: 98: CYP2B6 (CYP2C19, CYP3A4, CYP2D6) ... Vilazodone is a 5-HT 1A receptor partial agonist while vortioxetine is a 5 ...