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SB 224289 is a selective serotonin 5-hydroxytryptamine receptor 1B (5‑HT₁B) antagonist or inverse agonist. It displays more than 60-fold selectivity for the human 5‑HT₁B receptor over other serotonin receptors and is centrally active following oral administration in vivo. The compound was originally developed by SmithKline Beecham (now GlaxoSmithKline) and has been used primarily as a research tool to study serotonergic signaling. Its mechanism of action involves blocking inhibitory serotonin autoreceptors (5‑HT₁B), thereby indirectly increasing serotonin release. While it has been investigated for potential antidepressant activity in preclinical studies, no human clinical trials have been reported. Additionally, it has shown antagonistic activity against the antifungal effects of marine depsipeptide papuamide A in Candida albicans[1][2][3][4][5][6].
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