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Rauwolscine, a natural alkaloid, is a specific and reversible α2-adrenergic receptor antagonist (Ki: 12 nM) [1]. It is a stereoisomer of yohimbine, which potently antagonizes both α1- and α2-adrenergic receptors [1]. Rauwolscine also acts as a receptor antagonist at the serotonin 5-HT2B receptor (Ki: 14.3 nM) and as a weak partial agonist at 5-HT1A (IC50: 1.3 μM) [3]. The α2-adrenergic receptor has diverse physiological functions and antagonists like rauwolscine have numerous applications, including the modulation of mood and behavior [5].