Drug intelligence / Profile preview

mesembrine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Mesembrine is a naturally occurring alkaloid primarily found in the plant Sceletium tortuosum (Kanna), native to South Africa[1][2][7]. It features a tricyclic aryloctahydroindole skeleton and is most concentrated in the aerial parts of the plant[7]. Mesembrine is best known for its potent inhibition of the serotonin transporter (SERT), acting as a serotonin reuptake inhibitor (SRI) with greater potency than fluoxetine[3][5][7]. Additionally, it inhibits the enzyme phosphodiesterase-4 (PDE4), which increases intracellular cAMP and may contribute to its antidepressant, anxiolytic, and possible cognitive-enhancing effects[1][3]. Mesembrine-containing extracts have been traditionally used for managing symptoms of anxiety, depression, stress, and for mood elevation[1][3][7]. Other potential indications under investigation include reduction of substance cravings and amelioration of withdrawal symptoms[1][5].

Other names
3a-(3,4-dimethoxyphenyl)octahydro-1-methyl-6H-indol-6-one(-)-mesembrinemesembranone3a-(3,4-dimethoxyphenyl)tetrahydro-1-methyl-6(3aH)-indolinone
02

Targets

SERT (Sodium-dependent serotonin transporter)PDE4 (Phosphodiesterase 4A1)

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