Drug intelligence / Profile preview

harmaline

Development stage
Preclinical
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Peptides, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Oral, Inhalation
01

Overview

Harmaline is a naturally occurring beta-carboline alkaloid found primarily in the plant *Peganum harmala* and other sources. It is a reversible inhibitor of monoamine oxidase A (MAO-A), classifying it as a RIMA (reversible inhibitor of MAO-A). Harmaline exhibits central nervous system stimulant properties and mild psychedelic effects with pronounced physical side effects. Its mechanism of action includes inhibition of MAO-A, leading to increased levels of neurotransmitters such as serotonin and dopamine in the brain. Harmaline also acts as an acetylcholinesterase inhibitor, histamine N-methyltransferase inhibitor, and has weak affinity for serotonin 5-HT2A and 5-HT2C receptors. At high doses in animal models, it stimulates striatal dopamine release and can induce tremor by modulating T-type calcium channels within the inferior olive-cerebellar circuitry. Harmaline has been studied for its antiviral activity against herpes simplex virus types 1 and 2 by inhibiting viral transcription at noncytotoxic concentrations[1][2][3][5][6].

Other names
4,9-dihydro-7-methoxy-1-methyl-3H-pyrido[3,4-b]indoleharmalol methylene ether
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HTR2C (5-hydroxytryptamine 2C receptor)CaV3 (Caveolin-3)AcetylcholinesteraseMAOA (Monoamine oxidase A)HNMT (Histamine N-methyltransferase)

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