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Disulfiram Pathway, Pharmacodynamics (Serotonergic neuron)

PA166287781 Last updated September 2024
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Drugs & chemicals
0
Genes
0/0
Conditions
19
Reactions
Disulfiram Pathway, Pharmacodynamics (Serotonergic neuron) pathway diagram
Disulfiram Pathway, Pharmacodynamics (Serotonergic neuron) — pathway diagram from PharmGKB / ClinPGx
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About this pathway

Disulfiram inhibits ALDH in the metabolism of serotonin by serotonergic neurons. Here, serotonin (5-hydroxytryptamine, 5-HT) is converted into 5-hydroxyindole-3-acetaldehyde (5-hydroxyindole-3-aldehyde, 5-HIAL). 5-HIAL can be further metabolized by ALDH, which produces 5-hydroxyindole-3-acetic acid (5- HIAA), or by ADH and aldehyde reductase (ALDRL2/5), resulting in 5-hydroxytryptophol (5-HTOL). This change in the 5-HTOL/5-HIAA is thought to contribute to the cessation of cocaine use in patients [Article:9514292]. In addition to serotonin’s metabolism. disulfiram also impacts its synthesis. It does this by inhibiting tyrosine hydroxylase, primarily isoform 2 (TPH 2) [Article:2474765]. 5-HT is synthesized by the conversion of L-tryptophan into L-5-hydroxytryptophan (5-HTP) by TPH, which is further decarboxylated by AADC. By inhibiting the synthesis of serotonin—a neurotransmitter thought to heighten the effects of cocaine—disulfiram may be compromising the euphoric effects of cocaine.

Reactions & interactions (19)

  • Biochemical Reaction
    5-hydroxyindole-3-acetaldehyde → 5-hydroxyindole-3-acetic acid
  • Biochemical Reaction
    5-hydroxytryptophol → 5-hydroxytryptophol sulfate
  • Biochemical Reaction
    serotonin → 5-hydroxyindole-3-acetaldehyde
  • Biochemical Reaction
    5-hydroxyindole-3-acetaldehyde → 5-hydroxytryptophol
  • Biochemical Reaction
    l-tryptophan → 5-hydroxy-L-tryptophan
  • Biochemical Reaction
    5-hydroxytryptophol → 5-hydroxytryptophol glucuronide
  • Biochemical Reaction
    5-hydroxy-L-tryptophan → serotonin
  • Catalysis
    ALDH2 → Biochemical Reaction
  • Catalysis
    ALDH1A1 → Biochemical Reaction
  • Catalysis
    SULT1A1 → Biochemical Reaction
  • Catalysis
    MAOA → Biochemical Reaction
  • Catalysis
    MAOB → Biochemical Reaction
  • Catalysis
    ADH1B → Biochemical Reaction
  • Catalysis
    TPH2 → Biochemical Reaction
  • Catalysis
    UGT1A6 → Biochemical Reaction
  • Catalysis
    DDC → Biochemical Reaction
  • Inhibition
    disulfiram → ALDH2
  • Inhibition
    disulfiram → TPH2
  • Inhibition
    disulfiram → ALDH1A1

Edit history (5)

  • 2023-02-01 Create
  • 2023-07-21 Update Updated text and links.
  • 2023-09-22 Update Added citation
  • 2023-09-25 Update Added related pathways
  • 2024-09-04 Update fixed typo
Disulfiram Pathway, Pharmacodynamics (Serotonergic neuron) pathway diagram (enlarged)