PUBLICATION

Validation of L-type calcium channel blocker amlodipine as a novel ADHD treatment through cross-species analysis, drug-target Mendelian randomization, and clinical evidence from medical records

Authors
Þorsteinsson, H., Baukmann, H.A., Sveinsdóttir, H.S., Halldórsdóttir, D.Þ., Grzymala, B., Hillman, C., Rolfe-Tarrant, J., Parker, M.O., Cope, J.L., Ravarani, C.N.J., Schmidt, M.F., Karlsson, K.Æ.
ID
ZDB-PUB-250216-6
Date
2025
Source
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology : (Journal)
Registered Authors
Karlsson, Karl, Parker, Matt, Þorsteinsson, Haraldur
Keywords
none
MeSH Terms
  • Attention Deficit Disorder with Hyperactivity*/drug therapy
  • Attention Deficit Disorder with Hyperactivity*/genetics
  • Female
  • Rats, Inbred SHR
  • Calcium Channel Blockers*/pharmacology
  • Calcium Channel Blockers*/therapeutic use
  • Mendelian Randomization Analysis
  • Male
  • Calcium Channels, L-Type*/genetics
  • Rats
  • Humans
  • Animals
  • Species Specificity
  • Amlodipine*/pharmacology
  • Amlodipine*/therapeutic use
PubMed
39953207 Full text @ Neuropsychopharmacology
Abstract
ADHD is a chronic neurodevelopmental disorder that significantly affects life outcomes, and current treatments often have adverse side effects, high abuse potential, and a 25% non-response rate, highlighting the need for new therapeutics. This study investigates amlodipine, an L-type calcium channel blocker, as a potential foundation for developing a novel ADHD treatment by integrating findings from animal models and human genetic data. Amlodipine reduced hyperactivity in SHR rats and decreased both hyperactivity and impulsivity in adgrl3.1-/- zebrafish. It also crosses the blood-brain barrier, reducing telencephalic activation. Crucially, Mendelian Randomization analysis linked ADHD to genetic variations in L-type calcium channel subunits (α1-C; CACNA1C, β1; CACNB1, α2δ3; CACNA2D3) targeted by amlodipine, while polygenic risk score analysis showed symptom mitigation in individuals with high ADHD genetic liability. With its well-tolerated profile and efficacy across species, supported by genetic evidence, amlodipine shows potential to be refined and developed into a novel treatment for ADHD.
Genes / Markers
Figures
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Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Antibodies
Orthology
Engineered Foreign Genes
Mapping