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Related Experiment Video

Updated: Jan 20, 2026

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Rasagiline derivatives combined with histamine H3 receptor properties.

K Lutsenko1, S Hagenow1, A Affini1

  • 1Heinrich Heine University Düsseldorf, Institute of Pharmaceutical and Medicinal Chemistry, Universitaetsstr. 1, 40225 Duesseldorf, Germany.

Bioorganic & Medicinal Chemistry Letters
|August 19, 2019
PubMed
Summary

New rasagiline derivatives targeting both monoamine oxidase B (MAO-B) and histamine H3 receptors (H3R) show promise for Parkinson's disease. Compound 1 exhibits potent dual-target inhibition, suggesting a novel multitargeting therapeutic strategy.

Keywords:
LadostigilMAO B inhibitorMonoamine oxidaseMultitarget-directed ligandParkinson’s diseasehistamine H(3) receptor

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Area of Science:

  • Medicinal Chemistry
  • Neuroscience
  • Pharmacology

Background:

  • Rasagiline, a monoamine oxidase B (MAO-B) inhibitor, demonstrates disease-modifying effects in Parkinson's disease models.
  • Histamine H3 receptors (H3R) are emerging targets for neurological disorders.
  • Multitargeting ligands offer potential for enhanced therapeutic efficacy.

Purpose of the Study:

  • To design and synthesize novel multitargeting ligands combining MAO-B inhibition with H3R antagonism.
  • To evaluate the in vitro potency and selectivity of novel rasagiline derivatives.

Main Methods:

  • Synthesis of 5-substituted and 6-substituted 3-piperidinopropyloxy rasagiline derivatives.
  • In vitro enzymatic assays to determine MAO-A and MAO-B inhibition.
  • Radioligand binding assays to assess affinity for H3R and other receptors.

Main Results:

  • Derivative 1, a 5-substituted isomer, demonstrated superior potency at both MAO-B (IC50 = 256 nM) and H3R (Ki = 2.6 nM).
  • Compound 1 displayed high selectivity for MAO-B over MAO-A.
  • Negligible affinity was observed for histamine H1, H4 receptors, dopamine D2, D3 receptors, and cholinesterases.

Conclusions:

  • The 5-substituted rasagiline derivative 1 is a potent dual inhibitor of MAO-B and H3R.
  • This compound represents a promising lead for the development of novel multitargeting therapeutics for Parkinson's disease.
  • The findings support the strategy of combining MAO-B inhibition with H3R antagonism for neurodegenerative disorders.