Drug intelligence / Profile preview

LEK-8829

Development stage
Preclinical
Lead developer
Lek
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

LEK-8829 is an **ergoline derivative** with a unique pharmacological profile, acting as a **dopamine D1 receptor agonist** and a **dopamine D2 receptor antagonist**, while also exhibiting high affinity for **serotonin 5-HT2** and **5-HT1A receptors**. It is considered a putative atypical antipsychotic with potential applications in the treatment of **psychotic disorders**, including drug-induced psychosis in Parkinson’s disease, and as a candidate medication for **cocaine craving in addiction**. LEK-8829 demonstrates mesolimbic selectivity, which may contribute to a **lower propensity for extrapyramidal side effects**, sedation, anticholinergic, and hypotensive side effects compared to classic antipsychotics. It has been primarily developed as an experimental tool for investigating D1:D2 receptor interactions and exhibits beneficial effects in both dopaminergic and serotonergic systems[1][3][5][7].

Other names
9,10-didehydro-N-methyl-N-(2-propynyl)-6-methyl-8β-aminomethylergoline bimaleate
02

Targets

DRD1 (Dopamine D1 Receptor)DRD2 (Dopamine D2 Receptor)5-HT2 (5-HT2 receptor family)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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