Chemistry:LEK-8841

LEK-8841, also known as N-methyl-N-(2-propynyl)-2-bromolysergamide or as 2-bromo-LEK-8842, is a monoamine receptor modulator of the lysergamide family related to 2-bromo-LSD. It is the 2-bromo derivative of LEK-8842.

The drug shows affinity for serotonin 5-HT₂ and α₁-adrenergic receptors (K_i = 16.3 nM at 5-HT₂) and acts as a silent antagonist of these receptors (A₂ = 11.7 nM and 355 nM, respectively), with activity described as qualitatively similar to that of ketanserin but with greater selectivity for serotonin 5-HT₂ receptors over α₁-adrenergic receptors. However, LEK-8841 was also subsequently found to interact with the dopamine D₁ and D₂ receptors (K_i = 360 nM and 11.3 nM, respectively). The drug inhibits apomorphine-induced hyperlocomotion and climbing behavior, induces catalepsy, inhibits the 5-hydroxytryptophan (5-HTP)-induced head twitch response, and produces hypotension in rodents.

LEK-8841 was first described in the scientific literature by 1992. It was developed by the Slovenian pharmaceutical company LEK Pharmaceuticals. The drug has been suggested as a potential clinically effective antipsychotic for medical use. Based on ratio of dopamine D₂ receptor antagonism to serotonin 5-HT₂ receptor antagonism, it is said to appear more like a typical than atypical antipsychotic.

See also

• Substituted lysergamide
• LEK-8842, LEK-8829, LEK-8822
• BOL-148 (2-bromo-LSD)