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 (Ki = 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 (Ki = 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)
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