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CM699 is a dual σ receptor antagonist (Kis = 0.0141 and 0.00231 µM for the σ1 and σ2 receptors, respectively) and dopamine transporter (DAT) inhibitor (Ki = 0.311 µM).1 It is selective for the σ1 and σ2 receptors and DAT over the serotonin transporter (SERT; Ki = 2.83 µM) but also binds to the norepinephrine transporter (NET; Ki = 0.232 µM). CM699 inhibits dopamine uptake in rat striatal synaptosomes (IC50 = 6.01 µM) and induces σ1 receptor multimerization, indicating antagonist activity, in HEK293 cells expressing the human receptor when used at a concentration of 20 µM. In vivo, CM699 decreases self-administration of cocaine in rats.
WARNING This product is not for human or veterinary use.
1. Preclinical profile of CM699 as a medication candidate for stimulant use disorder. ACS Chem. Neurosci. 16(8), 1454-1468 (2025).