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E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.

The only target for E1R (inhibition or enhancement of radioligand binding exceeding 20%) is the sigma receptor. 10 μM E1R does not displace the radioligand, but instead increases the specific binding of a non-selective radioligand ([H]1,3-di(2-tolyl)guanidine) for the sigma receptor by 38% in Jurkat cells.

E1R demonstrates efficacy against scopolamine-induced cholinergic dysfunction in mice. Treatment with E1R (0.1-10 mg/kg; administered i.p. 60 min before the training session) significantly improves cognitive function in a dose-related manner in mice.

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