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E1R is a positive allosteric modulator of sigma-1 receptors ( Sig1R PAM ) with cognition-enhancing activity.
In Vitro
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 ([ 3 H]1,3-di(2-tolyl)guanidine) for the sigma receptor by 38% in Jurkat cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male ICR and Balb/c mice weighed 23-25 g Dosage: 0.1, 1 and 10 mg/kg Administration: Administered i.p. 60 min before the training session Result: Treatment at doses of 1 and 10 mg/kg increased retention latency by 194 and 211%, respectively, compared with the control group.