| Bioactivity | E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity[1]. | ||||||||||||
| Invitro | 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 ([3H]1,3-di(2-tolyl)guanidine) for the sigma receptor by 38% in Jurkat cells[1]. | ||||||||||||
| 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[1]. Animal Model: | ||||||||||||
| Name | E1R | ||||||||||||
| CAS | 1301211-78-8 | ||||||||||||
| Formula | C13H16N2O2 | ||||||||||||
| Molar Mass | 232.28 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Zvejniece L, et al. The cognition-enhancing activity of E1R, a novel positive allosteric modulator of sigma-1 receptors. Br J Pharmacol. 2014 Feb;171(3):761-71. |