E1R

• CAT Number: I019056
• CAS Number: 1301211-78-8
• Molecular Formula: C13H16N2O2
• Molecular Weight: 232.28
• Purity: ≥95%
• Synonyms: 2-[(2S,3R)-2-methyl-5-oxo-3-phenylpyrrolidin-1-yl]acetamide
• InChI: InChI=1S/C13H16N2O2/c1-9-11(10-5-3-2-4-6-10)7-13(17)15(9)8-12(14)16/h2-6,9,11H,7-8H2,1H3,(H2,14,16)/t9-,11-/m0/s1
• InChIKey: ZTGRWYMPQCQTHD-ONGXEEELSA-N
• SMILES: CC1C(CC(=O)N1CC(=O)N)C2=CC=CC=C2

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

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.
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