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1301211-78-8

1301211-78-8 Structure

1301211-78-8 Structure
IdentificationBack Directory
[Name]

E1R
[CAS]

1301211-78-8
[Synonyms]

E1R
1-Pyrrolidineacetamide, 2-methyl-5-oxo-3-phenyl-, (2S,3R)-
[Molecular Formula]

C13H16N2O2
[MDL Number]

MFCD32067912
[MOL File]

1301211-78-8.mol
[Molecular Weight]

232.28
Chemical PropertiesBack Directory
[Boiling point ]

480.0±45.0 °C(Predicted)
[density ]

1.168±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO: 60 mg/mL (258.31 mM)
[form ]

Solid
[pka]

15.67±0.40(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack Directory
[Biological Activity]

E1R is a positive allosteric modulator of the sigma-1 receptor (Sig1R PAM) with cognitive enhancing effects.
[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.

[in vivo]

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

Animal Model: Male ICR and Balb/c mice weighed 23-25 g
Dosage: 0.1, 1 and 10 mg/kg
Administration: Administered ip 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.
[storage]

Store at -20°C
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