NE 100 is a potent antagonist of sigma-1 (σ) receptors (IC = 4.16 nM). It only weakly antagonizes dopamine, serotonin, and PCP receptors, but may indirectly alter receptor activity through its effects on σ NE 100 is commonly used to study the role of σ receptor signaling in cells or animals.
NE 100 (NE 100 hydrochloride) is an orally active and selective sigma-1 receptor antagonist with an IC50 of 4.16 nM. NE 100 (NE 100 hydrochloride) can improve cognitive impairment and has neuroprotective and antipsychotic activities. NE 100 (NE 100 hydrochloride) can be used for research on nervous system diseases.
体外研究
NE 100 (0.1-3 µM; 1-25 h) can inhibit cell death and regulate the expression of endoplasmic reticulum stress-related proteins in HT22 cells treated with Tunicamycin. The mechanism involves activation of the ATF6 pathway [1].
Western Blot Analysis
Cell Line:
Tunicamycin treated HT22 cells
Concentration:
3 µM
Incubation Time:
Pretreated with 1 h, then co-incubation for 24 h
Result:
Inhibited the protein level of CHOP.
体内研究
NE 100 (oral; Single dose) has antipsychotic activity in rats.
NE 100 (0.03-1 mg/kg; oral administration; Single dose Hydrochloride has an improving effect in a rat model of cognitive impairment.
Animal Model:
Male Wistar rats (80-120 g) treated (+)SKF10047 or phencyclidine to induce head-weaving behavior model
Dosage:
Administration:
Oral administration; single dose
Result:
Dose-dependently antagonized (+)SKF10047 (HY-101376) or phencyclidine induced head-weaving behavior with oral ED50 at 0.27 and 0.12 mg/kg, respectively.
Animal Model:
Male Wistar rats (~250 g) treated phencyclidine to induce delayed cognitive dysfunction
Dosage:
0.03, 0.1 and 0.3 mg/kg (before the first trial of the water maze test)
0.1, 0.3 and 1 mg/kg (after phencyclidine injection)
Administration:
Oral administration; single dose
Result:
Significantly and dose-dependently reduced the escape latency of rats in the water maze task, indicating improvement of phencyclidine-induced delayed cognitive dysfunction.
Had lower effective doses when administered before the trial (late intervention) compared to administration after phencyclidine injection (early intervention).
分子式
C23H33NO2.HCl
分子量
391.97
CAS号
149409-57-4
中文名称
N,N-二乙基-2-(4-甲氧基-3-苯乙基氧基苯基)乙胺盐酸盐
运输条件
Room temperature in continental US; may vary elsewhere.