Pregnenolone 是一种由胆固醇合成的内源性类固醇激素,用于治疗阿尔茨海默病。它是大麻素CB1受体的信号传导特异性抑制剂,抑制由CB1受体介导的四氢大麻酚 的作用。它也是TRPM3通道激活剂,也可弱激活TRPM1通道。
产品描述
Pregnenolone is an endogenous steroid hormone synthesized from cholesterol, used in the treatment of Alzheimer's disease.
体外活性
Pregnenolone induces a large, dose-related increase of both the rate and extent of MAP2-induced tubulin assembly, whereas progesterone, inactive per se, counteracted the stimulatory effect of Pregnenolone. Pregnenolone-increased assembly of microtubules produces a completely normal structure. [1] Pregnenolone preserves microtubule abundance and promotes cell movement during epiboly. [2] Pregnenolone results in dramatic reduction in GR nuclear localization in mouse hippocampal cell line (HT-22). Pregnenolone has neuroprotective effects against both glutamate and amyloid beta protein neuropathology. [3]
体内活性
Pregnenolone sustains its proliferative activity in vivo and stimulates the growth of LNCaP-tumor xenografts in intact male SCID mice as well as in castrated animals. Pregnenolone is shown to activate transcription through the LNCaP androgen receptor (AR), but not the wild-type AR. [4] Pregnenolone results in a significant decrease in the accumulation of astrocytes in the proximity of the wound and in a decreased bromodeoxyuridine incorporation in reactive astrocytes of rats. [5] Pregnenolone administration results in elevations in downstream neurosteroids such as allopregnanolone, a molecule with neuroprotective effects that also increases neurogenesis, decreases apoptosis and inflammation, modulates the hypothalamic-pituitary-adrenal axis, and markedly increases GABA(A) receptor responses. Pregnenolone administration elevates pregnenolone sulfate, a neurosteroid that positively modulates NMDA receptors. [6]
Cas No.
145-13-1
分子式
C21H32O2
分子量
316.485
别名
3β-Hydroxy-5-pregnen-20-one;孕烯醇酮;Arthenolone
储存和溶解度
Ethanol:21 mg/mL (66.4 mM)
DMSO:21 mg/mL (66.4 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years