Allopregnanolone (Synonyms: ALLO, 3α,5α-tetrahydro Progesterone, 3α,5α-THP) |
| Katalog-Nr.GC14192 |
Allopregnanolone, a 3alpha, 5alpha progesterone metabolite, acts as a potent allosteric modulator of the γ-aminobutyric acid type A (GABAA) receptor, exerts antidepressant and neuroprotective action.
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Cas No.: 516-54-1
Sample solution is provided at 25 µL, 10mM.
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Allopregnanolone, a 3alpha, 5alpha progesterone metabolite, acts as a potent allosteric modulator of the γ-aminobutyric acid type A (GABAA) receptor, exerts antidepressant and neuroprotective action [1]. The levels of this neuroactive steroid as well as its effects are sexdimorphic [2].
Allopregnanolone (3 µM) present in the culture medium for 5 days did not change the amount of active, phosphorylated form of protein kinase B (PKB, Akt) and extracellular signal-regulated kinase (ERK). Allopregnanolone and THDOC inhibited basal and forskolin-induced CRH gene promoter activity in the differentiated Neuro-2A cells [1].
Allopregnanolone treatment exerted protective effects also in experimental models of neurodegeneration. For instance, Allopregnanolone(2 mg/kg, i.p.) is protective against kainic acidinduced excitotoxicity in the hippocampus in vivo [3]. In the nucleus accumbens of learned helplessness rats (i.e., an experimental model of depression) the astroglial glutamate transporter-1 and glutamine synthetase system is normalized by Allopregnanolone treatment [4]. In mood and anxiety disorders, Allopregnanolone (3 mg/kg and 1 mg/kg, s.c) treatment shows sex specific features. This neuroactive steroid attenuates in females, but not in males, the HPA axis responses to interleukin-1β in adult prenatally stressed rats [5].
References:
[1]. Budziszewska B, Zając A, Basta-Kaim A, et al. Effects of neurosteroids on the human corticotropin-releasing hormone gene[J]. Pharmacological Reports, 2010, 62(6): 1030-1040.
[2]. Diviccaro S, Cioffi L, Falvo E, et al. Allopregnanolone: An overview on its synthesis and effects[J]. Journal of Neuroendocrinology, 2022
[3]. Ciriza I, Carrero P, Frye C A, et al. Reduced metabolites mediate neuroprotective effects of progesterone in the adult rat hippocampus. The synthetic progestin medroxyprogesterone acetate (Provera) is not neuroprotective[J]. Journal of neurobiology, 2006, 66(9): 916-928.
[4]. Nangaku M, Yoshino K, Oda Y, et al. Astroglial glutamate transporter 1 and glutamine synthetase of the nucleus accumbens are involved in the antidepressant-like effects of allopregnanolone in learned helplessness rats[J]. Behavioural Brain Research, 2021, 401: 113092.
[5]. Brunton P J, Donadio M V, Yao S T, et al. 5α-Reduced neurosteroids sex-dependently reverse central prenatal programming of neuroendocrine stress responses in rats[J]. Journal of Neuroscience, 2015, 35(2): 666-677.
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