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Etiocholanedione Sale

(Synonyms: 雄甾-3,17-二酮) 目录号 : GC49762

A neurosteroid

Etiocholanedione Chemical Structure

Cas No.:1229-12-5

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1 mg
¥444.00
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25 mg
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产品描述

Etiocholanedione is a neurosteroid.1 It inhibits glycine-induced chloride currents (IGly) in isolated rat hippocampal pyramidal neurons when used at a concentration of 50 µM. Etiocholanedione (0.1, 0.3, and 0.5 mM) also inhibits glucose exchange transport in isolated human erythrocytes.2

1.Bukanova, J.V., SoIntserva, I., and Kudova, E.Neurosteroids as selective inhibitors of glycine receptor activity: Structure-activity relationship study on endogenous androstanes and androstenesFront. Mol. Neurosci.1344(2020) 2.Lacko, L., Wittke, B., and Geck, P.Interaction of steroids with the transport system of glucose in human erythrocytesJ. Cell. Physiol.86 Suppl 2(3 Pt 2)673-680(1975)

Chemical Properties

Cas No. 1229-12-5 SDF Download SDF
别名 雄甾-3,17-二酮
Canonical SMILES C[C@@]12[C@]3([H])[C@](CC[C@]1([H])CC(CC2)=O)([H])[C@@]4([H])[C@](CC3)(C(CC4)=O)C
分子式 C19H28O2 分子量 288.4
溶解度 DMSO: soluble,Ethanol: soluble 储存条件 -20°C
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1 mg 5 mg 10 mg
1 mM 3.4674 mL 17.337 mL 34.6741 mL
5 mM 0.6935 mL 3.4674 mL 6.9348 mL
10 mM 0.3467 mL 1.7337 mL 3.4674 mL
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Research Update

A randomized double-blind crossover study of the antiobesity effects of Etiocholanedione

Obes Res 1994 Jan;2(1):13-8.PMID:16353603DOI:10.1002/j.1550-8528.1994.tb00038.x.

Etiocholanedione (ED), a natural metabolite of dehydroepiandrosterone, has antiobesity effects in animals when given orally and is nontoxic. We carried out a trial of oral ED in obese humans. In a 20-week randomized double-blind crossover study, 14 subjects lost significantly more weight and body fat during treatment with oral ED, 4 gm daily, than during placebo administration. Mean weight loss during ED administration was 2.8 +/- 5.5 kilograms, which was equivalent to 0.53 +/- 0.91 kilograms per week per 100 kilograms of body fat; mean weight change during placebo administration was essentially zero: +0.21 +/- 4.2 kg, or +0.04 +/- 0.74 kg/wk/100 kg body fat. The difference between the weight changes in the two periods was significant: for delta kg, P < 0.05; for delta kg/wk/100 kg body fat, P < 0.03. Densitometric measurement of body fat content showed that the mean weight loss coincided almost exactly with the mean decrease in fat content; thus, over the 10-week period of ED administration, the mean fat loss was about 5% of the initial body fat content. Three of the obese subjects had strikingly greater fat loss, about 18%, 19%, and 25% of the initial body fat content. There were no significant subjective or objective side effects of ED administration.

Neurosteroids as Selective Inhibitors of Glycine Receptor Activity: Structure-Activity Relationship Study on Endogenous Androstanes and Androstenes

Front Mol Neurosci 2020 Mar 20;13:44.PMID:32265652DOI:10.3389/fnmol.2020.00044.

The ability of androstane and androstene neurosteroids with modifications at C-17, C-5, and C-3 (compounds 1-9) to influence the functional activity of inhibitory glycine and γ-aminobutyric acid (GABA) receptors was estimated. The glycine- and GABA-induced chloride current (I Gly and I GABA) were measured in isolated pyramidal neurons of the rat hippocampus and isolated rat cerebellar Purkinje cells, correspondingly, using the patch-clamp technique. Our results demonstrate that all the nine neurosteroids display similar biological activity, namely, they strongly inhibited I Gly and weakly inhibited I GABA. The threshold concentration of neurosteroids inducing effects on I Gly was 0.1 μM, and for effects on I GABA was 10-50 μM. Moreover, our compounds accelerated desensitization of the I Gly with the IC50 values varying from 0.12 to 0.49 μM and decreased the peak amplitude with IC50 values varying from 16 to 22 μM. Interestingly, our study revealed that only compounds 4 (epiandrosterone) and 8 (dehydroepiandrosterone) were able to cause a significant change in I GABA in 10 μM concentration. Moreover, compounds 3 (testosterone), 5 (epitestosterone), 6 (dihydroandrostenedione), and 9 (Etiocholanedione) did not modulate I GABA up to the concentration of 50 μM. Thus, we conclude that compounds 3, 5, 6, and 9 may be identified as selective modulators of I Gly. Our results offer new avenues of investigation in the field of drug-like selective modulators of I Gly.