Description: Positive allosteric modulator and direct agonist of GABAA receptors
Chemical Name: (2β,3α,5α)-21-Chloro-3-hydroxy-2-(4-morpholinyl)pregnan-20-one
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Positive allosteric modulator and at higher concentrations direct agonist of GABAA receptors (EC50 = 1.1 μM). Also displays positive modulation of glycine receptors (EC50 = 22.9 μM). Anesthetic steroid; induces hypnosis and loss of righting reflexes in mice.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
1eq. HCl
43.8
100
DMSO
43.8
100
Preparing Stock Solutions
The following data is based on the product molecular weight 438.04. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.28 mL
11.41 mL
22.83 mL
5 mM
0.46 mL
2.28 mL
4.57 mL
10 mM
0.23 mL
1.14 mL
2.28 mL
50 mM
0.05 mL
0.23 mL
0.46 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Hill-Venninget al (1996) The anaesthetic action and modulaton of GABAA receptor activity by the novel water-soluble aminosteroid Org 20599. Neuropharmacology 35 1209 PMID: 9014136
Visseret al (2002) Neuroactive steroids differ in potency but not in intrinsic efficacy at the GABAA receptor in vivo. J.Pharmacol.Exp.Ther. 303 616 PMID: 12388643
Weiret al (2004) The interaction of anaesthetic steroids with recombinant glycine and GABAA receptors. Br.J.Anaesth. 92 704 PMID: 15033889