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THDOC

(Synonyms: 3ALPHA,21-二羟基-5ALPHA-孕甾-20-酮,THDOC) 目录号 : GC45961

A neurosteroid and positive allosteric modulator of GABAA receptors

THDOC Chemical Structure

Cas No.:567-02-2

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5mg
¥2,340.00
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10mg
¥3,780.00
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Sample solution is provided at 25 µL, 10mM.

Description

THDOC is a neurosteroid and positive allosteric modulator of GABAA receptors.1 It inhibits binding of the convulsant t-butylbicyclophosphorothionate (TBPS) and increases binding of the benzodiazepine flunitrazepam to rat synaptosomal membrane preparations in a concentration-dependent manner.2 THDOC potentiates GABA-induced chloride currents in cultured rat hippocampal and spinal cord neurons. It inhibits seizures induced by pilocarpine or pentylenetetrazol in mice (ED50s = 7.3 and 15 mg/kg, respectively).3 THDOC (20 mg/kg) increases the number of entries into and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic activity.4

|1. Usami, N., Yamamoto, T., Shintani, S., et al. Substrate specificity of human 3(20)α-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol. Pharm. Bull. 25(4), 441-445 (2002).|2. Majewska, M.D., Harrison, N.L., Schwartz, R.D., et al. Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science 232(4753), 1004-1007 (1986).|3. Kokate, T.G., Cohen, A.L., Karp, E., et al. Neuroactive steroids protect against pilocarpine- and kainic acid-induced limbic seizures and status epilepticus in mice. Neuropharmacology 35(8), 1049-1056 (1996).|4. Rodgers, R.J., and Johnson, N.J. Behaviorally selective effects of neuroactive steroids on plus-maze anxiety in mice. Pharmacol. Biochem. Behav. 59(1), 221-232 (1998).

化学性质

Cas No. 567-02-2 SDF
别名 3ALPHA,21-二羟基-5ALPHA-孕甾-20-酮,THDOC
Canonical SMILES C[C@@]12[C@](CC[C@@H]2C(CO)=O)([H])[C@]3([H])CC[C@@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC1
分子式 C21H34O3 分子量 334.5
溶解度 DMSO: 100 mM,Ethanol: 100 mM 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.9895 mL 14.9477 mL 29.8954 mL
5 mM 0.5979 mL 2.9895 mL 5.9791 mL
10 mM 0.299 mL 1.4948 mL 2.9895 mL
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