|1-((3R,5S,8R,9S,10S,13S,14S,17S)-3-羟基-3,10,13-三甲基十六氢-1H-环戊二烯并[a]菲-17-基)乙酮|CsnPharm

CAS No.: 38398-32-2

加奈索酮 Catalog No. CSN25409

Synonyms: CCD 1042;C1042

Ganaxolone, also known as CCD 1042 and C1042, is a CNS-selective GABAA modulator that acts on well-characterized targets in the brain known to have anxiolytic and anticonvulsant effects. Ganaxolone protects against seizures in diverse animal models, including the pentylenetetrazol, 6 Hz and amygdala kindling models. Ganaxolone is a positive allosteric modulator of the action of the GABAA receptor and, unlike benzodiazepines, there does not appear to be tolerance to the anticonvulsant effects of ganaxolone.

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技术信息

生物活性

描述Ganaxolone (3alpha-hydroxy-3beta-methyl-5alpha-pregnan-20-one) (GNX) is the 3beta-methylated synthetic analog of allopregnanolone; it belongs to a class of compounds referred to as neurosteroids. GNX is an allosteric modulator of GABA(A) receptors acting through binding sites which are distinct from the benzodiazepine binding site. It has activity in a broad range of animal models of epilepsy. GNX has been shown to be well tolerated in adults and children. In early phase II studies, GNX has been shown to have activity in adult patients with partial-onset seizures and epileptic children with history of infantile spasms^[1]. Ganaxolone, a GABAA agonist neurosteroid, as a novel neonatal therapy. It is likely to prevent or reduce the incidence of the enduring disabilities associated with preterm birth, cerebral palsy, and epilepsy. Ganaxolone is an ideal anti-seizure treatment because it can be safely used prospectively, with minimal or no adverse effects on the neonatal brain^[2]. Allopregnanolone and ganaxolone (each at 3 mg/kg) terminated status epilepticus (SE) in, respectively, 92% and 75% of animals, and prevented mortality in 85% and 50% of animals; the mean times to termination of behavioral seizures were, respectively, 172 ± 16 and 447 ± 52 seconds. Allopregnanolone and ganaxolone are effective in the treatment of TETS-induced (tetramethylenedisulfotetramine) SE when administered by the intramuscular route^[3]. There is no significant differences between the effects of ganaxolone and placebo on Clinician Administered PTSD Symptom (CAPS) scores, global well-being, negative mood, or sleep. Dropout rates did not differ between groups, and ganaxolone was generally well tolerated^[4].

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0073 mL
- 15.0367 mL
- 30.0734 mL
- 5 mM
- 0.6015 mL
- 3.0073 mL
- 6.0147 mL
- 10 mM
- 0.3007 mL
- 1.5037 mL
- 3.0073 mL

技术信息

CAS号	38398-32-2	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C22H36O2	运输	蓝冰
分子量	332.52	别名	CCD 1042;C1042

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