Indiplon

Discontinued Product

3597 has been discontinued.

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说明: Positive allosteric modulator of GABAA; acts at benzodiazepine site
别名: NBI 34060
化学名: N-Methyl-N-[3-[3-[2-thienylcarbonyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide
纯度: ≥99% (HPLC)
说明书
引用文献 (2)
评论
文献 (2)

生物活性 for Indiplon

Potent GABAA receptor positive allosteric modulator that acts at the benzodiazepine site (Ki values are 1.2 and 1.7 nM in rat frontal cortex and cerebellum respectively). Displays ~ 10-fold selectivity for α1 subunit-containing receptors (EC50 values are 2.6, 24, 60 and 77 nM for α1β2γ2, α2β2γ2, α3β3γ2 and α5β2γ2 receptors respectively). Exhibits sedative, hypnotic, anxiolytic and anticonvulsant activity in vivo and is orally active.

技术数据 for Indiplon

分子量 376.43
公式 C20H16N4O2S
储存 Store at +4°C
纯度 ≥99% (HPLC)
CAS Number 325715-02-4
PubChem ID 6450813
InChI Key CBIAWPMZSFFRGN-UHFFFAOYSA-N
Smiles CN(C(C)=O)C1=CC=CC(C3=CC=NC2=C(C(C4=CC=CS4)=O)C=NN23)=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

参考文献 for Indiplon

参考文献是支持产品生物活性的出版物。

Sullivan et al (2004) Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor. J.Pharmacol.Exp.Ther. 311 537 PMID: 15256540

Foster et al (2004) In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic. J.Pharmacol.Exp.Ther. 311 547 PMID: 15256538

Petroski et al (2006) Indiplon is a high-affinity positive allosteric modulator with selectivity for α1 subunit-containing GABAA receptors. J.Pharmacol.Exp.Ther. 317 369 PMID: 16399882

Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem.Pharmacol. 158 339 PMID: 30121248

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关键词: Indiplon, Indiplon supplier, Subtype-selective, GABAA, receptor, positive, allosteric, modulators, Receptors, NBI34060, PAM, NBI, 34060, 3597, Tocris Bioscience

2 篇 Indiplon 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Indiplon 的部分引用包括:

Cass et al (2014) CB1 cannabinoid receptor stimulation during adolescence impairs the maturation of GABA function in the adult rat prefrontal cortex. Mol Psychiatry 19 536 PMID: 24589887

Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem Pharmacol 158 339 PMID: 30121248


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该领域的文献

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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