1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. Tracazolate hydrochloride

Tracazolate hydrochloride (Synonyms: ICI 136753 hydrochloride)

目录号: HY-B1803A
产品使用指南

Tracazolate hydrochloride (ICI 136753 hydrochloride) 是一种有效的 GABAA 受体调节剂。Tracazolate hydrochloride 浓度依赖性地增强 α1β1γ2s (EC50=13.2μM) 和 α1β3γ2 (EC50=1.5 μM)。Tracazolate hydrochloride 的效力 (EC50) 是由受体复合物中的第三亚基 (γ1-3, δ, ε) 的性质决定。Tracazolate hydrochloride 具有抗焦虑和抗惊厥活性。

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Tracazolate hydrochloride Chemical Structure

Tracazolate hydrochloride Chemical Structure

CAS No. : 1135210-68-2

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Description

Tracazolate hydrochloride (ICI 136753 hydrochloride) is a potent GABAA receptor modulator. Tracazolate hydrochloride potentiates α1β1γ2s (EC50=13.2 μM) and α1β3γ2 (EC50=1.5 μM) in a concentration-dependent manner. Tracazolate hydrochloride has the potency (EC50) is determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity[1][2].

IC50 & Target

GABAA[1]

In Vitro

Tracazolate hydrochloride (ICI 136753 hydrochloride) inhibits α1β1ε and α1β3ε GABAA receptors with IC50s of 4.0 μM, 1.2 μM, respectively. Replacement of Ser265 within the β1 subunit with Asn (the β3 counterpart) increases the sensitivity of tracazolate, whereas the opposite mutation (Asnβ3 to Ser) decreases the sensitivity to Tracazolate[1].
Tracazolate hydrochloride (10 μM) increases the maximum current amplitude and enhances the sensitivity of α1β2δ-containing GABAA receptors in oocytes[2].

Molecular Weight

340.85

Formula

C₁₆H₂₅ClN₄O₂

CAS No.

1135210-68-2

中文名称

盐酸西卡唑酯;盐酸曲卡唑酯

SMILES

O=C(C1=C(C)N=C(N(CC)N=C2)C2=C1NCCCC)OCC.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

TracazolateICI 136753ICI136753ICI-136753GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorGABAAα1β1γ2sα1β3γ2γ1-3δεanxiolytic anticonvulsantα1β1εα1β3εSer265AsnAsnβ3α1β2δInhibitorinhibitorinhibit

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Tracazolate hydrochloride
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