1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor
  3. L-838417

L-838417 

目录号: HY-W009009
产品使用指南

L-838417 是GABAA 受体 α2, α3 和 α5 亚型的选择性部分激动剂,是 α1 亚型的拮抗剂,其对 α1β3γ2、α2β3γ2、α3β3γ2、α4β3γ2、α5β3γ2 和 α6β3γ2 的Ki 值分别为 0.79 nM、0.67 nM、1.67 nM、267 nM、2.25 nM 和 2183 nM。

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L-838417 Chemical Structure

L-838417 Chemical Structure

CAS No. : 286456-42-6

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Description

L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2[1].

IC50 & Target

Ki: 0.79 nM (α1β3γ2), 0.67 nM (α2β3γ2), 1.67 nM (α3β3γ2), 267 nM (α4β3γ2), 2.25 nM (α5β3γ2) and 2183 nM (α6β3γ2)[1].

In Vivo

L-838417 (1.0 mg/kg) produces anxiolytic effects in adult rat, as indexed by a transformation of social avoidance into preference and an increase in social investigation[2].
L-838417 (2.0 mg/kg) eliminates social avoidance, but has no anxiolytic effects on social investigation[2].
L-838417 (0.5 mg/kg) reverses the anxiogenic effects of prior stress regardless of age, but with doses ≥ 1 mg/kg decreases social investigation, an effect possibly due in part to locomotor-impairing effects of this compound[2].

Animal Model: Male and female adolescent and adult Sprague–Dawley rats[2].
Dosage: 0, 0.5, 1.0, 2.0, or 4.0 mg/kg.
Administration: IP.
Result: Adolescents required a higher dose (2 mg/kg) to attenuate their social avoidance.
The lowest dose of 0.5 mg/kg was sufficient to reverse the anxiogenic effects of repeated restraint as reflected by a significant increase in the coefficient relative to vehicle-treated animals.
Molecular Weight

399.41

Formula

C₁₉H₁₉F₂N₇O

CAS No.

286456-42-6

SMILES

CN1N=CN=C1COC2=NN3C(C=C2C(C)(C)C)=NN=C3C4=CC(F)=CC=C4F

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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

L-838417L838417L 838417GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorsocialavoidanceanxiogeniceffectsInhibitorinhibitorinhibit

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L-838417
目录号:
HY-W009009
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