RO5126946
RO5126946 is a selective, orally active α7 nAChR allosteric potentiator with EC50 values of 0.06 μM (hα7 nAChR) and 770 nM (α7 nAChR), and it crosses the blood-brain barrier. RO5126946 enhances synaptic transmission and positively modulates GABA-ergic responses by increasing peak current, slowing current decay, and elevating the frequency of spontaneous inhibitory postsynaptic currents, without affecting the recovery of receptors from the desensitized state. RO5126946 not only enhances subthreshold nicotine effects and improves associative learning, but also does not interfere with the original pro-cognitive effects of nicotine. RO5126946 can be used to study cognitive impairments associated with diseases such as Alzheimer's disease and schizophrenia.
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- No. CAS: 1137233-79-4
- Fòrmula: C19H21ClN2O4S
- Peso molecular:408.90
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
RO5126946 (0.01-3 μM) potently potentiates nicotine-evoked currents in cultured rat hippocampal neurons via an α7 nAChR-dependent mechanism, with an EC50 of 7.7 ± 2.0 × 10-7 M and maximum potentiation of 2800% ± 730%, and this effect is independent of glutamate or GABAₐ receptor activity[1].
RO5126946 (0.3-1 μM) does not reactivate fully desensitized α7 nAChRs in cultured rat hippocampal neurons[1].
RO5126946 (0.3 μM; ~5 min) potentiates nicotine-induced increases in spontaneous inhibitory postsynaptic current frequency in cultured rat hippocampal neurons, an effect dependent on action potential propagation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:rat hippocampal neurons
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Concentration:0.3-1 μM
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Incubation Time:/
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Result:Couldn't reactivate fully desensitized α7 nAChRs in cultured rat hippocampal neurons.
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC | Bioavailability |
|---|---|---|---|---|---|---|---|
| Rat[1] | 3 mg/kg | i.v. | 3490 ± 1414 ng/mL | / | 4.90 h | 11,600 ng·h/mL | / |
| Rat[1] | 1 mg/kg | p.o. | 214 ± 81 ng/mL | 2.5 h | 5.19 h | 2280 ng·h/mL | ~100 % |
| Rat[1] | 3 mg/kg | p.o. | 1050 ± 31 ng/mL | 4.67 h | 4.00 h | 11,800 ng·h/mL | ~100 % |
| Rat[1] | 10 mg/kg | p.o. | 3470 ± 357 ng/mL | 3.33 h | 2.61 h | 25,900 ng·h/mL | ~100 % |
RO5126946 (1 mg/kg; p.o.; single dose 60 minutes before training) potentiates the procognitive effects of a subthreshold dose of nicotine to reverse scopolamine-induced associative memory deficits in rats[1].
RO5126946 (3 mg/kg; p.o.; single dose 60 minutes before training) reverses scopolamine-induced associative memory deficits in rats and does not interfere with the procognitive effects of an effective dose of nicotine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose 60 minutes before training
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Result:Significantly reversed scopolamine-induced deficits in freezing behavior.
Resulted in a freezing percentage significantly different from both vehicle and scopolamine groups at 3 mg/kg.
Restored freezing to levels statistically indistinguishable from vehicle-treated rats at 10 and 30 mg/kg.
Showed mean pre-tone freezing <4% across all groups.
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Animal Model:Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
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Dosage:1 mg/kg
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Administration:p.o.; single dose 60 minutes before training
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Result:Did not reverse scopolamine-induced memory deficits when administered alone.
Produced a significant reversal of scopolamine-induced memory deficits when coadministered with a subthreshold dose of nicotine.
Showed mean pre-tone freezing <2% across all groups.
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Animal Model:Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
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Dosage:3 mg/kg
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Administration:p.o.; single dose 60 minutes before training
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Result:Significantly reversed scopolamine-induced memory deficits when administered alone.
Maintained procognitive effect when coadministered with an effective dose of nicotine.
Showed mean pre-tone freezing <3% across all groups.
Chemical Information
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No. CAS 1137233-79-4
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Peso molecular 408.90
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Fòrmula C19H21ClN2O4S
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SMILES
N(C(=O)C1=C(OC)C=CC(Cl)=C1)[C@H]2[C@@H](C2(C)C)C3=CC=C(S(N)(=O)=O)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RO5126946 Related Classifications
HY-124057 Related Classifications
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