2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. 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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RO5126946

RO5126946 Chemical Structure

CAS No. : 1137233-79-4

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Description

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[1].

In Vitro

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.

RO5126946 Related Antibodies

Cell Viability Assay[1]

Cell Line: rat hippocampal neurons
Concentration: 0.3-1 μM
Incubation Time: /
Result: Couldn't reactivate fully desensitized α7 nAChRs in cultured rat hippocampal neurons.
Parmacokinetics
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 %
In Vivo

RO5126946 (3-30 mg/kg; p.o.; single dose 60 minutes before training) reverses scopolamine-induced associative memory deficits in rats, with 10 and 30 mg/kg fully restoring freezing behavior to vehicle levels[1].
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.

Animal Model: Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose 60 minutes before training
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.
Animal Model: Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
Dosage: 1 mg/kg
Administration: p.o.; single dose 60 minutes before training
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.
Animal Model: Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)[1]
Dosage: 3 mg/kg
Administration: p.o.; single dose 60 minutes before training
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.
Molecular Weight

408.90

Formula

C19H21ClN2O4S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RO5126946 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RO51269461137233-79-4RO 5126946RO-5126946nAChRNicotinic acetylcholine receptorsspontaneous inhibitory postsynaptic currentHEK293 cellsrat hippocampal neurons5-hydroxytryptamine 3 receptorsXenopus oocytesGABAergic responsesInhibitorinhibitorinhibit

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