TC-2559
TC-2559 is an orally active, selective central nervous system Nicotinic acetylcholine receptor agonist with a Ki value of 5 nM. TC-2559 activates central nervous system receptors selectively over peripheral nervous system receptors. TC-2559 improves scopolamine (HY-N0296)-induced cognitive impairment and enhances radial arm maze performance. TC-2559 can be used in the research of neurodegenerative diseases.
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- No. CAS: 326924-19-0
- Fòrmula: C12H18N2O·1/2C6H10O8
- Peso molecular:311.30
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Almacenamiento:
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Actividad biológica
Descripciòn
In Vitro
TC-2559 binds with high affinity to nicotinic acetylcholine receptors in rat brain cortex membranes, with a Ki of 5.5 nM[1].
TC-2559 (0.01-100 μM) potently and efficaciously stimulates dopamine release from rat striatal synaptosomes (EC50 = 203 nM) and induces significantly less residual inhibition of dopamine release than nicotine following pre-incubation[1].
TC-2559 (0.01-90 μM) potently stimulates 86Rb+ efflux from rat thalamic synaptosomes, with an EC50 of 367 nM and efficacy comparable to nicotine[1].
TC-2559 (10 μM; 2 h) significantly protects cultured fetal rat brain cells from glutamate-induced neurotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
TC-2559 (1-10 μmol/kg; p.o.; single administration or daily administration for 6 consecutive days) enhances radial arm maze working memory performance in male Sprague-Dawley rats (acute administration), improves their reference memory at an acute dose of 1 μmol/kg, and repeated oral administration (1-6 μmol/kg) further enhances their working memory performance[1].
TC-2559 (1-10 μmol/kg; subcutaneous injection; single administration) induces dose-dependent hypoactivity in male Sprague-Dawley rats. A dose of 1 μmol/kg produces a persistent effect, and both 1 μmol/kg and 10 μmol/kg doses significantly reduce locomotor activity over 30 minutes[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, 200-350 g, scopolamine-induced amnesia)[1]
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Dosage:0.6 μmol/kg; 1 μmol/kg; 3 μmol/kg; 6 μmol/kg; 10 μmol/kg
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Administration:s.c.; single dose
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Result:Significantly attenuated scopolamine-induced reduction in step-through retention latencies at 3 μmol/kg (median latency 88.7 s) and 6 μmol/kg (median latency 105.7 s).
Did not produce statistically significant attenuation at 0.6 μmol/kg, 1 μmol/kg, and 10 μmol/kg compared to scopolamine alone.
Chemical Information
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No. CAS 326924-19-0
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Peso molecular 311.30
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Fòrmula C12H18N2O·1/2C6H10O8
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SMILES
OC([C@@H](O)[C@H](O)[C@H](O)[C@@H](O)C(O)=O)=O.CNCC/C=C/C1=CN=CC(OCC)=C1.[1/2]
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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.
Protocolo
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TC-2559 Related Classifications
HY-183204 Related Classifications
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Keywords
- TC-2559
- 326924-19-0
- TC2559
- TC 2559
- nAChR
- scopolamine-induced cognitive deficits
- TE671/RD cells
- CNS nicotinic acetylcholine receptor
- PNS receptors
- dopamine
- ganglion-type nicotinic acetylcholine receptors
- muscle-type nicotinic acetylcholine receptors
- glutamate-induced neurotoxicity
- PC12 cells
- radial arm maze
- Inhibitor
- inhibitor
- inhibit