CSP-2503
CSP-2503 is a potent and selective 5-HT1A receptor agonist , with an EC50 of 0.15 μM and a Ki of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (Ki > 1000 nM), 5-HT4 receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders.
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- No. CAS: 581813-10-7
- Fòrmula: C22H26N4O2
- Peso molecular:378.48
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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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
5-HT1A Receptor 0.15 μM (EC50) |
5-HT1A Receptor 4.1 nM (Ki) |
5-HT2A Receptor 13.5 nM (Ki) |
5-HT3 Receptor 8.9 nM (Ki) |
5-HT4 Receptor >10000 nM (Ki) |
5-HT7 Receptor 100.9 nM (Ki) |
α1-adrenergic receptor >1000 nM (Ki) |
serotonin transporter 976.3 nM (Ki) |
benzodiazepine receptor >10000 nM (Ki) |
Dopamine D2 receptor 192.1 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HeLa | EC50 |
0.15 μM
Compound: 9 (S)
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Inhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cells
Inhibition of forskolin-induced increase in cAMP in human 5-hydroxytryptamine 1A receptor expressed HeLa cells
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[PMID: 15801844] |
In Vitro
In Vivo
CSP-2503 (2.5-20 mg/kg; s.c.; single dose) acts as a somatodendritic 5-HT1A receptor agonist in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:10 mg/kg
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Administration:s.c.; single dose
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Result:Increased time spent in the lit area to 155.4 seconds compared to 83 seconds in vehicle-treated mice.
Increased time spent in the lit area by 87.2%.
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Animal Model:Mice hypothermia model[1]
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Dosage:2.5, 5, 10, 20 mg/kg
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Administration:s.c.; single dose
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Result:Induced a dose-related decrease in rectal temperature.
Decreased the 5-HIAA/5-HT ratio in mouse hypothalamus.
Chemical Information
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No. CAS 581813-10-7
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Peso molecular 378.48
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Fòrmula C22H26N4O2
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SMILES
C(N1CCN(C=2C3=C(C=CC2)C=CC=C3)CC1)N4C(=O)[C@]5(N(C(=O)C4)CCC5)[H]
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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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Protocol for Elevated Plus Maze Test
The Elevated Plus Maze is a rodent anxiety-like behavior assay based on the conflict between spontaneous exploration and avoidance of open, elevated, exposed spaces. The apparatus contains two open arms and two closed arms arranged in a plus shape, and rodents normally spend more time in closed arms than open arms. The assay readout is generated by recording arm entries, time spent in open and closed arms, and related exploratory behaviors. Increased open-arm time or open-arm entries is commonly interpreted as reduced anxiety-like behavior, whereas reduced open-arm exploration is interpreted as increased anxiety-like behavior.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CSP-2503 Related Classifications
HY-180372 Related Classifications
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Keywords
- CSP-2503
- 581813-10-7
- CSP2503
- CSP 2503
- 5-HT Receptor
- Adrenergic Receptor
- GABA Receptor
- Serotonin Transporter
- Dopamine Receptor
- Mice
- serotonin receptor subtypes
- postsynaptic sites
- 5-HT1A receptor
- 5-HT?A receptors
- somatodendritic sites
- dopamine D? receptors
- α?-adrenergic receptors
- benzodiazepine receptors
- forskolin-induced cAMP increase
- Anxiety model
- hypothalamic 5-HIAA/5-HT ratio
- 5-HT? receptors
- anxiolytic properties
- serotonin transporter
- anxiety-related disorders
- 5-HT neuronal activity modulation model
- Somatodendritic 5-HT?A receptor activation model
- Inhibitor
- inhibitor
- inhibit