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Art. -Nr.: HY-180372

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CSP-2503

CSP-2503 is a potent and selective 5-HT_1A receptor agonist , with an EC₅₀ of 0.15 μM and a K_i of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (K_i > 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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 581813-10-7
Formel: C₂₂H₂₆N₄O₂
Molecular Weight:378.48

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

CSP-2503 Chemical Structure

CAS. Nr.: 581813-10-7

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Preis

Verfügbarkeit

Menge

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Protokoll (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

5-HT_1A Receptor

0.15 μM (EC₅₀)

5-HT_1A Receptor

4.1 nM (Ki)

5-HT_2A 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)

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen :

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	EC₅₀	0.15 μM Compound: 9 (S)	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	[PMID: 15801844]

In Vitro

CSP-2503 inhibits Forskolin (HY-15371)-induced cAMP increase in a dose-dependent manner with an EC₅₀ of 0.15 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

CSP-2503 (10 mg/kg; s.c.; single dose) exhibits anxiolytic activity in mice^[1].
CSP-2503 (2.5-20 mg/kg; s.c.; single dose) acts as a somatodendritic 5-HT_1A receptor agonist in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mice^[1]
Dosage:

10 mg/kg
Administration:

s.c.; single dose
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%.

Animal Model:

Mice hypothermia model^[1]
Dosage:

2.5, 5, 10, 20 mg/kg
Administration:

s.c.; single dose
Result:

Induced a dose-related decrease in rectal temperature.
Decreased the 5-HIAA/5-HT ratio in mouse hypothalamus.

Chemical Information

CAS. Nr. 581813-10-7
Molecular Weight 378.48
Formel C₂₂H₂₆N₄O₂
SMILES

C(N1CCN(C=2C3=C(C=CC2)C=CC=C3)CC1)N4C(=O)[C@]5(N(C(=O)C4)CCC5)[H]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Protokoll

All Animals and Diseases

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. López-Rodríguez ML, et al. Design and synthesis of S-(-)-2-[[4-(napht-1-yl)piperazin-1-yl]methyl]-1,4-dioxoperhydropyrrolo[1,2-a]pyrazine (CSP-2503) using computational simulation. A 5-HT1A receptor agonist. Bioorg Med Chem Lett. 2003;13(8):1429-1432. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protokoll
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
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CSP-2503

Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen