Sarizotan - 10mM in DMSO , CAS No.351862-32-3

CAS: 351862-32-3 Cat. No.: S656130 Formula: C₂₂H₂₁FN₂O Peso molecolare: 348.41 PubChem CID: 6918388

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Sarizotan (EMD 128130) is an orally active serotonin 5-HT 1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC 50 values of 6.5 nM (rat 5-HT 1A ), 0.1 nM (human 5-HT 1A ), 15.1 nM (rat D 2 ), 17 nM (human D 2 ), 6.8 nM (human D 3 ) and 2.4 nM (human D 4.2 ), respectively

In Vitro

Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC 50 value of 150 nM (E max 40% at 1 mM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Sarizotan (3, 10 mg/kg, po) at the higher dose slightly decreases 5-HT in the striatum and its metabolite 5-HIAA in frontal cortex and hippocampus. Sarizotan (10 mg/kg, po) substantially increases the DA metabolites DOPAC and HVA in the striatum and frontal cortex . Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease . Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response). Dosage: 1 ng, 10 ng and 1 μg in 0.3 μL solution. Administration: Administered via an injection cannula inserted to the guide cannula through the STN (V -8.4 mm from skull) with the injection cannula connected to a 10-μL syringe and mounted on a microinfusion pump for 22 consecutive days. Result: On day 23, the subthalamic administration of Sarizotan at the higher doses tested (10 ng and 1 μg) significantly decreased the total dyskinesia score in levodopa-treated rats in comparison with the rats treated only with levodopa (p<0.05, p<0.01, respectively).

IC50& Target:5-HT 1A Receptor 6.5 nM (IC 50 , rat) 5-HT 1A Receptor 0.1 nM (IC 50 , human) rD 2 Receptor 15.1 nM (IC 50 , rat) D 3 Receptor 6.8 nM (IC 50 , human) 5-HT 1B Receptor 600 nM (IC 50 , rat) 5-HT 1D Receptor 500 nM (IC 50 , calf) 5-HT 2A Receptor 960 nM (IC 50 , rat, agonist site) 5-HT 2A Receptor 587 nM (IC 50 , human, antagonist site) 5-HT 2B Receptor 108 nM (IC 50 , human) 5-HT 2C Receptor 800 nM (IC 50 , pig) 5-HT 3 Receptor 3500 nM (IC 50 , NG 108 cells) 5-HT 5A Receptor 313 nM (IC 50 , human) 5-HT 6 Receptor 3300 nM (IC 50 , human) 5-HT 7 Receptor 10 nM (IC 50 , human) hD 4.2 Receptor 2.4 nM (IC 50 ) hD 2 Receptor 17 nM (IC 50 )

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

Sarizotan (EMD 128130) is an orally active serotonin 5-HT 1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC 50 values of 6.5 nM (rat 5-HT 1A ), 0.1 nM (human 5-HT 1A ), 15.1 nM (rat D 2 ), 17 nM (human D 2 ), 6.8 nM (human D 3

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Nomi e identificatori

• Isomeri SMILES: C1CC2=CC=CC=C2O[C@H]1CNCC3=CC(=CN=C3)C4=CC=C(C=C4)F
• PubChem CID: 6918388
• Peso molecolare: 348.41

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 351862-32-3, the molecular formula is C22H21FN2O, and the molecular weight is 348.41 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.