Home Tools

Sarizotan

Catalog No. T40439 CAS 351862-32-3

Synonyms: EMD 128130

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Sarizotan, CAS 351862-32-3

Please contact us for prices and availability for the specification of product you are interested at.
Product consultation

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .
Targets&IC50	5-HT2A receptor:587 nM (IC50, human, antagonist site), 5-HT2A receptor:960 nM (IC50, rat, agonist site), 5-HT2C receptor:800 nM (IC50, pig), 5-HT6 receptor:3300 nM (IC50, human), 5-HT7 receptor:10 nM (IC50, human), 5-HT3 receptor:3500 nM (IC50, NG 108 cells), D3 receptor:6.8 nM (IC50, human), 5-HT2B receptor:108 nM (IC50, human), 5-HT1A receptor:0.1 nM (IC50, human), 5-HT1A receptor:6.5 nM (IC50, rat), 5-HT1B receptor:600 nM (IC50, rat), 5-HT5A receptor:313 nM (IC50, human), D 4.2:2.4 nM (IC50, human), D2 receptor:15.1 nM (IC50, rat), D2 receptor:17 nM (IC50, human), 5-HT1D receptor:500 nM (IC50, calf)
In vitro	Sarizotan exhibits concentration-dependent inhibition of electrically-induced contractions, achieving an inhibition concentration (IC50) value of 150 nM, with a maximum efficacy (E max) of 40% observed at a concentration of 1 mM[1].
In vivo	Sarizotan administered at a dose of 10 mg/kg orally, notably reduces 5-HT levels in the striatum and its metabolite 5-HIAA in the frontal cortex and hippocampus, while substantially enhancing DA metabolites DOPAC and HVA in the same regions[1]. This compounds symbolizes a novel strategy in addressing extrapyramidal motor disorders such as l-DOPA-induced dyskinesia in Parkinson's disease[1]. Furthermore, in a study involving male Sprague-Dawley rats (weighing 220-240 g and showing a strong rotational response), local administration of Sarizotan at doses of 10 ng and 1 μg effectively mitigated levodopa-induced dyskinesias in 6-OHDA-lesioned rats[2]. These rats received the compound via an injection cannula placed through the STN (V -8.4 mm from skull), utilizing a microinfusion pump over a period of 22 days. Notably, on the 23rd day, a significant reduction in total dyskinesia scores was observed in levodopa-treated rats at the higher doses of Sarizotan (10 ng and 1 μg) compared to those treated with levodopa alone (p<0.05, p<0.01, respectively).

Synonyms	EMD 128130
Molecular Weight	348.421
Formula	C22H21FN2O
CAS No.	351862-32-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. G D Bartoszyk, et al. Sarizotan, a Serotonin 5-HT1A Receptor Agonist and Dopamine Receptor Ligand. J Neural Transm (Vienna). 2004 Feb;111(2):113-26. 2. C Marin, et al. Local Administration of Sarizotan Into the Subthalamic Nucleus Attenuates Levodopa-Induced Dyskinesias in 6-OHDA-lesioned Rats. Psychopharmacology (Berl). 2009 Jun;204(2):241-50.

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Sarizotan 351862-32-3 EMD128130 EMD 128130 EMD-128130 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.