Atipamezole

Alias: Antisedan; MPV-1248; MPV1248; MPV 1248
Cat No.:V2590 Purity: ≥98%
Atipamezole (Antisedan, MPV-1248)is a synthetic α2 adrenergic receptor antagonistwith a Ki of 1.6 nM.
Atipamezole Chemical Structure CAS No.: 104054-27-5
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
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Other Forms of Atipamezole:

  • Atipamezole HCl (MPV-1248)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Atipamezole (Antisedan, MPV-1248) is a synthetic α2 adrenergic receptor antagonist with a Ki of 1.6 nM. It has also been studied as a possible anti-Parkinsonian medication in humans. Atipamezole, an alpha2-adrenoceptor antagonist, was a strong inhibitor of aldosterone release (with a 10-1000 nM range). Alpha 2/alpha 1 selectivity ratio of 8526 was found for atipamezole in receptor binding studies [(3H]-clonidine and [3H]-prazosin displacement], whereas ratios of 27 and 40 were observed for idazoxan and yohimbine, respectively. In comparison to reference compounds, atipamezole exhibited an approximately 100-fold greater affinity for alpha 2-adrenoceptors.

Biological Activity I Assay Protocols (From Reference)
Targets
α2 adrenergic receptor
ln Vitro

In vitro activity: Tipazine has a α21 selectivity ratio and a much higher affinity for α2-adrenoceptors than yohimbine. The α2-adrenoceptor subtypes are not selectively affected by atifamezole. For 5-HT1, 5-HT2, and I2 binding sites, its affinity is negligible[1].

ln Vivo
Atipamezole is well tolerated in rodents. Atipamezole (0.01–1 mg/kg, i.v.) has relatively mild cardiovascular effects in rats that have been anesthetized and have normal blood pressure. Veterinarians often administer atipamezole to animals to wake them from sedation or anesthesia. In rats and monkeys, atipamezole promotes sexual behavior. Atipamezole blocks noradrenergic feedback inhibition of pain, hence increasing pain-related responses in animals with sustained nociception. While it may not always improve short-term working memory, atipamezole at low dosages improves planning, learning, recall, attentiveness, and selective attention in experimental animals[1].
Enzyme Assay
Atipamezole Hcl(MPV1248 Hcl) exhibits high affinity and selectivity for the alpha 2-receptor as an antagonist of alpha-adrenoceptors.
Animal Protocol
i.v. injection of the drug (100 microCi/animal, rat tail vein administration)
Rats
References

[1]. Pharmacological properties, central nervous system effects, and potential therapeutic applicationsof atipamezole, a selective alpha2-adrenoceptor antagonist. CNS Drug Rev. 2005 Autumn;11(3):273-88.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C14H16N2
Molecular Weight
212.29
Exact Mass
212.13
Elemental Analysis
C, 79.21; H, 7.60; N, 13.20
CAS #
104054-27-5
Appearance
Solid powder
SMILES
CCC1(CC2=CC=CC=C2C1)C3=CN=CN3
InChi Key
HSWPZIDYAHLZDD-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H16N2/c1-2-14(13-9-15-10-16-13)7-11-5-3-4-6-12(11)8-14/h3-6,9-10H,2,7-8H2,1H3,(H,15,16)
Chemical Name
5-(2-ethyl-1,3-dihydroinden-2-yl)-1H-imidazole
Synonyms
Antisedan; MPV-1248; MPV1248; MPV 1248
HS Tariff Code
2934.99.03.00
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~42 mg/mL (~197.8 mM)
Water: <1 mg/mL
Ethanol: ~42 mg/mL (~197.8 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.7105 mL 23.5527 mL 47.1054 mL
5 mM 0.9421 mL 4.7105 mL 9.4211 mL
10 mM 0.4711 mL 2.3553 mL 4.7105 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in 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.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01435213 Completed Drug: Atipamezole
Drug: Atomoxetine
Healthy University of Turku September 2011 Phase 1
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