Tasipimidine
Tasipimidine is an orally active and selective α2A-adrenoceptor agonist with a pEC50 of 7.57 for human α2A-adrenoceptors and an EC50 of 5.7 nM for rat α2-adrenoceptor. Tasipimidine can be utilized in research related to situational anxiety and fear.
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- No. CAS: 1465908-70-6
- Fòrmula: C13H16N2O2
- Peso molecular:232.28
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
human α2A-adrenoceptor 7.57 (pEC50) |
rat α2-adrenergic receptor 5.7 nM (EC50) |
In Vivo
Tasipimidine (300-1000 μg/kg; subcutaneous injection; single dose) reduces the amplitude of the acoustic startle reflex in rats, with onset within 20 minutes, peak effect at 1 hour, and duration of at least 2 hours[1].
Tasipimidine (10-30 μg/kg; oral administration; total 3 treatment cycles) has an improving effect on separation anxiety in dogs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Non-habituated mice[1]
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Dosage:Subcutaneous injection: 10, 30 and 100 μg/kg
Oral administration: 900 and 3000 μg/kg -
Administration:Single dose
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Result:Significantly reduced the activity count at doses of 30 μg/kg and higher doses, with 100 μg/kg showing a more pronounced effect by subcutaneous injection.
Significantly decreased the spontaneous locomotor activity of 3.0 mg/kg, while 0.9 mg/kg had no effect by oral administration.
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Animal Model:Clinically healthy privately-owned dogs with a history of separation anxiety[2]
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Dosage:10 and 30 μg/kg
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Administration:Oral administration; three 4-day treatment periods in randomized order each followed by a 3-day washout
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Result:Had a statistically significant treatment effect.
Led to more positive owner ratings, significantly reduced destructive/rearranging behavior and vocalization at dose of 30 μg/kg. Most dogs remained fully responsive and able to walk normally, with no serious adverse events reported.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1465908-70-6
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Peso molecular 232.28
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Fòrmula C13H16N2O2
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SMILES
COC1=C2CCOC(C3=NCCN3)C2=CC=C1
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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.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tasipimidine Related Classifications
HY-109075 Related Classifications
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