Azapetine phosphate
Azapetine phosphate is an antagonist of α1-adrenoceptor, with an IC50 of 0.205 μM at rat α1-adrenoceptor and an IC50 of 1.3 μM at rat α2-adrenoceptor, and exhibits higher selectivity for α1-adrenoceptor than for α2-adrenoceptor. Azapetine phosphate functionally blocks postsynaptic α1-adrenoceptors, and at higher concentrations, it blocks presynaptic α2-adrenoceptors, central α-adrenoceptors, and H2 histamine receptors. Azapetine phosphate is used in related research on hypotension.
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- CAS. Nr.: 130-83-6
- Formel: C17H20NO4P
- Molecular Weight:333.32
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Platelet | IC50 |
28.9 μM
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Inhibition of epinephrine-induced aggregation of human platelets, with azapetine added 1 min before 3.0 μg/mL epinephrine and aggregation monitored for 10 min.
Inhibition of epinephrine-induced aggregation of human platelets, with azapetine added 1 min before 3.0 μg/mL epinephrine and aggregation monitored for 10 min.
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2869118 |
In Vitro
Azapetine (15 min) phosphate acts as an α1-adrenoceptor antagonist on isolated rat anococcygeus muscle with a pA2 value of 7.82[1].
Azapetine (10 min) phosphate acts as an α2-adrenoceptor antagonist on isolated rat vas deferens with a pA2 value of 6.43[1].
Azapetine (10 min) phosphate acts as an α2-adrenoceptor antagonist on isolated guinea-pig ileum (Clonidine (HY-12721)-induced twitch inhibition) with a pA2 value of 6.80[1].
Azapetine (10 min) phosphate acts as an α2-adrenoceptor antagonist on isolated guinea-pig ileum (Norepinephrine (HY-13715)-induced twitch inhibition) with a pA2 value of 6.70[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Azapetine (100 μg/kg; i.c.; single dose) phosphate produces a long-lasting central hypotensive effect in rabbits, and Clonidine does not induce further hypotension in Azapetine-pretreated animals[3].
Azapetine (200 μg/kg; i.c.; single dose) phosphate produces a long-lasting central hypotensive effect in dogs, and Clonidine still induces significant hypotension and bradycardia in Azapetine-pretreated animals[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:either sex, 200-300 g[3]
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Dosage:200 μg/kg
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Administration:i.c.; single dose
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Result:Induced a mean maximal hypotensive effect of 60 mmHg.
Reduced the mean blood pressure fall induced by clonidine from 54 mmHg to 30 mmHg.
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Animal Model:either sex, 2-3 kg[3]
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Dosage:100 μg/kg
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Administration:i.c.; single dose
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Result:Significantly reduced blood pressure, with mean blood pressure remaining at 75/47 mmHg 1 hour post-injection, which was significantly lower than baseline.
Prevented clonidine from producing additional hypotension.
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Animal Model:either sex, 7-12 kg[3]
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Dosage:200 μg/kg
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Administration:i.c.; single dose
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Result:Reduced blood pressure from 141/97 mmHg to 128/89 mmHg, with blood pressure remaining significantly lower than baseline 1 hour post-injection.
Did not prevent clonidine from inducing further decreases in blood pressure and heart rate that were not significantly different from changes seen in control dogs treated with clonidine alone.
Chemical Information
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CAS. Nr. 130-83-6
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Molecular Weight 333.32
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Formel C17H20NO4P
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SMILES
O=P(O)(O)O.C=CCN1CC2=C(C3=C(C1)C=CC=C3)C=CC=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Ishida Y, et al. Alpha-adrenolytic properties of apogalanthamine and azapetine analogs. Journal of pharmacobio-dynamics. 1985 Nov;8(11):917-23. [Content Brief]
[4]. Timmermans PB, et al. Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. Journal of medicinal chemistry. 1984 Apr;27(4):495-503. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Azapetine phosphate Related Classifications
HY-181635A Related Classifications
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