Azapetine
Azapetine 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 functionally blocks postsynaptic α1-adrenoceptors, and at higher concentrations, it blocks presynaptic α2-adrenoceptors, central α-adrenoceptors, and H2 histamine receptors. Azapetine is used in related research on hypotension.
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- CAS No.: 146-36-1
- Formule: C17H17N
- Masse moléculaire:235.32
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
In Vitro
Azapetine (15 min) acts as an α1-adrenoceptor antagonist on isolated rat anococcygeus muscle with a pA2 value of 7.82[1].
Azapetine (10 min) acts as an α2-adrenoceptor antagonist on isolated rat vas deferens with a pA2 value of 6.43[1].
Azapetine (10 min) 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) 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) 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) 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 No. 146-36-1
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Masse moléculaire 235.32
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Formule C17H17N
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SMILES
C=CCN1CC2=C(C3=C(C1)C=CC=C3)C=CC=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Azapetine Related Classifications
HY-181635 Related Classifications
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