MDL-19744A
MDL-19744A is an orally active and selective α1-adrenergic receptor antagonist, with rat α1-adrenergic receptor IC50 of 8 nM. MDL-19744A increases renal blood flow, dose-related decreases mean arterial blood pressure, increases urinary sodium excretion, and mediates renal vasodilation. MDL-19744A can be used for the research of hypertension.
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- CAS No.: 97233-26-6
- Formule: C21H25NO3S
- Masse moléculaire:371.49
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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α1-adrenergic receptor |
MDL-19744A (Compound 1) potently and selectively inhibits α1-adrenergic receptor binding in rat cerebrocortex tissue, with an IC50 of 8 nM for α1 receptors[1].
MDL-19744A (30 min) potently antagonizes α1-adrenergic receptor-mediated vasoconstriction in isolated rabbit aortic strips, with a pA2 of 8.13[1].
MDL-19744A (3 μM) is inactive as a β-adrenergic receptor blocker in isolated guinea pig ventricles[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MDL-19744A (0.03-3 mg/kg; i.v.; single dose) produces decreases in mean arterial blood pressure in anesthetized normotensive dogs, with an ED15 for hypotension of 0.08 mg/kg and a maximal mean arterial blood pressure reduction of -47 mmHg at 1 mg/kg i.v[1].
MDL-19744A (0.01-1 mg/kg; i.v.; cumulative dose) produces dose-dependent increases in renal blood flow and increases in urinary sodium excretion in anesthetized normotensive dogs[1].
MDL-19744A (0.1-3 mg/kg; i.v.; single dose) selectively antagonizes α1-adrenergic receptors in pithed rats, shifting Phenylephrine (HY-B0769)-induced pressor responses at 0.1-1.0 mg/kg i.v. while only weakly affecting α2-mediated responses at 3.0 mg/kg i.v[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:spontaneously hypertensive rats (SHR) (conscious)[1]
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Dosage:30 mg/kg
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Administration:p.o.; single dose
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Result:Produced a maximal decrease in mean arterial blood pressure of -70 mmHg.
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Animal Model:normotensive dogs (anesthetized)[1]
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Dosage:0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg
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Administration:i.v.; cumulative dose
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Result:Produced a 9% increase in renal blood flow and a -5% change in mean arterial blood pressure at 0.01 mg/kg cumulative dose.
Produced a 17% increase in renal blood flow and a -9% change in mean arterial blood pressure at 0.03 mg/kg cumulative dose.
Produced a 27% increase in renal blood flow and a -15% change in mean arterial blood pressure at 0.1 mg/kg cumulative dose.
Produced a 34% increase in renal blood flow, a -23% change in mean arterial blood pressure, and increased urinary sodium excretion from a baseline of 42 to 104 µequiv/min at 0.3 mg/kg cumulative dose.
Produced a 42% increase in renal blood flow and a -32% change in mean arterial blood pressure at 1.0 mg/kg cumulative dose.
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Animal Model:rats[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg; 3 mg/kg
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Administration:i.v.; single dose
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Result:Shifted the Phenylephrine-induced diastolic blood pressure dose-response curve (DR2 = 0.07, 0.02 mg/kg) at doses of 0.1-1.0 mg/kg.
Weakly affected α2-mediated responses at 3.0 mg/kg i.v.
Chemical Information
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CAS No. 97233-26-6
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Masse moléculaire 371.49
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Formule C21H25NO3S
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SMILES
O=C1C2=C(SC(C)=C2)CC[C@H]1CN[C@@H]3[C@@H]([C@H](CC3)OC4=CC=CC=C4)O
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MDL-19744A Related Classifications
HY-183954 Related Classifications
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