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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 97233-26-6
- Fòrmula: C21H25NO3S
- Peso molecular:371.49
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas Adrenergic Receptor
More
Actividad biológica
|
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.
-
Animal Model:spontaneously hypertensive rats (SHR) (conscious)[1]
-
Dosage:30 mg/kg
-
Administration:p.o.; single dose
-
Result:Produced a maximal decrease in mean arterial blood pressure of -70 mmHg.
-
Animal Model:normotensive dogs (anesthetized)[1]
-
Dosage:0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg
-
Administration:i.v.; cumulative dose
-
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.
-
Animal Model:rats[1]
-
Dosage:0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg; 3 mg/kg
-
Administration:i.v.; single dose
-
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
-
No. CAS 97233-26-6
-
Peso molecular 371.49
-
Fòrmula C21H25NO3S
-
SMILES
O=C1C2=C(SC(C)=C2)CC[C@H]1CN[C@@H]3[C@@H]([C@H](CC3)OC4=CC=CC=C4)O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
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)
MDL-19744A Related Classifications
HY-183954 Related Classifications
Powered by Bioz