Fluprofylline
Fluprofylline (Sgd 144/8) is a selective α1-adrenergic receptor antagonist with a pIC50 of 7.55. Fluprofylline attenuates the pressor response induced by 5-HT (HY-B1473A). Fluprofylline can be used in hypertension research.
For research use only. We do not sell to patients.
- CAS No.: 85118-43-0
- Formula: C22H26FN5O3
- Molecular Weight:427.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Adrenergic Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
α1-adrenergic receptor 7.55 (pIC50) |
α2-adrenergic receptor 4.63 (pIC50) |
5-HT2R 6.70 (pIC50) |
In Vitro
Fluprofylline binds to central α2-adrenoceptor sites in rat brain membranes with a very low -log IC50 of 4.63[1].
Fluprofylline binds to rat brain membrane α1-adrenoceptors with a -log IC50 of 7.55, and is highly selective for α1-adrenoceptors over α2-adrenoceptors and 5-HT2 receptors.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Fluprofylline (10-5 mol/kg; i.a.; single dose) acts as a selective α1-adrenoceptor antagonist in pithed normotensive rats, with a 43-fold greater potency for α1- over α2-adrenoceptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 200-300 g, pithed for vascular adrenoceptor antagonism testing)[1]
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Dosage:10-5 mol/kg
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Administration:i.a.; single dose
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Result:Produced a dose-ratio (DR) of 95 for antagonism of amidephrine-induced α1-adrenoceptor-mediated pressor responses.
Produced a DR of 2.2 for antagonism of B-HT 920-induced α2-adrenoceptor-mediated pressor responses.
Yielded an α1/α2 selectivity ratio of 43.
Did not significantly influence baseline diastolic pressure.
Chemical Information
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CAS No. 85118-43-0
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Molecular Weight 427.47
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Formula C22H26FN5O3
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SMILES
O=C1C2=C(N(C)C(N1C)=O)N=CN2CCCN3CCC(CC3)C(C4=CC=C(C=C4)F)=O
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Synonyms
Sgd 144/8
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Korstanje C, et al. Characterization of flufylline, fluprofylline, ritanserin, butanserin and R 56413 with respect to in-vivo alpha 1-,alpha 2- and 5-HT2-receptor antagonism and in-vitro affinity for alpha 1-,alpha 2- and 5-HT2-receptors: comparison with ketanserin. J Pharm Pharmacol. 1986 May;38(5):374-9. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fluprofylline Related Classifications
HY-184666 Related Classifications
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