Fiduxosin
Fiduxosin is a potent α1-adrenoceptor antagonist, with Ki of 0.160 nM, 24.9 nM, and 0.920 nM for α1a-, α1b-, and α1d-adrenoceptors, respectively.
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- CAS. Nr.: 208993-54-8
- Formel: C30H29N5O4S
- Molecular Weight:555.65
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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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Biologische Aktivität
Ki: 0.16 nM (α1a-adrenoceptor), 24.9 nM (α1b- adrenoceptor), 0.92 nM (α1d-adrenoceptor), 92 nM (Human α2a-adrenoceptor), 22 nM (Human α2c-adrenoceptor), 21 nM (Rat α2b-adrenoceptor), 29 nM (Rat 5HT1A receptor)[1]
Fiduxosin displays low affinity for other adrenoceptors, including cloned human α2a- (92 nM) and α2c-adrenoceptors (22 nM) and rat neonatal lung α2b-adrenoceptors (21 nM), in addition to β-adrenoceptors (2-5 μM). Fiduxosin also has low affinity for 5HT1A receptors in rat cortex (29 nM) compared with its affinity at α1a-adrenoceptors (0.16 nM). Fiduxosin antagonizes competitively PE-induced responses with a pA2 value of 7.58, in the rabbit urethra[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 208993-54-8
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Molecular Weight 555.65
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Formel C30H29N5O4S
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SMILES
O=C(N1CCCCN2C[C@]3([H])[C@](COC4=CC=CC(OC)=C34)([H])C2)C5=C(NC1=O)C6=NC(C7=CC=CC=C7)=CN=C6S5
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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.
Protokoll
Male beagle dogs (>2 years old, 12-15 kg) are chronically instrumented for the continuous measurement of arterial blood pressure by implanting a telemetry transducer/transmitter (TA11PA-C40) into a carotid artery. On test day, dogs are placed in sling restraints and an Abbocath-T i.v. catheter (18-G) is inserted into a cephalic vein for blood sampling and for the administration of agonist. Prostatic intraurethral pressure (IUP) is measured using a transurethral 7F Swan-Ganz balloon catheter (41224-01). Dose responses of the intraurethral and arterial pressor effects of 8, 16, and 32 μg/kg i.v. phenylephrine (PE) are obtained before and at various time points after a single p.o. dose of an antagonist. Fiduxosin is dissolved in a vehicle of 20% ethanol, 30% propylene glycol, and 50% water. Terazosin and tamsulosin are dissolved in water. All antagonists are given by gavage in a volume of 1 mL/kg. PE is dissolved in saline and administered in a volume of 0.1 mL/kg. The increase in IUP or mean arterial pressure (MAP) caused by PE is allowed to return to baseline before the next dose is administered.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
Verweise
[1]. Hancock AA, et al. Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties. J Pharmacol Exp Ther. 2002 Feb;300(2):478-86. [Content Brief]
[2]. Brune ME, et al. Effect of fiduxosin, an antagonist selective for alpha(1A)- and alpha(1D)-adrenoceptors, on intraurethral and arterial pressure responses in conscious dogs. J Pharmacol Exp Ther. 2002 Feb;300(2):487-94. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Fiduxosin Related Classifications
HY-U00399 Related Classifications
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