1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. QF0301B

QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.

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QF0301B

QF0301B Chemical Structure

CAS No. : 149247-12-1

Size Prix Stock Quantité
1 mg Obtenir un devis 2 - 3 weeks 1-2 weeks 3 - 4 weeks 2-3 weeks
5 mg Obtenir un devis 2 - 3 weeks 1-2 weeks 3 - 4 weeks 2-3 weeks
10 mg   Obtenir un devis  
50 mg   Obtenir un devis  
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Description

QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.

IC50 & Target

α adrenergic receptor

 

5-HT2A Receptor

 

In Vitro

In isolated rubbed rat aorta rings, QF0301B shows marked α1-adrenoceptor blocking activity, with a pA2 value of 9.00±0.12. QF0301B reverses and competitively antagonizes the inhibitory action produced by clonidine in electrically stimulated rat vas deferens and inhibits the force and rate of contraction in rat isolated atria (pA2=5.91±0.43), competitively antagonizes the contractile effect of 5-HT in rat aorta (pA2=6.75±0.06) and in rat stomach fundus (pA2=7.13±0.48) and the contractions induced by histamine in isolated guinea pig longitudinal ileal muscle (pA2=7.40±0.40). QF0301B shows noncompetitive low action in 5-HT3, muscarinic and nicotinic receptors, or as Ca2+ antagonist[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

QF0301B (0.1-0.2 mg/kg iv) can cause a pronounced and prolonged fall in mean arterial blood pressure accompanied by bradycardia. QF0301B does not significantly modify the cardiovascular effects of either 5-hydroxytryptamine (serotonin, 5-HT, 75 mg/kg iv) or the selective a2-adrenoceptor agonist B-HT 920 (0.2 mg/kg iv), but markedly inhibits the hypertensive effect of noradrenaline (5 mg/kg iv), a nonselective a-adrenergic receptor agonist[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Masse moléculaire

364.48

Formule

C23H28N2O2

CAS No.
SMILES

O=C1C(CCN2CCN(C3=CC=CC=C3OC)CC2)CCC4=C1C=CC=C4

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation
Références
Administration animale
[1]

Rats: Normotensive rats are anaesthetized. When blood pressure and heart rate have stabilized (30 min after cannulation), vehicle (1 ml/kg), QF0301B, or prazosin solution (0.1-0.2 mg/kg) is injected intravenously via the femoral vein, and the effects on blood pressure and heart rate are observed[1].

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

Références
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Inquiry Information

Nom du produit:
QF0301B
Cat. No.:
HY-101690
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