Description
QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.
Product information
CAS Number: 149247-12-1
Molecular Weight: 364.48
Formula: C23H28N2O2
Chemical Name: 2-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-1,2,3,4-tetrahydronaphthalen-1-one
Smiles: COC1=CC=CC=C1N1CCN(CCC2CCC3C=CC=CC=3C2=O)CC1
InChiKey: PJOARVZMKMVACL-UHFFFAOYSA-N
InChi: InChI=1S/C23H28N2O2/c1-27-22-9-5-4-8-21(22)25-16-14-24(15-17-25)13-12-19-11-10-18-6-2-3-7-20(18)23(19)26/h2-9,19H,10-17H2,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
Products are for research use only. Not for human use.
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