UR 8225
UR 8225 is an orally active ATP-sensitive K+ channel activator with vasodilator, smooth muscle relaxant, antihypertensive, and bronchodilator activities. UR 8225 induces membrane hyperpolarization by increasing outward K+ conductance and reduces Ca2+ influx through voltage-gated L-type Ca2+ channels. UR 8225 reduces total peripheral vascular resistance, shortens cardiac action potential duration, inhibits agonist-induced Ca2+ influx, and stimulates renin release. UR 8225 induces reflex tachycardia but lacks β-adrenergic receptor blocking activity. UR 8225 is widely applicable to research in fields related to hypertension, myocardial ischemia, ventricular fibrillation, and other conditions.
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- CAS. Nr.: 149455-36-7
- Formel: C18H14N2O2
- Molecular Weight:290.32
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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
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L-type calcium channel |
UR 8225 (0.05-6.9 μM) inhibits spontaneous myogenic contractions (IC50=0.05 μM) and norepinephrine-induced contractions (IC50=6.9 μM) in rat portal vein segments, with effects antagonized by glyburide (HY-15206)[1].
UR 8225 (0.32-0.76 μM) relaxes spontaneous tone (EC50=0.32 μM) and inhibits histamine-induced contractions (EC50=0.76 μM) in isolated guinea pig trachea, with effects reversed by glyburide (HY-15206)[1].
UR 8225 (0.1-10 μM) concentration-dependently inhibits spontaneous contractile activity in guinea pig urinary bladder detrusor muscle, significantly reduces low KCl-induced contractions at 10 μM, and only slightly inhibits Carbamoylcholine chloride (HY-B1208)-induced contractions at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
UR 8225 (0.1-1 mg/kg; p.o.) produces dose-dependent, long-lasting antihypertensive effects in conscious SHR with an ED20 of 0.1 mg/kg, accompanied by reflex tachycardia and transient activation of the renin-angiotensin system[1].
UR 8225 (0.03-0.3 mg/kg; i.v.) produces dose-dependent hypotensive effects in anesthetized normotensive rats with an ED20 of 0.04 mg/kg, and these effects are completely blocked by pretreatment with 20 mg/kg i.v. glyburide (HY-15206)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male guinea pigs (anesthetized)[1]
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Dosage:0.01 mg/kg; 0.1 mg/kg
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Administration:i.v.
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Result:Produced a dose-related reduction in metacholine-induced bronchoconstriction, with an IC50 of 0.029 mg/kg.
Decreased metacholine-induced bronchospasm by 75.5% and reduced mean arterial blood pressure by 49.9%.
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Animal Model:Normotensive rats (anesthetized)[1]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
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Administration:i.v.
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Result:Produced dose-dependent reductions in MAP, with an ED20 of 0.04 mg/kg.
Decreased MAP by 43% at 0.1 mg/kg i.v.; this effect was reduced to 30%, 14%, and 0.4% by pretreatment with glyburide at 3 mg/kg, 10 mg/kg, and 20 mg/kg i.v., respectively, with 20 mg/kg glyburide completely blocking the hypotensive response.
Chemical Information
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CAS. Nr. 149455-36-7
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Molecular Weight 290.32
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Formel C18H14N2O2
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SMILES
N#CC1=CC2=C(C(C(C)(C)C=C2N3C=CC=CC3=O)=O)C=C1
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
UR 8225 Related Classifications
HY-183206 Related Classifications
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- UR 8225
- 149455-36-7
- UR8225
- UR-8225
- Potassium Channel
- Calcium Channel
- guinea pig trachea
- SHR
- voltage-gated L-type Ca2+ channels
- guinea pig urinary bladder detrusor muscle
- WKY rats
- DOCA-salt-induced hypertensive rats
- rat portal vein segments
- ATP-sensitive K+ channel
- rat aortic vascular smooth muscle cells
- guinea pig papillary muscle fibres
- Inhibitor
- inhibitor
- inhibit