A potent 5-HT2 receptor antagonist (IC50 = 6.3 nM; Ki = 2.1 nM); has activity at H1

Ketanserin (tartrate) – 100 mg

Brand:
Cayman
CAS:
83846-83-7
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Ketanserin is a potent antagonist of the serotonin (5-HT) receptor that is selective for 5-HT2 (IC50 = 6.3 nM; Ki = 2.1 nM).{40001} It has no activity at 5-HT1 receptors but does have activity at histamine type 1, α1-adrenergic, and dopamine receptors with Ki values of 10, 10, and 220 nM, respectively. Ketanserin induces dose-dependent inhibition of contractile responses to 5-HT in isolated rat caudal artery, canine basilar, carotid, coronary and gastrosplenic arteries, and canine gastrosplenic and saphenous veins.{40003} Ketanserin (10 mg/kg/day) significantly decreases blood pressure (BP), blood pressure variability (BPV), and hypertensive organ damage in spontaneously hypertensive rats.{40002} Formulations containing ketanserin have been used to treat hypertension in early-onset preeclampsia.{40000}  

 

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Description

A potent 5-HT2 receptor antagonist (IC50 = 6.3 nM; Ki = 2.1 nM); has activity at H1, α1-ARs, and DA receptors; Kis = 10, 10, and 220 nM, respectively); induces dose-dependent inhibition of contractile responses to 5-HT in arteries and veins; significantly decreases BP, BPV, and hypertensive organ damage in spontaneously hypertensive rats,

Formal name: 3-[2-[4-(4-fluorobenzoyl)-1-piperidinyl]ethyl]-2,4(1H,3H)-quinazolinedione (2R,3R)-2,3-dihydroxybutanedioate

Synonyms: 

Molecular weight: 545.5

CAS: 83846-83-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation

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