A histamine H1 receptor antagonist (Ki = 38.4 nM in cell membranes expressing human recombinant H1 receptors); reduces histamine-induced IL-6 and IL-8 production in human conjunctival epithelial cells (IC50s = 1 and 0.652 μM

Antazoline (hydrochloride) – 1 g

Brand:
Cayman
CAS:
2508-72-7
Storage:
-20
UN-No:
Non-Hazardous - /

Antazoline is a histamine H1 receptor antagonist that binds to histamine H1receptors with a Ki value of 38.4 nM in cell membranes expressing human recombinant H1 receptors.{33247} Antazoline reduces histamine-induced IL-6 and IL-8 production in human conjunctival epithelial cells (IC50s = 1 and 0.652 μM, respectively). It completely prevents anaphylaxis in rabbits sensitized to egg albumin and increases survival in a guinea pig model of histamine-induced bronchospasm.{40285} Antazoline (10-30 µM) eliminates atrial fibrillation induced by acetylcholine and isoproterenol (Item No. 15592) in isolated rabbit hearts by increasing the atrial effective refractory period and interatrial conduction time in a dose-dependent manner.{40286} Antazoline also binds to NMDA receptors (Ki = 13 μM) and reduces glutamate-induced toxicity in cerebellar granule cells (EC50 = 13 μM).{40287}  

 

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SKU: 23415 - 1 g Category:

Description

A histamine H1 receptor antagonist (Ki = 38.4 nM in cell membranes expressing human recombinant H1 receptors); reduces histamine-induced IL-6 and IL-8 production in human conjunctival epithelial cells (IC50s = 1 and 0.652 μM, respectively); prevents anaphylaxis in rabbits sensitized to egg albumin and increases survival in a guinea pig model of histamine-induced bronchospasm; eliminates atrial fibrillation induced by acetylcholine and isoproterenol in isolated rabbit hearts by increasing the atrial effective refractory period and interatrial conduction time in a dose-dependent manner; binds to NMDA receptors (Ki = 13 μM) and reduces glutamate-induced toxicity in cerebellar granule cells (EC50 = 13 μM)

Formal name: 4,5-dihydro-N-phenyl-N-(phenylmethyl)-1H-imidazole-2-methanamine, monohydrochloride

Synonyms:  2-(N-Benzylanilinomethyl)-2-imidazoline Hydrochloride

Molecular weight: 301.8

CAS: 2508-72-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Heart|Arrhythmia||Research Area|Immunology & Inflammation|Allergy||Research Area|Neuroscience

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