Antazoline hydrochloride - CAS 2508-72-7
Catalog number: 2508-72-7
Category: Inhibitor
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Molecular Formula:
C17H19N3.HCl
Molecular Weight:
301.81
COA:
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Targets:
Histamine Receptor
Description:
Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine.
Purity:
>98%
Synonyms:
Phenazocine HCl
MSDS:
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InChIKey:
SWKDMSRRIBZZAY-UHFFFAOYSA-N
InChI:
InChI=1S/C17H19N3.ClH/c1-3-7-15(8-4-1)13-20(14-17-18-11-12-19-17)16-9-5-2-6-10-16;/h1-10H,11-14H2,(H,18,19);1H
Canonical SMILES:
C1CN=C(N1)CN(CC2=CC=CC=C2)C3=CC=CC=C3.Cl
1.A review of the use of olopatadine in allergic conjunctivitis
James I. McGill. International Ophthalmology 25: 171–179, 2004.
The relative functional potency of olopatadine at ocular H1-receptors has been measured by looking at intracellular phospoinositide (PI) turnover or calcium mobilization (both involved in mast cell degranulation) and by measuring extracellular release of appropriate cytokines. In studies of this type, olopatadine has been shown to antagonize histamine-induced PI turnover in cultured human conjunctival epithelial cells (IC50 = 9.5–10 nM), human corneal fibroblasts (IC50 = 15.8–19 nM) and transformed human trabecular meshwork cells (IC50 = 31.6–39.9 nM). In a further comparative study, primary human conjunctival epithelial cell cultures were stimulated with histamine in the presence or absence of a variety of anti-histamines. Antazoline hydrochloride, emedastine difumarate, levocabastine hydrochloride, olopatadine hydrochloride and pheniramine maleate were all shown to attenuate histamine-stimulated phosphatidylinositol turnover and IL-6 and IL-8 secretion. Emedastine was the most potent, with IC50 1–3 nM, while olopatadine was of similar potency to levocabastine and far more potent than antazoline and pheniramine. Olopatadine was of similar potency to emedastine as an inhibitor of cytokine secretion (IC50 1.7–5.5 nM) and more potent than the other three antihistamines tested.
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CAS 2508-72-7 Antazoline hydrochloride

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