Antazoline Phosphate

Antazoline Phosphate, as phosphate salt of antazoline, is the histamine H1 receptor antagonist. It acts as an antihistamine. Generally by combinating with a decongestant, antazoline phosphate is applied topically to relieve the symptoms of allergic conjunctivitis.

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CAT#	10-101-109
CAS	91-75-8 (net), 154-68-7 (phosphate)
Background	An imidazoline agonist that is more potent than efaroxan in inducing insulin release from β cells
Synonyms/Alias	2-(N-Phenyl-N-benzyl-aminomethyl)imidazoline . phosphate; 2-[(N-Benzylanilino)methyl]-2-imidazoline . phosphate; 4,5-Dihydro-N-phenyl-N-(phenylmethyl)-1H-imidazole-2-methanamine . phosphate
Chemical Name	N-benzyl-N-(4,5-dihydro-1H-imidazol-2-ylmethyl)aniline;phosphoric acid
M.F/Formula	C17H22N3O4P
M.W/Mr.	265.36 (net), 363.35 (phosphate)
Labeling Target	Histamine Receptor
Application	Conjunctivitis
Appearance	Solid powder
Purity	>98% (or refer to the Certificate of Analysis)
Activity	Antagonist
Areas of Interest	Neurological Disease
Target	Histamine H1 receptor

CAT#	Product Name	M.W	Molecular Formula	Inquiry
10-101-108	Antazoline Hydrochloride Ph. Eur.	265.36 (net), 301.82 (hydrochloride)	C17H20ClN3	Inquiry
10-101-110	Antazoline Sulfate	363.35	C17H19N3·H2O4S	Inquiry

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Solubility	Soluble in DMSO, not in water
Shipping Condition	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Short-term Storage Conditions	Dry, dark and at 0 - 4 °C
Long-term Storage Conditions	-20 °C
Format	neat
InChI	InChI=1S/C17H19N3.H3O4P/c1-3-7-15(8-4-1)13-20(14-17-18-11-12-19-17)16-9-5-2-6-10-16;1-5(2,3)4/h1-10H,11-14H2,(H,18,19);(H3,1,2,3,4)
InChI Key	DUIGUKRYYAGJAF-UHFFFAOYSA-N
Canonical SMILES	C1CN=C(N1)CN(CC2=CC=CC=C2)C3=CC=CC=C3.OP(=O)(O)O
BoilingPoint	235-236 °C(lit.)
ShelfLife	>2 years if stored properly
References	A controlled, double-blind comparison of naphalzoline hydrochloride 0.05%, antazoline phosphate 0.5%, a combination of both components and a placebo was performed on 51 ragweed sensitive patients presenting allergic conjunctivitis. Evaluation of response at various times after instillation of medication for lacrimation, conjunctival inflammation, pruritus, photophobia and pain showed naphazoline hydrochloride, antazoline phosphate and the combination product superior to placebo. The combination product was statistically significantly superior for conjunctival inflammation and photophobia. The need for post-challenge treatment with epinephrine hydrochloride was significantly less in those eyes treated with the combination product. demonstrating prophylactic efficacy. Miller J, Wolf E H. Antazoline phosphate and naphazoline hydrochloride, singly and in combination for the treatment of allergic conjunctivitis-a controlled, double-blind clinical trial[J]. Annals of allergy, 1975, 35(2): 81-86. A method for the determination of 2-[(N-phenyl)benzylaminomethyl]-2-imidazoline X H3PO4 (antazoline phosphate) and 2-(1,2,3,4-tetrahydro-1-naphthyl)-2-imidazoline X HCl (tetrahydrozoline hydrochloride) in ophthalmic solution is described. The pharmaceutical preparation is analysed directly by reversed-phase ion-pair high-performance liquid chromatography and the method is very rapid, selective and simple. Puglisi G, Sciuto S, Chillemi R, et al. Simultaneous high-performance liquid chromatographic determination of antazoline phosphate and tetrahydrozoline hydrochloride in ophthalmic solution[J]. Journal of Chromatography A, 1986, 369: 165-170.
Melting Point	120-122ºC