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Antazoline API

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CAS No.:

91-75-8

Grade:

Pharmaceutical Grade

Content:

99.9%

Port:

Shanghai

Packaging:

1KG

Price valid (until):

2025-12-31

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Geliad

Company Type:

Trader

Location:

China

Qualification:

Main Products:

Lacosamide,Minoxidil,Strontium Ranelate,Pizotifen,Sildenafil,Tadalafil

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Product Description
Seller Information

Description

Product Detail

Antazoline is an antihistamine and α-adrenergic blocker primarily used in:

Ophthalmology:
- Allergic conjunctivitis (often combined with naphazoline, e.g., Antistine® eye drops).
Cardiology (Historical Use):
- Antiarrhythmic (Class Ia, similar to quinidine) — now rare due to safer alternatives.

4. Mechanism of Action

H1-Receptor Antagonist: Blocks histamine-induced inflammation.
α-Adrenergic Blockade: Reduces vascular congestion (explains its use in eye drops with vasoconstrictors).

5. Key Literature & Patents

Synthesis & Chemistry

Original Synthesis: From 4-amino-benzhydryl chloride + ethylenediamine.
Patents:
- US Patent 2,502,115 (Ciba-Geigy, 1950): Early synthesis method.
- WO 2010/135689: Improved formulations for ophthalmic use.

Clinical Studies

Ophthalmic Efficacy:
- Abelson et al. (1980): Demonstrated rapid relief of allergic conjunctivitis symptoms.
  DOI: 10.1016/S0002-9394(14)75305-5

6. Pharmacokinetics

Absorption: Poor systemic absorption from ocular use.
Metabolism: Hepatic (CYP450).
Half-life: ~4–6 hours (topical).

Items	Specifications
Antazoline	Ophthalmic Grade

Certificates

Basic Info

Product Name:

Antazoline

Other Name:

1H-Imidazole-2-methanamine,4,5-dihydro-N-phenyl-N-(phenylmethyl)-;2-Imidazoline,2-[(N-benzylanilino)methyl]-;4,5-Dihydro-N-phenyl-N-(phenylmethyl)-1H-imidazole-2-methanamine;Allergan A;Antazoline;Antistine;2-[(N-Benzylanilino)methyl]-2-imidazoline;Phenazoline;Analergine

CAS No.:

91-75-8

Molecular Formula:

C17H19N3

InChIKeys:

InChIKey=REYFJDPCWQRWAA-UHFFFAOYSA-N

Molecular Weight:

265.35

Exact Mass:

265.35

EC Number:

202-094-0

UNII:

DHA8014SS1

DSSTox ID:

DTXSID3022613

NCI Thesaurus Code:

C61638

Color/Form:

White, crystalline powder

ATC Code:

R - Respiratory system

Categories:

Other Chemical Drugs

Characteristics

PSA:

27.6

XLogP3:

3.38 (est)

Appearance:

Solid

Density:

1.1±0.1 g/cm3

Melting Point:

120-122 °C

Boiling Point:

475.5±38.0 °C at 760 mmHg

Flash Point:

241.4±26.8 °C

Refractive Index:

1.608

Water Solubility:

In water, 6.63X10+2 mg/L at 30 deg C

Storage Conditions:

Keep in a cool, dry, dark location in a tightly sealed container or cylinder. Keep away from incompatible materials, ignition sources and untrained individuals. Secure and label area. Protect containers/cylinders from physical damage.

Vapor Pressure:

2.3X10-8 mm Hg at 25 deg C (est)

Toxicity:

LD50 oral in mouse: 398mg/kg

Odor:

Odorless

Taste:

Bitter

Henrys Law Constant:

Henry's Law constant = 6.0X10-11 atm-cu m/mol at 25 °C (est)

Dissociation Constants:

pKa = 4.90 (non-cyclic tertiary nitrogen); pKa = 10.68 (tertiary imidazoline nitrogen) (est)

Experimental Properties:

Hydroxyl radical reaction rate constant = 2.4X10-10 cu cm/molecule-sec at 25 °C (est)

See More Antazoline Properties 

Hazard Identification

Classification of the substance or mixture

Acute toxicity - Category 4, Oral

Acute toxicity - Category 4, Dermal

Skin irritation, Category 2

Eye irritation, Category 2

Specific target organ toxicity â single exposure, Category 3

GHS label elements, including precautionary statements

Precautionary statement(s)
Pictogram(s)
Signal word	Warning
Hazard statement(s)	H302 Harmful if swallowed H312 Harmful in contact with skin H315 Causes skin irritation H319 Causes serious eye irritation H335 May cause respiratory irritation
Prevention	P264 Wash ... thoroughly after handling. P270 Do not eat, drink or smoke when using this product. P280 Wear protective gloves/protective clothing/eye protection/face protection/hearing protection/... P261 Avoid breathing dust/fume/gas/mist/vapours/spray. P271 Use only outdoors or in a well-ventilated area.
Response	P301+P317 IF SWALLOWED: Get medical help. P330 Rinse mouth. P302+P352 IF ON SKIN: Wash with plenty of water/... P317 Get medical help. P321 Specific treatment (see ... on this label). P362+P364 Take off contaminated clothing and wash it before reuse. P332+P317 If skin irritation occurs: Get medical help. P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P304+P340 IF INHALED: Remove person to fresh air and keep comfortable for breathing. P319 Get medical help if you feel unwell.
Storage	P403+P233 Store in a well-ventilated place. Keep container tightly closed. P405 Store locked up.
Disposal	P501 Dispose of contents/container to an appropriate treatment and disposal facility in accordance with applicable laws and regulations, and product characteristics at time of disposal.

Other hazards which do not result in classification

no data available

Handling and Storage

Precautions for safe handling

Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.

Conditions for safe storage, including any incompatibilities

Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.

See More Antazoline Safety Data Sheet 

Seller Information

Business Type:
Trader

Main Products:
Lacosamide,Minoxidil,Strontium Ranelate,Pizotifen,Sildenafil,Tadalafil

Location:
1-2F, No. 365, 367, 377, Gubei East Road, Baoshan District, Shanghai

Payment Terms:
TT against copy of documents,D/P,L/C,D/A,TT against B/L draft before shipment,100% TT in advance

Average lead Time:
28

Total Annual Revenue:
$10 million-$25 million

Total Employees:
11-50

Year of Establishment:
2024

Shanghai Geliad Biotechnology Co. Ltd. is committed to advancing pharmaceutical research by leveraging cutting-edge technology and scientific expertise to develop novel active pharmaceutical ingredients (APIs). Our research team collaborates with leading academic institutions, biotech firms, and industry experts to explore innovative drug synthesis techniques, optimize production processes, and enhance the efficacy and safety of pharmaceutical compounds. With a strong focus on small-scale, high-value APIs, we continuously invest in state-of-the-art laboratories and analytical tools to ensure precision, quality, and regulatory compliance. By integrating global trends with local R&D strengths, we strive to bring groundbreaking pharmaceutical solutions to the international market, supporting drug manufacturers in creating next-generation therapeutics.
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