Apraclonidine Hydrochloride

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Cat Number

API73218798

CAS Number

73218-79-8

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Product Detail Description Scientific Support Customer Q&A

CAS Number

73218-79-8

Storage

Room temperature

Synonyms

2-(4-amino-2,6-dichlorophenylimino)imidazolidinehydrochloride;2,6-dichloro-n(sup1)-(2-imidazolidinylidene)-1,4-benzenediaminehydrochlorid

Molecular Formula

C9H11Cl3N4

Molecular Weight

281.6

Smiles

C1CN=C(N1)NC2=C(C=C(C=C2Cl)N)Cl.Cl

Appearance

White solid

Melting Point

>230℃

General Description

Apraclonidine Hydrochloride is a synthetic alpha-2 adrenergic agonist with high selectivity for the alpha-2 receptor subtype, used primarily in ophthalmology for the management of glaucoma and ocular hypertension. Its chemical structure is a clonidine derivative with a para-amino group that reduces its ability to cross the blood-brain barrier, minimizing central nervous system side effects compared to non-selective alpha-2 agonists.

Mechanism of Action

Apraclonidine activates alpha-2 adrenergic receptors on the ciliary epithelium, which decreases aqueous humor production by suppressing the adenylate cyclase signaling pathway and reducing cAMP levels in ciliary epithelial cells. Additionally, activation of alpha-2 receptors on presynaptic nerve terminals in the ciliary muscle reduces sympathetic outflow, further decreasing aqueous humor secretion. The dual-action mechanism lowers intraocular pressure (IOP) without causing significant vasoconstriction of retinal vessels.

Application

Apraclonidine Hydrochloride is indicated for the short-term adjunctive treatment of chronic glaucoma and ocular hypertension in patients who are inadequately controlled by beta-blocker monotherapy.

Apraclonidine (APR) is a selective α2-adrenergic receptor agonist used to diagnose Horner’s syndrome and treat glaucoma. Its mechanism of action involves binding to and activating α2-adrenergic receptors, which reduces aqueous humor production and lowers intraocular pressure. At the molecular level, APR interacts with serum albumin as a carrier protein. Fluorescence and UV-Vis spectroscopy, along with molecular docking, reveal that APR binds to bovine serum albumin (BSA) primarily at drug site 2 (DS2) via hydrophobic forces, hydrogen bonds, and van der Waals interactions. The binding is entropy-driven with positive enthalpy and entropy changes. APR binding quenches BSA fluorescence and alters the microenvironment near tryptophan and tyrosine residues. These interactions influence APR’s pharmacokinetics, including its transport, distribution, and potential accumulation in tissues, which may lead to central nervous and cardiovascular effects.

Fig. 1 Molecular interaction between Apraclonidine and bovine serum albumin. (Kucuk I.; et al. 2025)

References

Kucuk I, et al. Investigation of the molecular interaction between apraclonidine, an α2-adrenergic receptor agonist, and bovine serum albumin using fluorescence and molecular docking techniques. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy, 2025, 326: 125246.

What is the recommended storage condition for Apraclonidine Hydrochloride?

It should be stored at controlled room temperature in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.

Is a Certificate of Analysis (COA) available for Apraclonidine Hydrochloride?

Yes, a fully verified COA is issued for every batch and can be shared electronically. Additional documentation such as MSDS or impurity profiles may be requested separately.

What quantities of Apraclonidine Hydrochloride are available for order?

We accommodate orders of varying scale, from small research quantities through bulk commercial supply. Contact our sales team to discuss pack sizes and volume pricing.

What grade is available for ophthalmic formulation of Apraclonidine Hydrochloride?

Ophthalmic-grade material meeting stringent sterility and particulate specifications is available; please consult our team for full specification details.

What quality standards govern the production of Apraclonidine Hydrochloride?

Production is carried out under GMP-aligned quality systems with full traceability and documented quality controls for each manufacturing run.