Apraclonidine

Names

[ Name ]:
Apraclonidine

[Synonym ]:
para-aminoclonidine
4-Aminoclonidine
Apraclonidinum
Iopidine
Apraclonidina
Apraclonidinum [INN-Latin]
2,6-dichloro-1-N-(4,5-dihydro-1H-imidazol-2-yl)benzene-1,4-diamine
2-(4-amino-2,6-dichlorophenylamino)-2-imidazoline
[3H]-p-aminoclonidine
2,6-Dichloro-N1-(4,5-dihydro-1H-imidazol-2-yl)benzene-1,4-diamine
p-amino clonidine
Apraclonidina [INN-Spanish]
MFCD00865638
Aplonidine

Biological Activity

[Description]:

Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution[1][2].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Neurological Disease

[In Vitro]

Apraclonidine hydrochloride (ALO 2145) is more commonly used topically for glaucoma, as it penetrates the cornea and blood-brain barrier to a lesser extent and, thus, has fewer adverse systemic effects[2].

[In Vivo]

Apraclonidine hydrochloride (ALO 2145) is effective in animal models of elevated IOP as well as glaucoma in humans. The ocular hypotensive effects of Apraclonidine are usually attributed to reduced aqueous humor synthesis and vasoconstrictor actions at the anterior segment branches of the ophthalmic artery. Apraclonidine (1.15%, single instillation) inhibits 98% of PGE2-induced aqueous flare elevationy[2][3] . Animal Model: male rabbits[3] Dosage: 1.15% Administration: Apraclonidine (1.15%, single instillation) Result: Inhibited PGE2-induced elevation of aqueous flare in pigmented rabbits.

[References]

[1]. Subhashie Wijemanne, et al. Apraclonidine in the treatment of ptosis. J Neurol Sci

[2]. R V Searles, et al. Aqueous humor dynamics in anesthetized rats infused with intracameral apraclonidine. Pharmacology. 1999 Apr;58(4):220-6.

[3]. Yoriko Hayasaka, et al. Effects of topical antiglaucoma eye drops on prostaglandin E(2)-induced aqueous flare elevation in pigmented rabbits. Invest Ophthalmol Vis Sci

Chemical & Physical Properties

[ Density]:
1.63g/cm3

[ Boiling Point ]:
395.5ºC at 760mmHg

[ Molecular Formula ]:
C₉H₁₀Cl₂N₄

[ Molecular Weight ]:
245.10800

[ Flash Point ]:
193ºC

[ Exact Mass ]:
244.02800

[ PSA ]:
62.44000

[ LogP ]:
2.36530

[ Appearance of Characters ]:
solid | white

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: 1.4 mg/mL Solutions may be stored for several days at 4?#x00b0;C

Safety Information

[ Hazard Codes ]:
T

[ Risk Phrases ]:
R23/24/25

[ Safety Phrases ]:
S22-S36/37/39-S45

[ RIDADR ]:
UN 2811 6.1/PG 1

[ WGK Germany ]:
3

[ HS Code ]:
2933290090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933290090

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Related Compounds

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