Apraclonidine

Modify Date: 2024-01-01 19:00:23

Apraclonidine Structure
Apraclonidine structure
Common Name Apraclonidine
CAS Number 66711-21-5 Molecular Weight 245.10800
Density 1.63g/cm3 Boiling Point 395.5ºC at 760mmHg
Molecular Formula C9H10Cl2N4 Melting Point N/A
MSDS N/A Flash Point 193ºC

 Use of Apraclonidine


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].

 Names

Name apraclonidine
Synonym More Synonyms

 Apraclonidine 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
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

~79%

Apraclonidine Structure

Apraclonidine

CAS#:66711-21-5

Literature: Van Dort; Neubig; Counsell Journal of medicinal chemistry, 1987 , vol. 30, # 7 p. 1241 - 1244

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Apraclonidine Structure

Apraclonidine

CAS#:66711-21-5

Literature: Journal of medicinal chemistry, , vol. 30, # 7 p. 1241 - 1244

 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%

 Synonyms

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
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