Iopidine

Names

[ Name ]:
Iopidine

[Synonym ]:
UNII-D2VW67N38H
Iopidine ophthalmic solution
MFCD00135922
2-(4-Amino-2,6-dichlorophenylimino)imidazolidine
2-[(4-amino-2,6-dichlorophenyl)imino]imidazolidine monohydrochloride
APRACLONIDINE HYDROCHLORIDE
ALO-2145
2,6-dichloro-1-N-(4,5-dihydro-1H-imidazol-2-yl)benzene-1,4-diamine,hydrochloride
p-aminoclonidine hydrochloride
NC 14 hydrochloride
2-[(2,6-dichloro-4-aminophenyl)imino]imidazolidine hydrochloride
p-aminoclonidine
mono hydrochloride
Apraclonidine HCl

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 and has the ability to elevate the eye lid[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Others

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[2].

[References]

[1]. Wijemanne S, et al. Apraclonidine in the treatment of ptosis. J Neurol Sci. 2017;376:129‐132.

[2]. Searles RV, et al. Aqueous humor dynamics in anesthetized rats infused with intracameral apraclonidine. Pharmacology. 1999;58(4):220‐226.

Chemical & Physical Properties

[ Density]:
1.63 g/cm3

[ Boiling Point ]:
395.5ºC at 760 mmHg

[ Melting Point ]:
>230ºC

[ Molecular Formula ]:
C₉H₁₁Cl₃N₄

[ Molecular Weight ]:
281.56900

[ Flash Point ]:
193ºC

[ Exact Mass ]:
280.00500

[ PSA ]:
62.44000

[ LogP ]:
3.16730

[ Storage condition ]:
2-8°C

[ Stability ]:
Moisture Sensitive

[ 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

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CZ1582000

CHEMICAL NAME :: 1,4-Benzenediamine, 2,6-dichloro-N(sup 1)-(4,5-dihydro-1H-imidazol-2-yl)-, monohydrochloride

CAS REGISTRY NUMBER :: 73218-79-8

LAST UPDATED :: 199604

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C9-H10-Cl2-N4.Cl-H

MOLECULAR WEIGHT :: 281.59

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 38 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 24,557,1988

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 24,557,1988

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 24,557,1988

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 6 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 24,557,1988

Safety Information

[ Symbol ]:

GHS06, GHS08

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H300-H370

[ Precautionary Statements ]:
Missing Phrase - N15.00950417-P308 + P311

[ Target Organs ]:
Cardio-vascular system

[ Hazard Codes ]:
T: Toxic;

[ Risk Phrases ]:
R23/24/25

[ Safety Phrases ]:
22-36/37/39-45

[ RIDADR ]:
UN 2811

[ WGK Germany ]:
3

[ Packaging Group ]:
III

[ Hazard Class ]:
6.1(b)

[ HS Code ]:
2933290090

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%