| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Apraclonidine (iopidine) is a novel and potent α2 receptor agonist used in glaucoma therapy. It is also a weak alpha-1 adrenergic receptor agonist. Apraclonidine enhances aqueous humor uveoscleral outflow and decreases aqueous production by vasoconstriction.
| Targets |
α2/α1 receptor
|
|---|---|
| ln Vitro |
Because it has less negative systemic effects and less penetration into the cornea and blood-brain barrier, apraclonidine (ALO 2145 (free base)) is more frequently used topically to treat glaucoma [2].
|
| ln Vivo |
Apraclonidine (ALO 2145 (free base)) is useful in treating human glaucoma and increased intraocular pressure in animal models. Praclonidine's IOP-lowering effects are typically linked to decreased aqueous humor production and anterior ophthalmic artery vasoconstriction. 98% of PGE2-induced increases in aqueous humor flare are inhibited by apaclonidine (ALO 2145 (free base)) (1.15%, single infusion) [2][3].
The apraclonidine (1.15%, single infusion) inhibits 98% of PGE2-induced increases in aqueous humor flare [3]. Apraclonidine hydrochloride (ALO 2145) is effective in human glaucoma and animal models of elevated intraocular pressure. The IOP-lowering effect of apraclonidine is generally attributed to reduced aqueous humor synthesis and vasoconstriction of the anterior branches of the ophthalmic artery [2].
A single instillation of apraclonidine 1.15%, two instillations of epinephrine 1.25%, two instillations of dipivefrin 0.1%, and two instillations and one instillation of dipivefrin 0.04% eye drops inhibited 98%, 96%, 87%, 73%, and 47% of PGE(2)-induced aqueous flare elevation, respectively. Timolol 0.5%, nipradilol 0.25%, dorzolamide 1%, and pilocarpine 2% eye drops had no effects on the increase of PGE(2)-induced flare. Conclusions: Apraclonidine, epinephrine, and dipivefrin eye drops inhibit PGE(2)-induced elevation of aqueous flare in pigmented rabbits [3]. |
| Animal Protocol |
Animal/Disease Models: Male rabbit [3]
Doses: 1.15% Route of Administration: Apraclonidine (1.15%, single infusion) Experimental Results: Inhibited PGE2-induced increase in aqueous humor flare in pigmented rabbits. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Topical application of apraclone eye drops can lead to systemic absorption. Studies in healthy volunteers showed that, with one drop of apraclone (0.5% eye drops) three times daily for 10 consecutive days in both eyes, the average peak and trough concentrations were 0.9 ng/mL and 0.5 ng/mL, respectively. Biological Half-Life 8 hours |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use During Lactation There is currently no information regarding the use of apraclofen during lactation. To significantly reduce the amount of medication that enters breast milk after using eye drops, press your finger against the tear duct near the corner of your eye for at least 1 minute, then wipe away any excess medication with absorbent tissue. One manufacturer recommends avoiding breastfeeding on the day of argon laser trabeculoplasty, argon laser iridotomy, or posterior capsulotomy. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. Protein binding 98.7% Oral LD50 in rats: 38 mg/kg, Medicamentos de Actualidad., 24(557), 1988 Intravenous LD50 in rats: 9 mg/kg, Medicamentos de Actualidad., 24(557), 1988 Oral LD50 in mice: 3 mg/kg, Medicamentos de Actualidad., 24(557), 1988 Intravenous LD50 in mice: 6 mg/kg, Medicamentos de Actualidad., 24(557), 1988 |
| References | |
| Additional Infomation |
Apraclonidine is an imidazoline compound with the chemical name 2-amino-4,5-dihydro-1H-imidazoline, in which one of the outer amino hydrogen atoms is replaced by 4-amino-2,6-dichlorophenyl. It has multiple functions, including as an α-adrenergic agonist, an anti-glaucoma drug, an ophthalmic drug, a β-adrenergic agonist, and a diagnostic reagent. It belongs to the imidazoline, dichlorobenzene, and guanidine classes. It is the conjugate base of Apraclonidine(1+). Apraclonidine, also known as iodopyridine, is a sympathomimetic drug used to treat glaucoma. It is an α2-adrenergic agonist. The mechanism of action of Apraclonidine is as an α-adrenergic receptor agonist. Apraclonidine is a clonidine derivative with selective α2-adrenergic agonist activity. Following intraocular administration, Apraclonidine lowers intraocular pressure (IOP) by increasing aqueous humor outflow from the uvea and sclera and reducing aqueous humor production through vasoconstriction. See also: Apraclonidine hydrochloride (salt form). Indications: For the prevention or reduction of elevated intraocular pressure (IOP) before or after laser eye surgery. Also used as short-term adjunctive therapy in patients with open-angle glaucoma who have received the maximum tolerated dose but require further IOP reduction. FDA label. Mechanism of Action: Apraclonidine is a relatively selective α2-adrenergic receptor agonist with less stimulation of α1 receptors. Its IOP-lowering effect peaks two hours after administration. The exact mechanism of action is unclear, but animal and human fluorophotometric studies suggest that Apraclonidine has a dual mechanism of action: reducing aqueous humor production by constricting ciliary afferent vessels and increasing uveal-scleral outflow.
Pharmacodynamics Apraclonidine significantly lowers intraocular pressure with minimal effects on cardiovascular and pulmonary parameters. It lowers intraocular pressure by reducing aqueous humor production and increasing uveal-scleral outflow. |
| Molecular Formula |
C9H10CL2N4
|
|---|---|
| Molecular Weight |
245.11
|
| Exact Mass |
244.028
|
| Elemental Analysis |
C, 44.10; H, 4.11; Cl, 28.93; N, 22.86
|
| CAS # |
66711-21-5
|
| Related CAS # |
Apraclonidine hydrochloride;73218-79-8; 73217-88-6
|
| PubChem CID |
2216
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.63g/cm3
|
| Boiling Point |
395.5ºC at 760mmHg
|
| Flash Point |
193ºC
|
| LogP |
2.365
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
15
|
| Complexity |
247
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
NC1=CC(Cl)=C(NC2=NCCN2)C(Cl)=C1
|
| InChi Key |
IEJXVRYNEISIKR-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H10Cl2N4/c10-6-3-5(12)4-7(11)8(6)15-9-13-1-2-14-9/h3-4H,1-2,12H2,(H2,13,14,15)
|
| Chemical Name |
2,6-dichloro-1-N-(4,5-dihydro-1H-imidazol-2-yl)benzene-1,4-diamine
|
| Synonyms |
Apraclonidine HCl; apraclonidine; 66711-21-5; 4-Aminoclonidine; Aplonidine; Apraclonidina; Apraclonidinum; p-aminoclonidine; Apraclonidinum [INN-Latin]; Apraclonidine HCl
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0798 mL | 20.3990 mL | 40.7980 mL | |
| 5 mM | 0.8160 mL | 4.0798 mL | 8.1596 mL | |
| 10 mM | 0.4080 mL | 2.0399 mL | 4.0798 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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