| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 1g |
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| Other Sizes |
| ln Vivo |
In a clinical study involving 20 healthy myopic children (aged 9-12 years), topical administration of 0.05% racanisodamine eye drops (two drops, 5 minutes apart) in one eye caused a biphasic change in pupil size. After an initial, statistically non-significant miosis (minimum diameter at 10 min post-treatment), the pupil underwent significant mydriasis. The peak mydriatic effect occurred at 120 minutes post-treatment, with the mean pupil diameter of the treated eye increasing by 0.75 ± 0.22 mm (from a baseline of 5.83 ± 0.74 mm to 6.58 ± 0.66 mm, p=0.036). Pupil size did not fully return to baseline within the 360-minute observation period. The contralateral untreated eye showed no significant change in pupil size. [1]
Accommodative responses to near targets (at 50, 33, and 20 cm) were measured in the same subjects. The study found that 0.05% racanisodamine eye drops did not cause a statistically significant change in accommodative response in either the treated or the untreated eye at any time point during the 360-minute observation period. [1] Subjective evaluation indicated minimal side effects. Only 1 out of 20 subjects reported tolerable photophobia outdoors in the treated eye at 120 and 180 minutes post-treatment. No subjects reported reading difficulty at any time. [1] |
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| ADME/Pharmacokinetics |
Reference [1] did not provide quantitative pharmacokinetic parameters (e.g., absorption, distribution, metabolism, excretion, half-life, bioavailability) for racanisoldamine. The article states that, based on unpublished observations by the authors, the pharmacological effect of 0.05% racanisoldamine eye drops lasts less than 24 hours. [1]
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| Toxicity/Toxicokinetics |
In clinical studies, 0.05% ricanisodamine eye drops were well tolerated. The main observed side effect was mydriasis, which resulted in photophobia in 1 of 20 subjects (5%), and this symptom was reported to be tolerable and transient. In this study, no other ocular side effects (e.g., significant cycloplegia/accommodative dysfunction, allergic reactions) or systemic side effects (e.g., tachycardia) were reported or observed at the tested doses and formulations. [1] No data on LD₅₀, hepatotoxicity, nephrotoxicity, drug interactions, or plasma protein binding were provided in the literature [1].
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| References | |
| Additional Infomation |
Anisodamine has been investigated for the treatment of intestinal diseases. It has been reported that 6-hydroxy-8-methyl-8-azabicyclo[3.2.1]oct-3-yl-3-hydroxy-2-phenylpropionate is found in scopolia, and relevant data are available. See also: Anisodamine hydrobromide (note moved here). Lacanisodamine is one of the racemic isomers of anisodamine. Anisodamine (C₁₇H₂₃NO₄) is a non-selective muscarinic receptor antagonist extracted from the traditional Chinese medicine Scopolia tangutica Maxim. Compared to atropine, anisodamine has an additional hydroxyl group on the azabicyclo, which increases its polarity and results in a weaker effect on the central nervous system. [1] 0.05% ricanisordamine eye drops were approved by the China Food and Drug Administration in 2006. [1] This study aimed to evaluate the ocular side effects (mydriasis and cycloplegia) of 0.05% ricanisordamine eye drops (a potential myopia control drug) and compare them with the known side effects of atropine. [1] The authors concluded that 0.05% ricanisordamine had a significant but clinically moderate effect on pupil size and no effect on accommodative response in children. [1]
|
| Molecular Formula |
C17H23NO4
|
|---|---|
| Molecular Weight |
305.3688
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| Exact Mass |
305.162
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| CAS # |
17659-49-3
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| PubChem CID |
2198
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
474.6±45.0 °C at 760 mmHg
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| Flash Point |
240.8±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.600
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| LogP |
0.25
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
396
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
WTQYWNWRJNXDEG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H23NO4/c1-18-12-7-13(9-15(18)16(20)8-12)22-17(21)14(10-19)11-5-3-2-4-6-11/h2-6,12-16,19-20H,7-10H2,1H3
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| Chemical Name |
(6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 3-hydroxy-2-phenylpropanoate
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| Synonyms |
Racanisodamine
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~61 mg/mL (~199.8 mM)
Ethanol: ~61 mg/mL Water: ~30 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2747 mL | 16.3736 mL | 32.7472 mL | |
| 5 mM | 0.6549 mL | 3.2747 mL | 6.5494 mL | |
| 10 mM | 0.3275 mL | 1.6374 mL | 3.2747 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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