| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Laudanosine does not have a specific therapeutic target. Its primary relevance is as a metabolite. It has been shown to interact with various receptors and ion channels, including GABA receptors, where it may act as an antagonist, contributing to its excitatory effects. It may also interact with opioid receptors, though its affinity is low. Its mechanism of action for its excitatory effects is not fully understood but is thought to involve the inhibition of inhibitory neurotransmission.
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|---|---|
| ln Vitro |
In vitro, Laudanosine has been shown to have weak inhibitory effects on acetylcholinesterase and to interact with GABA receptors. It does not have significant neuromuscular blocking activity. Its central nervous system excitatory effects have been observed in animal models. Detailed in vitro potency data are not extensively provided in the referenced sources.
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| ln Vivo |
DL-Laudanosine has been shown to cause awakening from anesthesia at subconvulsive doses and seems to have the unusual capacity to stimulate the brain in animals under mild anesthesia [1]. Male Wistar rats weighing 120–150 grams and male CFLP mice measuring 18–25 grams are used as animal models [2]. 10–20 mg/kg is the dosage. IV. Management. As a result, the rear limbs twitch and stretch.
In vivo, Laudanosine does not produce significant neuromuscular blockade. However, it has been shown to cause central nervous system excitation, including tremors and convulsions, at high doses in animal models. Its accumulation is a concern in patients with renal or hepatic failure receiving atracurium. These effects are dose-dependent. |
| Enzyme Assay |
Non-cell-based assays for Laudanosine are not typical, as it is a metabolite. However, its interaction with receptors can be studied using radioligand binding assays. For example, its affinity for GABA receptors can be assessed using membrane preparations from brain tissue and radiolabeled GABA receptor ligands.
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| Cell Assay |
Cellular assays for Laudanosine are performed using neuronal cell lines or primary neurons to study its effects on neuronal excitability. Cells are treated with the compound, and electrophysiological recordings or calcium imaging are used to measure its effects on neurotransmitter signaling.
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| Animal Protocol |
Animal/Disease Models: Male CFLP mice, weighing 18-25 grams, male Wistar rats, weighing 120-150 grams [2].
Doses: 10-20 mg/kg. Management: IV Experimental Results: Causes twitching and stretching of the hind limbs. In vivo animal models for Laudanosine are used to study its excitatory effects. The compound is administered intravenously or intraperitoneally, and its effects on behavior, such as tremors and seizure activity, are observed. These studies are important for understanding the safety profile of atracurium and its metabolites. |
| ADME/Pharmacokinetics |
Laudanosine has a molecular weight of 357.44 g/mol and a molecular formula of C₂₁H₂₇NO₄. Its CAS number is 1699-51-0. The compound is a solid. Purity is typically ≥98%. It is soluble in DMSO. Storage conditions: -20°C. The compound is supplied for research use only.
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| Toxicity/Toxicokinetics |
Laudanosine is a metabolite with potential central nervous system excitatory effects. It can cause seizures at high doses. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinoline is a member of the isoquinoline class of compounds.
Laudanosine is a tetrahydroisoquinoline alkaloid and a metabolite of atracurium and papaverine. It has central nervous system excitatory effects and can cause seizures. Its CAS number is 1699-51-0. |
| Molecular Formula |
C21H27NO4
|
|---|---|
| Molecular Weight |
357.45
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| Exact Mass |
357.194
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| CAS # |
1699-51-0
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| PubChem CID |
15548
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| Appearance |
White to light yellow solid powder
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| Melting Point |
115℃
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| LogP |
3.43
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
434
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1CCC2=CC(=C(C=C2[C@@H]1CC3=CC(=C(C=C3)OC)OC)OC)OC
|
| InChi Key |
KGPAYJZAMGEDIQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H27NO4/c1-22-9-8-15-12-20(25-4)21(26-5)13-16(15)17(22)10-14-6-7-18(23-2)19(11-14)24-3/h6-7,11-13,17H,8-10H2,1-5H3
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| Chemical Name |
1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinoline
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| Synonyms |
AI3 61890; AI3-61890; Laudanosine
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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 : ~100 mg/mL (~279.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.99 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 25.0 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: ≥ 2.5 mg/mL (6.99 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 25.0 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: ≥ 2.5 mg/mL (6.99 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 | 2.7976 mL | 13.9880 mL | 27.9759 mL | |
| 5 mM | 0.5595 mL | 2.7976 mL | 5.5952 mL | |
| 10 mM | 0.2798 mL | 1.3988 mL | 2.7976 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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