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Anisodamine is a ntural product extracted from Chinese solanacea plant, acting as a weak inhibitor/antagonist of alpha-1 adrenergic receptors and mAChRs.
| Targets |
Nicotinic cholinoceptor
|
|---|---|
| ln Vitro |
Anisodamine pretreatment (100 μg/mL; 20 minutes; RAW264.7 cells) significantly attenuates the average fluorescence intensity of α-bungarotoxin binding compared to Ach alone[2].
Anisodamine may act by blocking muscarinic receptors, which in turn increases the amount of endogenous ACh that binds to the α-7nAChR[2]. |
| ln Vivo |
Anisodamine (50 mg/kg; intraperitoneally; 72 hours) significantly lowers mortality to 20%[2].
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| Animal Protocol |
LPS-Induced Shock Mice
50 mg/kg I.p. |
| References |
| Molecular Formula |
C17H23NO4
|
|---|---|
| Molecular Weight |
305.36882
|
| Exact Mass |
305.16
|
| Elemental Analysis |
C, 66.86; H, 7.59; N, 4.59; O, 20.96
|
| CAS # |
55869-99-3
|
| Related CAS # |
Anisodamine hydrobromide; 55449-49-5; Anisodamine hydrochloride; 131674-05-0
|
| Appearance |
Solid powder
|
| SMILES |
CN1[C@H]2C[C@@H](C[C@@H]1[C@H](C2)O)OC(=O)[C@H](CO)C3=CC=CC=C3
|
| InChi Key |
WTQYWNWRJNXDEG-RBZJEDDUSA-N
|
| 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/t12-,13-,14+,15+,16-/m0/s1
|
| Chemical Name |
[(1R,3S,5R,6S)-6-hydroxy-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] (2S)-3-hydroxy-2-phenylpropanoate
|
| Synonyms |
6-Hydroxy hyoscyamine; 654 II; 654-II; 654II
|
| 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) |
DMSO: ≥ 100 mg/mL (~327.5 mM)
H2O: ~20 mg/mL (~65.5 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.19 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 (8.19 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 (8.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (163.74 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05634057 | Completed | Drug: Anisodamine hydrobromide combined with heparin |
Sepsis | Chen Ying | January 11, 2024 | Not Applicable |
| NCT06045364 | Not yet recruiting | Drug: Glycopyrrolate Drug: Anisodamine |
PIK3CA E545A | Jie Chen | October 1, 2023 | Phase 1 Phase 2 |
| NCT05727163 | Recruiting | Drug: Amisulpride Drug: Olanzapine |
BPSD Amisulpride |
Tianjin Anding Hospital | December 1, 2019 | Not Applicable |
| NCT05822713 | Recruiting | Drug: Anisodamine Drug: Anisodamine |
Colorectal Cancer Metastatic | Sun Yat-sen University | July 29, 2022 | Phase 2 |
| NCT01929044 | Completed | Drug: 654-II (anisodamine) Drug: Buscopan® (hyoscine butylbromide) |
Intestinal Diseases | Boehringer Ingelheim | Phase 3 | August 2013 |
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