| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Atropine‑d5 targets muscarinic acetylcholine receptors (mAChRs), specifically the M1, M2, M3, M4 and M5 subtypes, acting as a non‑selective competitive antagonist. By blocking the action of acetylcholine at these receptors, atropine inhibits parasympathetic nerve activity, leading to effects such as mydriasis (pupil dilation), reduced salivary and bronchial secretions, increased heart rate and smooth muscle relaxation.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
Atropine‑d5 itself is not typically used in activity assays because the deuterium label is chemically inert and does not alter the pharmacological activity of the parent compound. The non‑deuterated atropine binds to human recombinant mAChRs with high affinity (Ki values: M1 ~0.2‑0.5 nM, M2 ~0.5‑1 nM, M3 ~0.3‑0.6 nM, M4 ~0.5‑1 nM, M5 ~0.3‑0.8 nM). |
| ln Vivo |
Atropine (non‑deuterated) is administered intravenously or intramuscularly to treat bradycardia, reduce salivation and bronchial secretions during surgery, and as an antidote for organophosphate poisoning (e.g., nerve agents). Atropine‑d5 is not administered therapeutically but is used as an internal standard to quantify atropine levels in biological samples from treated animals or humans.
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| Enzyme Assay |
A standard in vitro muscarinic receptor binding assay: Human recombinant mAChR subtypes (M1‑M5) are expressed in CHO or HEK293 cells. Membrane preparations are incubated with 3H‑N‑methylscopolamine (3H‑NMS, 0.2‑1 nM) and increasing concentrations of atropine‑d5 (0.01 nM‑10 uM) in binding buffer (50 mM Tris‑HCl pH 7.4, 5 mM MgCl2, 1 mM EDTA) at 25degC for 60‑120 min. Non‑specific binding is determined in the presence of 10 uM atropine. Bound radioactivity is separated by filtration onto GF/B filters and counted by liquid scintillation. Ki values are calculated from IC50 using the Cheng‑Prusoff equation.
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| Cell Assay |
A general cellular mAChR functional assay (calcium flux): CHO or HEK293 cells stably expressing individual mAChR subtypes (M1, M3, M5 couple to Gq/PLC, increasing intracellular Ca2+; M2, M4 couple to Gi, decreasing cAMP) are loaded with a Ca2+‑sensitive dye (e.g., Fluo‑4 AM). Cells are pre‑treated with atropine‑d5 (0.1‑1000 nM) for 5‑10 min, then stimulated with the mAChR agonist carbachol (EC80 concentration, typically 1‑10 uM). Fluorescence is measured in a plate reader at Ex=488 nm/Em=525 nm. For M2/M4 functional assays, cAMP levels are measured by HTRF after stimulation with carbachol and forskolin. IC50 values for atropine‑d5 are similar to the non‑deuterated form.
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| Animal Protocol |
A general animal protocol for atropine PK study using atropine‑d5 as an internal standard: Male Sprague‑Dawley rats (n=6/group) are administered non‑deuterated atropine sulphate (1 mg/kg, intravenous or intramuscular). Blood samples (0.2‑0.3 mL) are collected from the tail vein or jugular vein at pre‑dose and at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 12 and 24 h post‑dose. Plasma is separated by centrifugation. An aliquot of plasma (50 uL) is spiked with a known amount of atropine‑d5 as the internal standard. After protein precipitation with acetonitrile, atropine and atropine‑d5 are extracted and analysed by LC‑MS/MS in positive ion mode using multiple reaction monitoring (MRM). PK parameters (AUC, Cmax, t½, clearance, volume of distribution) are calculated by non‑compartmental analysis.
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| ADME/Pharmacokinetics |
Atropine‑d5 has identical physicochemical properties to non‑deuterated atropine, with similar absorption, distribution, metabolism and excretion profiles. The deuterium substitution does not significantly alter the PK properties of the parent compound (no kinetic isotope effect for this compound). Atropine has a plasma half‑life of 2‑4 h in humans and rodents, a high volume of distribution (~2‑4 L/kg), and is metabolised primarily by CYP3A4 to tropine and tropic acid. Atropine‑d5 is used as an internal standard to correct for matrix effects and extraction efficiency in LC‑MS/MS bioanalysis.
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| Toxicity/Toxicokinetics |
Atropine (non‑deuterated) has an LD50 of approximately 500 mg/kg (oral) in rats. Human toxic effects include dry mouth, blurred vision, photophobia, tachycardia, urinary retention, constipation, confusion, hallucinations and delirium. Severe toxicity can cause hyperthermia, seizures, respiratory depression and coma. Atropine‑d5 is for research use only; it is not intended for human therapeutic administration. Standard precautions for handling toxic alkaloids (gloves, lab coat, working in a fume hood) should be followed.
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| References | |
| Additional Infomation |
Atropine‑d5 (also known as Tropine tropate‑d5 or DL‑Hyoscyamine‑d5) is a stable isotope‑labeled compound used primarily as an analytical standard. The deuterium atoms are typically incorporated at positions 2, 2, 4, 4, and 6 of the tropine ring or at the methyl group of tropine, depending on the synthesis. Atropine‑d5 is available as a research‑grade chemical and is not approved for clinical use. It is commonly used in forensic toxicology to quantify atropine in post‑mortem samples and in pharmacokinetic studies to support drug development.
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| Molecular Formula |
C17H18D5NO3
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|---|---|
| Molecular Weight |
294.40
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| Related CAS # |
Atropine sulfate monohydrate;5908-99-6
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| Appearance |
Typically exists as solid at room temperature
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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) |
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
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| 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 | 3.3967 mL | 16.9837 mL | 33.9674 mL | |
| 5 mM | 0.6793 mL | 3.3967 mL | 6.7935 mL | |
| 10 mM | 0.3397 mL | 1.6984 mL | 3.3967 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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