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| Targets |
Norbormide's mechanism of action involves the inhibition of signal transduction pathways, specifically the mitogen-activated protein kinase (MAPK) pathway. It also acts as a vasoconstrictor by blocking calcium channels. Norbormide's vasoconstrictor activity is species- and tissue-specific; it is endothelium-independent and limited to peripheral arteries of the rat. This selective vasoconstriction in rats is the basis for its use as a rodenticide. The compound's ability to block calcium channels leads to vasoconstriction, which can cause ischemia and death in target species. Its specificity for rat peripheral arteries makes it less toxic to other species, although it does show some toxicity to mice, hamsters, guinea pigs, and rabbits.
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| ln Vitro |
In vitro studies have characterized Norbormide's vasoconstrictor activity. Its activity is typically measured using isolated blood vessel preparations. In a typical assay, rat peripheral arteries (e.g., mesenteric or tail arteries) are mounted in a wire myograph, and the isometric tension is measured. Norbormide is added at various concentrations, and the contractile response is recorded. The compound induces vasoconstriction in a concentration-dependent manner. The effect is endothelium-independent, meaning it does not require the presence of the endothelial layer. The vasoconstrictor activity is specific to rat arteries and is not observed in arteries from other species or in other types of blood vessels. These in vitro studies confirm Norbormide's species- and tissue-specific vasoconstrictor activity.
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| ln Vivo |
In vivo studies have demonstrated Norbormide's efficacy as a rodenticide. When administered to rats, Norbormide causes vasoconstriction of peripheral arteries, leading to ischemia and death. The compound's oral LD50 in rats is not specified in the available literature, but it is effective at doses that are lethal to rats. Its toxicity to other species varies, with oral LD50 values of 2250, 140, 620, and 1000 mg/kg in mice, hamsters, guinea pigs, and rabbits, respectively. These differences in toxicity contribute to its selectivity as a rodenticide. Norbormide is used in pest control to manage rat populations.
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| Enzyme Assay |
The in vitro assays for Norbormide measure its vasoconstrictor activity. In a typical assay, isolated rat peripheral arteries (e.g., mesenteric arteries) are mounted in a wire myograph. The arteries are bathed in a physiological salt solution and equilibrated under tension. Norbormide is added cumulatively to the bath, and the isometric tension is recorded. The concentration-response curve is generated, and the EC50 is determined. To confirm the mechanism of action, the effect of calcium channel blockers or other modulators can be tested. The endothelium dependence is assessed by comparing the response in arteries with and without an intact endothelium. These assays provide a quantitative measure of Norbormide's vasoconstrictor activity.
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| Cell Assay |
In vitro cell-based assays for Norbormide are used to study its effects on calcium signaling and cell viability. In a typical assay, vascular smooth muscle cells are isolated from rat arteries and cultured. The cells are loaded with a calcium-sensitive dye (e.g., Fura-2), and the intracellular calcium concentration is measured upon Norbormide addition. The compound's ability to increase intracellular calcium is assessed. Cell viability assays, such as MTT or LDH release, can be used to measure the cytotoxic effects of Norbormide on vascular smooth muscle cells. These cell-based assays confirm that Norbormide modulates calcium signaling in vascular smooth muscle cells.
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| Animal Protocol |
In vivo animal experiments for Norbormide are conducted to evaluate its efficacy as a rodenticide and its toxicity to other species. In a typical efficacy study, rats are administered Norbormide orally at various doses, and mortality is recorded. The LD50 is determined. For toxicity studies, other species (e.g., mice, hamsters, guinea pigs, rabbits) are administered Norbormide, and the LD50 is determined for each species. The selectivity of Norbormide for rats over other species is assessed by comparing the LD50 values. These studies are essential for characterizing the toxicological profile of Norbormide and for its use as a rodenticide.
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| ADME/Pharmacokinetics |
Norbormide has a molecular weight of 511.6 g/mol and a molecular formula of C33H25N3O3. It is a solid compound. Norbormide is practically insoluble in water unless the pH is below 4. Its solubility at room temperature is 60 mg/L in water, 14 mg/L in ethanol, >150 mg/L in chloroform, 1 mg/L in diethyl ether, and 29 mg/L in 0.1 M hydrochloric acid (all at 30 °C). For storage, it is recommended to keep the compound in a dry, dark environment. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have been studied in the context of its use as a rodenticide. Norbormide is absorbed after oral administration and is distributed to various tissues.
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| Toxicity/Toxicokinetics |
Non-Human Toxicity Values
Oral LD50 in rats: 5.3 mg/kg Intravenous LD50 in rats: 0.65 mg/kg Oral LD50 in Norwegian rats: 5.3-15.0 mg/kg (wild and domestic) Oral LD50 in roof rats: 52 mg/kg For more complete non-human toxicity data on NORBORMIDE (9 in total), please visit the HSDB records page. Norbormide is a toxic compound. It is moderately to highly toxic to humans, with a probable human lethal dose of 50 to 500 mg/kg. Its toxicity to other species varies, with oral LD50 values of 2250, 140, 620, and 1000 mg/kg in mice, hamsters, guinea pigs, and rabbits, respectively. The toxicity of Norbormide is primarily due to its vasoconstrictor activity, which can lead to ischemia and tissue damage. In humans, exposure to Norbormide can cause vasoconstriction, hypertension, and other cardiovascular effects. As a rodenticide, it should be handled with extreme caution, and appropriate safety measures should be taken to avoid exposure. |
| Additional Infomation |
Norbormide is a colorless to off-white crystalline powder used as a selective rodenticide. (EPA, 1998)
Norbormide is a sesquiterpene compound. Mechanism of Action Differences in peripheral vascular responses to Norbormide in different species appear to be the primary cause of species-specific toxicity variations. This compound causes extreme, irreversible vasoconstriction in experimental rats, which is believed to be the cause of death. …Oral or intraperitoneal administration of a dose of 1020 mg/kg doubled blood glucose levels in rats, decreased liver and muscle glycogen content, and caused coma 0.5–2 hours after administration. The same dose had no effect on blood glucose levels in either strain of mice, nor did it cause disease. Insulin antagonized the hyperglycemia induced by Norbormide in rats but did not prevent toxicity and death, suggesting that hyperglycemia is secondary… Norbormide is a rodenticide used for the control of rat populations. It is a bicyclic compound that acts as a vasoconstrictor by blocking calcium channels. Norbormide's activity is species- and tissue-specific, endothelium-independent, and limited to peripheral arteries of the rat. This selective vasoconstriction in rats is the basis for its use as a rodenticide. Its toxicity to other species varies, with oral LD50 values of 2250, 140, 620, and 1000 mg/kg in mice, hamsters, guinea pigs, and rabbits, respectively. Norbormide is a research compound and a rodenticide, and it is not approved for human use. Its mechanism of action involves the inhibition of signal transduction pathways, specifically the MAPK pathway, and the blocking of calcium channels. |
| Molecular Formula |
C33H25N3O3
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|---|---|
| Molecular Weight |
511.581
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| Exact Mass |
511.19
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| CAS # |
991-42-4
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| Related CAS # |
63907-08-4 (mono-hydrochloride)
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| PubChem CID |
13814
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| Appearance |
CRYSTALS FROM METHYLENE CHLORIDE + ETHER
COLORLESS TO OFF-WHITE CRYSTALLINE POWDER White solid White crystals |
| Density |
1.346g/cm3
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| Boiling Point |
780.539ºC at 760 mmHg
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| Melting Point |
190-198ºC
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| Flash Point |
>230 °F
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| Index of Refraction |
1.69
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| LogP |
4.618
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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 |
39
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| Complexity |
1040
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C(=C2C3C=C(C2C4C3C(=O)NC4=O)C(C5=CC=CC=C5)(C6=CC=CC=N6)O)C7=CC=CC=N7
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| InChi Key |
DNTHHIVFNQZZRD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H25N3O3/c37-31-28-22-19-23(33(39,21-13-5-2-6-14-21)25-16-8-10-18-35-25)29(30(28)32(38)36-31)27(22)26(20-11-3-1-4-12-20)24-15-7-9-17-34-24/h1-19,22,28-30,39H,(H,36,37,38)
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| Chemical Name |
8-(hydroxy-phenyl-pyridin-2-ylmethyl)-10-[phenyl(pyridin-2-yl)methylidene]-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione
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| Synonyms |
Norbormide Mcneil 1025 S 6999 S-6,999Raticate Shoxin MCN 1025
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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 | 1.9547 mL | 9.7736 mL | 19.5473 mL | |
| 5 mM | 0.3909 mL | 1.9547 mL | 3.9095 mL | |
| 10 mM | 0.1955 mL | 0.9774 mL | 1.9547 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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