| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
In adrenocortical cell suspensions, medetomidine (0–1 µM, 1 hour) suppresses the release of aldosterone [7]. Cyprids' kicking reaction is activated by 10 nM metetomidine [8]. By stimulating beta-like receptors in CHO cells, metetomidine (1 µM) raises the amount of cAMP produced by the cells [8].
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| ln Vivo |
Cats may get drowsy when given metetomidine (200 μg/kg orally or intramuscularly) [4]. Dogs respond sedatively and analgesically to intravenous medetomidine (20 µg/kg) [5]. In mice, diazinon-induced poisoning can be avoided using metetomidine (0.05–0.3 mg/kg, subcutaneous injection) [6].
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| Animal Protocol |
Animal/Disease Models: Diazinon (75 mg/kg, oral) induced poisoning in mice [6] Doses: 0.05, 0.1 and 0.3 mg/kg
Route of Administration: subcutaneous injection, 15 minutes before diazinon. Experimental Results: Mice were protected from diazinon-induced toxicity. Reduces the occurrence of strew tail, hypersalivation and tremors. The latency to onset of tremor and death was increased compared with controls. Animal/Disease Models: dog [5] Doses: 20 µg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results:It has sedative and analgesic effects. SAP, MAP, DAP, MPAP, PCWP, CVP, SVR, PVR, increased core body temperature. HR, CO, CI, SV, SI, RR, pH diminished. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Limited data indicate that very small amounts of dexmedetomidine are excreted into breastmilk for 4 to 6 hours after the end of an intravenous infusion. The drug is absent from breastmilk by 24 hours after the end of an infusion. The amounts in milk after sublingual use are expected to be less than after intravenous infusion. Because of the low dose in milk and its poor oral bioavailability, dexmedetomidine would not be expected to cause adverse effects in breastfed infants or neonates. Monitor the breastfed infant for irritability during sublingual use. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk A double-blind study randomized 160 women receiving an elective cesarean section under spinal anesthesia to receive either sufentanil for patient-controlled intravenous analgesia (standard care) or standard care plus dexmedetomidine. Dexmedetomidine was given as 5 mcg/kg, followed by a continuous infusion of 0.5 mcg/kg per hour until the end of surgery. Patient in this latter group received dexmedetomidine plus sufentanil for patient-controlled intravenous analgesia postoperatively for 2 days. Patients who received dexmedetomidine had a shorter time to the first lactation (28 vs 34 hours), achieved exclusive breastfeeding sooner (8 vs 11 days) and had a greater amount of milk on the second day postpartum. In a retrospective study of women undergoing cesarean section deliveries, 3 regimens were compared: dexmedetomidine before anesthesia and during delivery (n = 115), normal saline before anesthesia and during delivery and dexmedetomidine after delivery (n = 109), and normal saline before anesthesia and during delivery (n = 168). Women who received dexmedetomidine before anesthesia and during delivery consumed less sufentanil and ondansetron during their hospitalization and had a slightly shorter time to the first production of milk than women in the other groups (25 minutes vs 27 to 28 minutes). |
| References | |
| Additional Infomation |
Medetomidine is a member of imidazoles.
Medetomidine is a synthetic compound used as a surgical anesthetic and analgesic. It is normally found as its hydrochloride salt, medetomidine hydrochloride. Medetomidine is an intravenously available alpha-2 adrenergic agonist. The drug has been developed by Orion Pharma. In the United States, it is currently approved for its veterinary use in dogs and distributed by Pfizer Animal Health. In Canada, medetomidine is distributed by Novartis Animal Health. The marketed product is a racemic mixture of two stereoisomers from which dexmedetomidine is the main active isomer. An agonist of RECEPTORS, ADRENERGIC ALPHA-2 that is used in veterinary medicine for its analgesic and sedative properties. It is the racemate of DEXMEDETOMIDINE. See also: Medetomidine Hydrochloride (has salt form). |
| Molecular Formula |
C13H16N2
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|---|---|
| Molecular Weight |
200.2795
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| Exact Mass |
200.131
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| CAS # |
86347-14-0
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| Related CAS # |
Dexmedetomidine;113775-47-6;Dexmedetomidine hydrochloride;145108-58-3;Medetomidine hydrochloride;86347-15-1
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| PubChem CID |
68602
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
381.9±11.0 °C at 760 mmHg
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| Melting Point |
151.5 - 152.5ºC
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| Flash Point |
191.3±5.7 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.570
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
205
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CUHVIMMYOGQXCV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H16N2/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13/h4-8,11H,1-3H3,(H,14,15)
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| Chemical Name |
5-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole
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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 : ~250 mg/mL (~1248.25 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.48 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 (12.48 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 (12.48 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 | 4.9930 mL | 24.9650 mL | 49.9301 mL | |
| 5 mM | 0.9986 mL | 4.9930 mL | 9.9860 mL | |
| 10 mM | 0.4993 mL | 2.4965 mL | 4.9930 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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