Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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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. |
References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
[2]. Kallio A, et al. Acute effects of medetomidine, a selective alpha 2-adrenoceptor agonist, on anterior pituitary hormone and cortisol secretion in man. Acta Endocrinol (Copenh). 1988 Sep;119(1):11-5. [3]. R Virtanen, et al. Characterization of the selectivity, specificity and potency of medetomidine as an a2-adrenoceptor agonist. [4]. O. B. Ansah, et al. Comparing oral and intramuscular administration of medetomidine in cats. [5]. Kuo WC, et al. Comparative cardiovascular, analgesic, and sedative effects of medetomidine, medetomidine-hydromorphone, and medetomidine-butorphanol in dogs. Am J Vet Res. 2004 Jul;65(7):931-7. [6]. Yakoub LK, et al. Medetomidine protection against diazinon-induced toxicosis in mice. Toxicol Lett. 1997 Sep 19;93(1):1-8. [7]. Jager LP, et al. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro. Eur J Pharmacol. 1998 Apr 3;346(1):71-6. [8]. Ulrika Lind, et al. Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine. |
Molecular Formula |
C13H16N2
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Molecular Weight |
200.2795
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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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SMILES |
N1([H])C([H])=NC([H])=C1C([H])(C([H])([H])[H])C1=C([H])C([H])=C([H])C(C([H])([H])[H])=C1C([H])([H])[H]
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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 |
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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.