Medetomidine |
カタログ番号GC13144
One-Click Copy Product Info
|
Medetomidine is a potent and selective agonist of α2-adrenoceptors, with a Ki value of 1.08nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 86347-14-0
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Medetomidine is a potent and selective agonist of α2-adrenoceptors, with a Ki value of 1.08nM[1]. By inhibiting sympathetic nerve tension in the central nervous system, Medetomidine produces a series of characteristic pharmacological effects, such as hypotension, bradycardia, sedation, relief of anxiety, analgesia, and hypothermia[2]. Medetomidine has been widely used as a sedative to induce anaesthesia in animal models[3].
In vitro, 0.1µM of Medetomidine incubated for 1 hour significantly inhibited the release of aldosterone by porcine adrenocortical cells and inhibited mitochondrial cytochrome P45011β/18[4]. Treatment with 1ng/ml of Medetomidine for 1 hour significantly increased the contraction frequency and amplitude of human uterine muscle layers[5].
In vivo, Medetomidine treatment via a single intraperitoneal injection at a dose of 50μg/kg resulted in a decrease in plasma insulin concentration and an increase in plasma glucose concentration in C57BL/6 mice after 45 minutes[6]. Long-term exposure of rainbow trout (Oncorhynchus mykiss) to 5nM Medetomidine in water for 54 days resulted in pale body coloration and melanocyte aggregation[7].
References:[1] de Andrade Horn P, Berida T I, Parr L C, et al. Classics in chemical neuroscience: medetomidine[J]. ACS Chemical Neuroscience, 2024, 15(21): 3874.
[2] Virtanen R. Pharmacological profiles of medetomidine and its antagonist, atipamezole[J]. Acta Veterinaria Scandinavica. Supplementum, 1989, 85: 29-37.
[3] Sood N. Rise of illicit medetomidine use: A worrisome trend[J]. The American Journal on Addictions, 2025, 34(5): 558-561.
[4] Jager L P, De Graaf G J, Widjaja-Greefkes H C A. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro[J]. European journal of pharmacology, 1998, 346(1): 71-76.
[5] Sia A T, Kwek K, Yeo G S. The in vitro effects of clonidine and dexmedetomidine on human myometrium[J]. International journal of obstetric anesthesia, 2005, 14(2): 104-107.
[6] Guedes A G P, Rude E P, Kannan M S. Potential role of the CD 38/cADPR signaling pathway as an underlying mechanism of the effects of medetomidine on insulin and glucose homeostasis[J]. Veterinary anaesthesia and analgesia, 2013, 40(5): 512-516.
[7] Lennquist A, Lindblad L G E M, Hedberg D, et al. Colour and melanophore function in rainbow trout after long term exposure to the new antifoulant medetomidine[J]. Chemosphere, 2010, 80(9): 1050-1055.
| Cell experiment [1]: | |
|
Cell lines |
Porcine adrenocortical cells |
|
Preparation Method |
Porcine adrenocortical cells were kept suspended overnight in RPMI 1640 medium (about 1×106 cells/ml) at 4°C. The next morning, the cells were transferred to fresh RPMI 1640 medium. The cell suspension was usually prepared in a day, and the experiment was started the next morning. Throughout the experiments, cell suspensions of 1×106 cells/ml were used. All incubations were done at 37±0.5°C in a shaking water bath. RPMI 1640 medium with 1μM substrate (deoxycorticosterone) was used to preincubate the cell suspension for 30min. Usually, incubations of 1h were used with fresh RPMI 1640 medium, 1μM deoxycorticosterone, and different concentrations of Medetomidine (0, 10, 33, 100, 333, and 1000nM). Effects of the Medetomidine on aldosterone release from the adrenocortical cell suspension was detected. |
|
Reaction Conditions |
0, 10, 33, 100, 333, and 1000nM; 1h |
|
Applications |
Medetomidine treatment reduced aldosterone release from porcine adrenocortical cells in a dose-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
C57BL/6J wild-type mice |
|
Preparation Method |
C57BL/6J wild-type mice were housed in a 12-hour light-dark schedule with food and water available ad libitum. Mice received Medetomidine (50μg/kg) or a similar volume of 0.9% NaCl (each group; n=8) by intraperitoneal injection and were euthanized 45 minutes later with an intraperitoneal injection of sodium pentobarbital (180mg/kg). Food and water were not withheld prior to the experiments. Blood (approximately 1.0ml) was collected immediately after euthanasia for analysis. |
|
Dosage form |
50μg/kg; once; i.p. |
|
Applications |
Medetomidine treatment decreased plasma insulin concentrations and increased plasma glucose in mice. |
| References: [1] Jager L P, De Graaf G J, Widjaja-Greefkes H C A. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones by porcine adrenocortical cells in vitro[J]. European journal of pharmacology, 1998, 346(1): 71-76. [2] Guedes A G P, Rude E P, Kannan M S. Potential role of the CD 38/cADPR signaling pathway as an underlying mechanism of the effects of medetomidine on insulin and glucose homeostasis[J]. Veterinary anaesthesia and analgesia, 2013, 40(5): 512-516. | |
| Cas No. | 86347-14-0 | SDF | |
| Chemical Name | 5-(1-(2,3-dimethylphenyl)ethyl)-1H-imidazole | ||
| Canonical SMILES | CC1=C(C)C(C(C2=CN=CN2)C)=CC=C1 | ||
| Formula | C13H16N2 | M.Wt | 200.28 |
| 溶解度 | DMSO : 250 mg/mL (1248.25 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.993 mL | 24.965 mL | 49.9301 mL |
| 5 mM | 998.6 μL | 4.993 mL | 9.986 mL |
| 10 mM | 499.3 μL | 2.4965 mL | 4.993 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)