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Medetomidine HCl (MPV-785; MPV 785; MPV785; Precedex. Domitor; Selektope) is a selective and synthetic α2-adrenoceptor agonist with analgesic and anesthetic effects. It demonstrates 1620-fold selectivity over α1-adrenoceptor and activates α2-adrenoceptor with a Ki of 1.08 nM. The use of medetomidine as an analgesic and surgical anesthetic has been approved. It is an intravenous drug solution containing sterile water that can be used as an alpha-2 adrenergic agonist. A racemic mixture of two stereoisomers, medetomidine is now sold under the brand name Dexdomitor; the more beneficial isomer is dexmedetomidine.
Physicochemical Properties
| Molecular Formula | C13H17CLN2 | |
| Molecular Weight | 236.74 | |
| Exact Mass | 236.108 | |
| Elemental Analysis | C, 65.95; H, 7.24; Cl, 14.97; N, 11.83 | |
| CAS # | 86347-15-1 | |
| Related CAS # | Dexmedetomidine; 113775-47-6; Medetomidine; 86347-14-0; Dexmedetomidine hydrochloride; 145108-58-3; Medetomidine-d3 hydrochloride; 1246820-20-1 | |
| PubChem CID | 68601 | |
| Appearance | White to off-white solid powder | |
| Boiling Point | 381.9ºC at 760 mmHg | |
| Melting Point | 164-166°C | |
| Flash Point | 191.3ºC | |
| LogP | 3.98 | |
| Hydrogen Bond Donor Count | 2 | |
| Hydrogen Bond Acceptor Count | 1 | |
| Rotatable Bond Count | 2 | |
| Heavy Atom Count | 16 | |
| Complexity | 205 | |
| Defined Atom Stereocenter Count | 0 | |
| SMILES | Cl.N1C=C(C(C)C2C(C)=C(C)C=CC=2)NC=1 |
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| InChi Key | VPNGEIHDPSLNMU-UHFFFAOYSA-N | |
| InChi Code | InChI=1S/C13H16N2.ClH/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);1H | |
| Chemical Name | 5-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole;hydrochloride | |
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| HS Tariff Code | 2934.99.9001 | |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | α2-adrenergic receptor ( Ki = 1.08 nM ); α1-adrenergic receptor ( Ki = 1750 nM ) | |
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| References |
[1]. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. 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]. Characterization of the selectivity, specificity and potency of medetomidine as an a2-adrenoceptor agonist. [4]. Comparing oral and intramuscular administration of medetomidine in cats. [5]. 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]. Medetomidine protection against diazinon-induced toxicosis in mice. Toxicol Lett. 1997 Sep 19;93(1):1-8. [7]. 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]. Octopamine receptors from the barnacle balanus improvisus are activated by the alpha2-adrenoceptor agonist medetomidine. |
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| Additional Infomation |
Medetomidine hydrochloride is a hydrochloride. 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 (has active moiety) ... View More ... |
Solubility Data
| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.56 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 (10.56 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. Solubility in Formulation 4: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% EtOH + 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 EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 5: ≥ 2.5 mg/mL (10.56 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (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 EtOH stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: Saline: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2240 mL | 21.1202 mL | 42.2404 mL | |
| 5 mM | 0.8448 mL | 4.2240 mL | 8.4481 mL | |
| 10 mM | 0.4224 mL | 2.1120 mL | 4.2240 mL |