Medetomidine

α2-adrenoceptor agonist CAS# 86347-14-0

Medetomidine

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Chemical structure

Medetomidine

3D structure

Chemical Properties of Medetomidine

Cas No. 86347-14-0 SDF Download SDF
PubChem ID 68602 Appearance Powder
Formula C13H16N2 M.Wt 200.28
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 100 mg/mL (499.30 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 5-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole
SMILES CC1=C(C(=CC=C1)C(C)C2=CN=CN2)C
Standard InChIKey CUHVIMMYOGQXCV-UHFFFAOYSA-N
Standard InChI 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)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Medetomidine Dilution Calculator

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Medetomidine Molarity Calculator

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Preparing Stock Solutions of Medetomidine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.993 mL 24.965 mL 49.9301 mL 99.8602 mL 124.8252 mL
5 mM 0.9986 mL 4.993 mL 9.986 mL 19.972 mL 24.965 mL
10 mM 0.4993 mL 2.4965 mL 4.993 mL 9.986 mL 12.4825 mL
50 mM 0.0999 mL 0.4993 mL 0.9986 mL 1.9972 mL 2.4965 mL
100 mM 0.0499 mL 0.2497 mL 0.4993 mL 0.9986 mL 1.2483 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Medetomidine

Medetomidine is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively). Medetomidine displays greater selectivity over α1-adrenoceptors than clonidine and UK 14,304 (1620-, 220- and 300-fold respectively). Medetomidine inhibits twitch response in electrically stimulated mouse vas deferens (pD2 = 9.0). Active in vivo; displays hypotensive, bradycardic, sedative, anxiolytic, hypothermic and analgesic effects.

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References on Medetomidine

Evaluation of BAM (butorphanol-azaperone-medetomidine) in captive African lion (Panthera leo) immobilization.[Pubmed:28330727]

Vet Anaesth Analg. 2017 Jul;44(4):883-889.

OBJECTIVE: The combination of butorphanol, azaperone and Medetomidine (BAM) with subsequent antagonism by naltrexone-yohimbine or naltrexone-atipamezole was evaluated for reversible immobilization of captive African lions (Panthea leo). STUDY DESIGN: Prospective, clinical trial. ANIMALS: Twenty lions, 11 males and nine females, weighing 38-284 kg were immobilized in South Africa. METHODS: The BAM volume dose rate administered was 0.005-0.008 mL kg(-1) (0.6 mL 100 kg(-1)). Physiologic variables were recorded every 5 minutes. Four arterial blood samples were collected from all animals at 20, 30, 40 and 50 minutes after immobilization for analysis of blood-gases and acid-base status. RESULTS: The actual doses administered were as follows: butorphanol, 0.18+/-0.03 mg kg(-1); azaperone, 0.07+/-0.01 mg kg(-1); and Medetomidine, 0.07+/-0.01 mg kg(-1). The inductions were calm and smooth, and induction time ranged from 4 to 10 minutes (7+/-2 minutes). The amount of time needed to work with each lion was 70 minutes, and no additional drug doses were needed. Heart rate (40+/-8 beats minute(-1)) and respiratory frequency (15+/-4 breaths minute(-1)) were stable throughout immobilization. The mean arterial blood pressure of all animals was stable but elevated (142+/-16 mmHg). The rectal temperature slightly increased over time but remained within acceptable range. The recovery time was significantly shorter when using naltrexone and atipamezole (9+/-1 minutes) compared to using naltrexone and yohimbine (22+/-7 minutes). CONCLUSION AND CLINICAL RELEVANCE: The BAM combination proved to be reliable for general veterinary anaesthesia in lions. During anaesthesia, minor veterinary procedures such a blood collection, intubation, vaccination and collaring could safely be performed with no additional dosing required.

CONTINUOUS INTRAVENOUS INFUSION ANESTHESIA WITH MEDETOMIDINE, KETAMINE, AND MIDAZOLAM AFTER INDUCTION WITH A COMBINATION OF ETORPHINE, MEDETOMIDINE, AND MIDAZOLAM OR WITH MEDETOMIDINE, KETAMINE, AND BUTORPHANOL IN IMPALA (AEPYCEROS MELAMPUS).[Pubmed:28363076]

J Zoo Wildl Med. 2017 Mar;48(1):62-71.

In order to develop a long-term anesthesia for flighty antelope species in field situations, two different protocols for induction and maintenance with an intravenous infusion were evaluated in wild-caught impala ( Aepyceros melampus ). Ten adult female impala were induced with two induction protocols: one consisted of 0.2 mg/kg Medetomidine, 4 mg/kg ketamine, and 0.15 mg/kg butorphanol (MKB) and one consisted of 0.375 mg/kg etorphine, 0.2 mg/kg Medetomidine, and 0.2 mg/kg midazolam (EMM). In both treatments, anesthesia was maintained with a continuous intravenous infusion (CII) at an initial dose rate of 1.2 mug/kg per hr Medetomidine, 2.4 mg/kg per hr ketaminen and 36 mug/kg per hr midazolam. Partial reversal was achieved with naltrexone (2 : 1 mg butorphanol; 20 : 1 mg etorphine) and atipamezole (5 : 1 mg Medetomidine). Evaluation of anesthesia included respiratory rate, heart rate, rectal temperature, arterial blood pressure, oxygen saturation, end tidal carbon dioxide tension, and tidal volume at 5-min intervals, palpebral reflex and response to painful stimuli at 15-min intervals, and arterial blood gases at 30-min intervals. Plasma cortisol concentration was determined after induction and before reversal. Duration and quality of induction and recovery were evaluated. EMM caused a faster induction of 9.5 +/- 2.9 min compared to 11.0 +/- 6.4 min in MKB. Recovery was also quicker in EMM (EMM: 6.3 +/- 5.4 min; MKB: 9.8 +/- 6.0 min). However, EMM also produced more cardiopulmonary side effects, including hypoxemia and hypercapnia, and calculated oxygenation indices (PaCO2-PETCO2) were worse than in MKB. One animal died after induction with EMM. The CII provided surgical anesthesia in 7 of 10 animals in MKB and in 9 of 9 animals in EMM for 120 min. In conclusion, the MKB induction protocol had advantages for prolonged anesthesia in impala with significantly less cardiopulmonary depression compared to EMM. The comparably decreased anesthetic depth could easily be adjusted by an increase of the CII.

Immobilization of Asiatic Black Bears ( Ursus thibetanus ) with Medetomidine-Zolazepam-Tiletamine in South Korea.[Pubmed:28323561]

J Wildl Dis. 2017 Jul;53(3):636-641.

The Asiatic black bear ( Ursus thibetanus ; ABB) is a globally endangered species for which a restoration program has been ongoing in South Korea since 2001. However, there is little information on immobilization protocols for ABBs. We evaluated the use of Medetomidine-zolazepam-tiletamine for their immobilization. During 2005-13, we anesthetized 60 ABBs (32 males, 28 females; 7 mo to 12 yr old) with Medetomidine 0.03-0.045 mg/kg and zolazepam-tiletamine 1.54-2.3 mg/kg; reversal of anesthesia was done with atipamezole 0.15-0.225 mg/kg administered intravenously alone or intravenously and intramuscularly (50:50). Mean (and SD) for physiologic collected for 373 immobilizations of at least 60 min were: time to sedation, 7.8 (5.4) min; anesthesia induction time, 13.7 (8.1) min; complete recovery time, 14.8 (12.4) min; respiratory rate, 14 (7) breaths/min; heart rate, 51 (16) beats/min; rectal temperature, 37.3 (1.3) C; and hemoglobin oxygen saturation, 88% (6%). Few cardiopulmonary side effects occurred during immobilization and adequate depth of anesthesia was maintained for >60 min without need for supplementation. The dosage and drug combination used was effective for immobilization of ABBs with minimal adverse effects on vital signs and can be recommended in most clinical applications.

Repeated anaesthesia with isoflurane and medetomidine-midazolam-fentanyl in guinea pigs and its influence on physiological parameters.[Pubmed:28328950]

PLoS One. 2017 Mar 22;12(3):e0174423.

Repeated anaesthesia may be required in experimental protocols and in daily veterinary practice, but anaesthesia is known to alter physiological parameters in GPs (Cavia porcellus, GPs). This study investigated the effects of repeated anaesthesia with either Medetomidine-midazolam-fentanyl (MMF) or isoflurane (Iso) on physiological parameters in the GP. Twelve GPs were repeatedly administered with MMF or Iso in two anaesthesia sets. One set consisted of six 40-min anaesthesias, performed over 3 weeks (2 per week); the anaesthetic used first was randomized. Prior to Iso anaesthesia, atropine was injected. MMF anaesthesia was antagonized with AFN (atipamezole-flumazenil-naloxone). Abdominally implanted radio-telemetry devices recorded the mean arterial blood pressure (MAP), heart rate (HR) and core body temperature continuously. Additionally, respiratory rate, blood glucose and body weight were assessed. An operable state could be achieved and maintained for 40 min in all GPs. During the surgical tolerance with MMF, the GPs showed a large MAP range between the individuals. In the MMF wake- up phase, the time was shortened until the righting reflex (RR) returned and that occurred at lower MAP and HR values. Repeated Iso anaesthesia led to an increasing HR during induction (anaesthesias 2-6), non-surgical tolerance (anaesthesias 3-6) and surgical tolerance (anaesthesias 4, 6). Both anaesthetics may be used repeatedly, as repeating the anaesthesias resulted in only slightly different physiological parameters, compared to those seen with single anaesthesias. The regular atropine premedication induced HR increases and repeated MMF anaesthesia resulted in a metabolism increase which led to the faster return of RR. Nevertheless, Iso's anaesthesia effects of strong respiratory depression and severe hypotension remained. Based on this increased anaesthesia risk with Iso, MMF anaesthesia is preferable for repeated use in GPs.

Description

Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively).

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