Medetomidine HCl

CAS# 86347-15-1

Medetomidine HCl

Catalog No. BCC4351----Order now to get a substantial discount!

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Quality Control of Medetomidine HCl

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Chemical structure

Medetomidine HCl

3D structure

Chemical Properties of Medetomidine HCl

Cas No. 86347-15-1 SDF Download SDF
PubChem ID 68601 Appearance Powder
Formula C13H17ClN2 M.Wt 236.74
Type of Compound N/A Storage Desiccate at -20°C
Solubility : ≥ 50 mg/mL (211.20 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 5-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole;hydrochloride
SMILES CC1=C(C(=CC=C1)C(C)C2=CN=CN2)C.Cl
Standard InChIKey VPNGEIHDPSLNMU-UHFFFAOYSA-N
Standard InChI 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
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.

Biological Activity of Medetomidine HCl

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

Medetomidine HCl Dilution Calculator

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Medetomidine HCl Molarity Calculator

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Preparing Stock Solutions of Medetomidine HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 4.224 mL 21.1202 mL 42.2404 mL 84.4809 mL 105.6011 mL
5 mM 0.8448 mL 4.224 mL 8.4481 mL 16.8962 mL 21.1202 mL
10 mM 0.4224 mL 2.112 mL 4.224 mL 8.4481 mL 10.5601 mL
50 mM 0.0845 mL 0.4224 mL 0.8448 mL 1.6896 mL 2.112 mL
100 mM 0.0422 mL 0.2112 mL 0.4224 mL 0.8448 mL 1.056 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 HCl

Medetomidine is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

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References on Medetomidine HCl

Evaluation of three immobilization combinations in the capybara (Hydrochoerus hydrochaeris).[Pubmed:19645047]

Zoo Biol. 2010 Jan-Feb;29(1):59-67.

Capybaras (Hydrochoerus hydrochaeris) are the world's largest rodent. Owing to its uniqueness, 50 AZA institutions in North America display this species. As shown by a survey, no standard anesthetic protocol has been developed for this species. As a part of an ongoing behavioral study in Venezuela, capybaras were surgically implanted with radio transmitters. Animals were randomly assigned to one of the three immobilization protocols: (1) Tiletamine HCl/Zolazepam HCl, (2) Tiletamine HCl/Zolazepam HCl/Medetomidine HCl, and (3) Tiletamine HCl/Zolazepam HCl/Medetomidine HCl/Butorphanol tartrate. The protocol recommended for minimally invasive procedures when inhalant anesthetics are unavailable is a combination of Tiletamine HCl/Zolazepam HCl/Medetomidine HCl/Butorphanol tartrate. This is based on ease of administration, volume, onset of action, depth of anesthetic achieved, reversibility, safety, and costs.

Medetomidine--a novel alpha 2-adrenoceptor agonist: a review of its pharmacodynamic effects.[Pubmed:2571177]

Prog Neuropsychopharmacol Biol Psychiatry. 1989;13(5):635-51.

1. The pharmacodynamic effects of medetomidine, a novel alpha 2-adrenoceptor agonist, are reviewed. 2. In receptor binding experiments, and in isolated organ preparations medetomidine shows high specificity and selectivity to alpha 2-adrenoceptors. Its alpha 2/alpha 1 selectivity ratio is 1620 compared to 220 of clonidine. It is a highly potent full agonist at alpha 2-adrenoceptors, a fact that also distinguishes it from clonidine. 3. Medetomidine induces a dose-dependent decrease in the central release and turnover of norepinephrine (NE) measured as changes in metabolite concentrations or using pharmacological intervention techniques. 4. The selectivity, specificity and potency of medetomidine is further supported by various in vivo experiments showing dose-dependent hypotensive, bradycardic, sedative, anxiolytic mydriatic, hypothermic and analgesic effects. 5. The pharmacological, neurochemical and behavioral effects of medetomidine can be inhibited by prior, simultaneous or subsequent administration of selective and specific alpha 2-antagonists. 6. In humans medetomidine is well-tolerated and pharmacodynamic effects including e.g. dose-dependent decrease of vigilance, blood pressure, heart rate, salivary secretion and plasma NE are compatible with an agonistic action at alpha 2-adrenoceptors.

Characterization of the selectivity, specificity and potency of medetomidine as an alpha 2-adrenoceptor agonist.[Pubmed:2900154]

Eur J Pharmacol. 1988 May 20;150(1-2):9-14.

Medetomidine (4-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole) was tested for alpha 2-adrenoceptor agonist activity and compared to several reference agents. In binding studies carried out with rat brain membrane preparations, medetomidine showed high affinity for alpha 2-adrenoceptors, as measured by the displacement of [3H]clonidine (Ki 1.08 nM compared to 1.62, 3.20, 6.22 and 194 nM for detomidine, clonidine, UK 14,304 and xylazine, respectively). The affinity of medetomidine for alpha 1-adrenoceptors, as measured by [3H]prazosin displacement, was much weaker, yielding a relative alpha 2/alpha 1 selectivity ratio of 1620 which is 5-10 times higher than that of the reference compounds. Medetomidine caused a concentration-dependent inhibition of the twitch response in electrically stimulated mouse vas deferens with a pD2 value of 9.0 compared to that of 8.6, 8.5, 8.2 and 7.1 for detomidine, clonidine, UK 14,304 and xylazine, respectively. The effect of medetomidine was antagonized by idazoxan. In anaesthetized rats, medetomidine caused a dose-dependent mydriasis which could be reversed by alpha 2-adrenoceptor blockade. In receptor binding experiments and isolated organs medetomidine had no affinity or effects on beta 1-, beta 2-, H1, H2, 5-HT1, 5-HT2, muscarine, dopamine, tryptamine, GABA, opiate and benzodiazepine receptors. Based on these results, medetomidine can be classified as a potent, selective and specific alpha 2-adrenoceptor agonist.

Evidence for medetomidine as a selective and potent agonist at alpha 2-adrenoreceptors.[Pubmed:2880852]

J Auton Pharmacol. 1986 Dec;6(4):275-84.

The activity on alpha-adrenoreceptors of medetomidine ((+/-)-4-(alpha,2,3-trimethylbenzyl)imidazole), an alpha-methyl derivative of detomidine, has been characterized in vivo and in vitro using detomidine, MPV 207, MPV 295, azepexole, clonidine and xylazine for reference purposes. Medetomidine (1-100 micrograms/kg i.v.) was a hypotensive and bradycardic compound in anaesthetized rats. Furthermore, it induced vasopressor (PD50 1.7 microgram/kg) and sympatho-inhibitory (ID50 1.6 microgram/kg) actions in pithed rats, the effects being antagonized by idazoxan (0.3 mg/kg i.v.) but not by prazosin (0.1 mg/kg i.v.). Medetomidine (30-300 micrograms/kg i.m.) had an alpha 2-adrenoreceptor mediated sedative effect on chicks. Medetomidine was, overall, more potent than detomidine, MPV 207, clonidine, xylazine, MPV 295 or azepexole in central (sedation in the chick) and peripheral (cardiac presynaptic in the pithed rat) actions on alpha 2-adrenoreceptors. Clonidine had, however, about an equal potency to medetomidine in the vascular smooth muscle of the pithed rat. Like detomidine and MPV 295, medetomidine had no agonistic activity in the rat aortic ring, but high concentrations antagonized methoxamine-induced contractions, giving a pA2 value of 5.68 for alpha 1-adrenoreceptor antagonism. The overall lipophilicity (log P') of medetomidine in the octanol/buffer (pH 7.4, 24-26 degrees C, HPLC technique) was 2.80. In summary, the experimental data suggest that medetomidine is a lipophilic compound with selective alpha 2-adrenoreceptor-stimulating properties and high potency. It may, therefore, prove to be a suitable pharmacologic tool for interventions in alpha 2-adrenoreceptor mediated effects in the autonomic nervous system.

Description

Medetomidine hydrochloride is an agonist of adrenergic alpha-2 receptor, which is used in veterinary medicine for its analgesic and sedative properties.

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