Dexmedetomidine HCl

CAS# 145108-58-3

Dexmedetomidine HCl

2D Structure

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Dexmedetomidine HCl

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Chemical Properties of Dexmedetomidine HCl

Cas No. 145108-58-3 SDF Download SDF
PubChem ID 6918081 Appearance Powder
Formula C13H17ClN2 M.Wt 236.74
Type of Compound N/A Storage Desiccate at -20°C
Synonyms <em>d</em>-Medetomidine hydrochloride
Solubility H2O : ≥ 50 mg/mL (211.20 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 5-[(1S)-1-(2,3-dimethylphenyl)ethyl]-1H-imidazole;hydrochloride
SMILES CC1=C(C(=CC=C1)C(C)C2=CN=CN2)C.Cl
Standard InChIKey VPNGEIHDPSLNMU-MERQFXBCSA-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/t11-;/m0./s1
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 Dexmedetomidine HCl

DescriptionActive isomer of medetomidine, a potent, 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). Active in vivo; displays hypotensive, bradycardic, sedative, anxiolytic, hypothermic and analgesic effects.

Dexmedetomidine HCl Dilution Calculator

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Dexmedetomidine HCl Molarity Calculator

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Preparing Stock Solutions of Dexmedetomidine 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 Dexmedetomidine HCl

Dexmedetomidine 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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References on Dexmedetomidine HCl

Antinociceptive properties of intrathecal dexmedetomidine in rats.[Pubmed:1674472]

Eur J Pharmacol. 1991 Jan 10;192(2):221-5.

Dexmedetomidine is a highly selective alpha 2-adrenoceptor agonist. In this study, the intrathecal administration of dexmedetomidine into the rat lumbar subarachnoid space produced dose-dependent, prolonged antinociception as measured by hot plate and tail flick testing. Intrathecal administration of 3 or 10 micrograms of dexmedetomidine increased hot plate and tail flick latencies to cutoff values within 15 min of injection. Animals receiving 1 microgram of intrathecal dexmedetomidine did not show any significant antinociception when compared to saline controls. The intrathecal administration of the alpha 2-adrenoceptor antagonist, idazoxan, ablated all measurable antinociception produced by the prior injection of 10 micrograms of dexmedetomidine.

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.

Description

Dexmedetomidine 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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