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Imiloxan hydrochloride

CAS# 81167-22-8

Imiloxan hydrochloride

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Chemical structure

Imiloxan hydrochloride

3D structure

Chemical Properties of Imiloxan hydrochloride

Cas No. 81167-22-8 SDF Download SDF
PubChem ID 76972120 Appearance Powder
Formula C14H17ClN2O2 M.Wt 280.75
Type of Compound N/A Storage Desiccate at -20°C
Synonyms RS 21361
Solubility Soluble to 100 mM in water
Chemical Name 2-[[(3R)-2,3-dihydro-1,4-benzodioxin-3-yl]methyl]-1-ethylimidazole;hydrochloride
SMILES CCN1C=CN=C1CC2COC3=CC=CC=C3O2.Cl
Standard InChIKey ANDJPJNFVJXEKX-RFVHGSKJSA-N
Standard InChI InChI=1S/C14H16N2O2.ClH/c1-2-16-8-7-15-14(16)9-11-10-17-12-5-3-4-6-13(12)18-11;/h3-8,11H,2,9-10H2,1H3;1H/t11-;/m1./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 Imiloxan hydrochloride

DescriptionA moderately potent, but highly selective α2-adrenoceptor antagonist, the only reported selective antagonist at the α2B-adrenoceptor not having potent α1-adrenoceptor antagonist activity.

Imiloxan hydrochloride Dilution Calculator

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Preparing Stock Solutions of Imiloxan hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.5619 mL 17.8094 mL 35.6189 mL 71.2378 mL 89.0472 mL
5 mM 0.7124 mL 3.5619 mL 7.1238 mL 14.2476 mL 17.8094 mL
10 mM 0.3562 mL 1.7809 mL 3.5619 mL 7.1238 mL 8.9047 mL
50 mM 0.0712 mL 0.3562 mL 0.7124 mL 1.4248 mL 1.7809 mL
100 mM 0.0356 mL 0.1781 mL 0.3562 mL 0.7124 mL 0.8905 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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References on Imiloxan hydrochloride

The metabolism of imiloxan hydrochloride in healthy male volunteers.[Pubmed:1352928]

Xenobiotica. 1992 Feb;22(2):237-46.

1. The metabolism of Imiloxan hydrochloride [(+-)-2-(1-ethyl-2-imidazoyl)methyl-1,4-benzodioxane hydrochloride], an alpha 2-adrenoceptor antagonist, was studied in four male volunteers given a 500 mg oral dose containing 0.48 MBq of the 14C-labelled material. Compound-related radioactivity was rapidly excreted chiefly in the urine within 24 h of dosing. 2. Metabolites derived by initial oxidation on either or both the benzodioxane and imidazoyl moieties followed by glucuronic acid and sulphate conjugation, and an N-glucuronide of imiloxan were tentatively identified in urine. 3. The major urinary metabolites, comprising some 37-41% of the dose, appeared to be +-2-(1-ethyl-2-imidazoyl)methyl-1,4-benzodioxane-6/7-sulphonic acid (19% of dose), [+-2-(1-ethyl-2-imidazoyl)methyl-1,4-benzodioxane- 6/7-ylium D-glucopyranoside]uronate (10-14% of dose), and a glucuronide conjugate of +-2-(1-ethyl-2-imidazoyl-4/5-hydroxy)methyl-1,4-benzodioxane (8% of dose).

Assessment of imiloxan as a selective alpha 2B-adrenoceptor antagonist.[Pubmed:1970500]

Br J Pharmacol. 1990 Mar;99(3):560-4.

1. The alpha 2-adrenoceptor binding sites of rabbit spleen and rat kidney, labelled with [3H]-rauwolscine, were characterized using a range of subtype selective ligands. 2. In rabbit spleen, the alpha-2-adrenoceptor binding sites displayed high affinity for oxymetazoline and WB 4101 and low affinity for prazosin and chlorpromazine suggesting the presence of an alpha 2A subtype. 3. There was evidence for heterogeneity of the alpha 2-adrenoceptor binding sites present in rabbit spleen. The results obtained with oxymetazoline and WB 4101 indicated that at least 75% of the [3H]-rauwolscine binding sites in this preparation displayed a pharmacology consistent with the presence of an alpha 2A subtype. 4. In rat kidney, the alpha 2-adrenoceptor binding sites displayed high affinity for prazosin and chlorpromazine and low affinity for oxymetazoline and WB 4101 suggesting the presence of an alpha 2B subtype. 5. The inclusion of guanylylimidodiphosphate (Gpp(NH)p, 0.1 mM) did not modify the pharmacology of the alpha 2-adrenoceptor binding sites present in the two preparations. Furthermore, when the two membrane preparations were combined, the resultant pharmacology was still consistent with the presence of two receptors that retained the characteristics of the alpha 2A and alpha 2B subtypes. 6. Imiloxan was identified as a selective alpha 2B ligand while benoxathian displayed a high degree of selectivity for the alpha 2A-adrenoceptor binding site. The selectivity of imiloxan for the alpha 2B-adrenoceptor binding site, coupled with its specificity for alpha 2-adrenoceptors, should make it a valuable tool in the classification of alpha 2-adrenoceptor subtypes.

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