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Homatropine Methylbromide

Muscarinic AChR antagonist CAS# 80-49-9

Homatropine Methylbromide

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Quality Control of Homatropine Methylbromide

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Chemical structure

Homatropine Methylbromide

3D structure

Chemical Properties of Homatropine Methylbromide

Cas No. 80-49-9 SDF Download SDF
PubChem ID 6646 Appearance Powder
Formula C17H24BrNO3 M.Wt 370.28
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Homatropine methobromide
Solubility DMSO : ≥ 31 mg/mL (83.72 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (8,8-dimethyl-8-azoniabicyclo[3.2.1]octan-3-yl) 2-hydroxy-2-phenylacetate;bromide
SMILES C[N+]1(C2CCC1CC(C2)OC(=O)C(C3=CC=CC=C3)O)C.[Br-]
Standard InChIKey FUFVKLQESJNNAN-UHFFFAOYSA-M
Standard InChI InChI=1S/C17H24NO3.BrH/c1-18(2)13-8-9-14(18)11-15(10-13)21-17(20)16(19)12-6-4-3-5-7-12;/h3-7,13-16,19H,8-11H2,1-2H3;1H/q+1;/p-1
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 Homatropine Methylbromide

DescriptionHomatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively. target: mAChR IC 50: WKY-E(162.5 nM), SHR-E(170.4nM ) In vitro: Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs. Homatropine (20 μM) produces a dose ratio of only 95.0 when combined with hexamethonium in atrium from guinea-pigs. In vivo: : Pre-treatment with homatropine (20 mg/kg) was comparable with atropine (10 mg/kg) in preventing lethality in this rat model of acute OC poisoning. All rats pre-treated with normal saline, atropine 5 mg/kg, and homatropine 10 mg/kg died. Survival in the homatropine (20 mg/kg) and atropine (10 mg/kg) groups was 30% and 40% respectively.

References:
[1]. Sim MK et al. Muscarinic receptors in the aortae of normo- and hypertensive rats: a binding study. Clin Exp Hypertens. 1993 Mar;15(2):409-21. [2]. Bryant SM et al. Intramuscular ophthalmic homatropine vs. atropine to prevent lethality in rates with dichlorvos poisoning. J Med Toxicol. 2006 Dec;2(4):156-9. [3]. Leung E et al. Modification by hexamethonium of the muscarinic receptors blocking activity of pancuronium and homatropine in isolated tissues of the guinea-pig. Eur J Pharmacol. 1982 May 7;80(1):11-7.

Homatropine Methylbromide Dilution Calculator

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Homatropine Methylbromide Molarity Calculator

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Preparing Stock Solutions of Homatropine Methylbromide

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7007 mL 13.5033 mL 27.0066 mL 54.0132 mL 67.5165 mL
5 mM 0.5401 mL 2.7007 mL 5.4013 mL 10.8026 mL 13.5033 mL
10 mM 0.2701 mL 1.3503 mL 2.7007 mL 5.4013 mL 6.7516 mL
50 mM 0.054 mL 0.2701 mL 0.5401 mL 1.0803 mL 1.3503 mL
100 mM 0.027 mL 0.135 mL 0.2701 mL 0.5401 mL 0.6752 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 Homatropine Methylbromide

Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.

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References on Homatropine Methylbromide

Flow-injection turbidimetric determination of homatropine methylbromide in pharmaceutical formulations using silicotungstic acid as precipitant reagent.[Pubmed:18970560]

Talanta. 2006 Mar 15;69(1):239-42.

A flow-injection turbidimetric procedure exploiting merging zones is proposed for determining Homatropine Methylbromide (HMB) in pharmaceutical preparations. The determination is based on the precipitation reaction of Homatropine Methylbromide with silicotungstic acid in acidic medium to form a precipitate, which was measured at 410 nm. The analytical curve was linear in the HMB concentration range from 8.1 x 10(-5) to 2.2 x 10(-4)mol l(-1), with a detection limit of 5.0 x 10(-6)mol l(-1). The recoveries ranged from 96 to 103%, the sampling frequency was 70 determinations per hour and relative standard deviations were less than 1.5% (n=10). The results obtained for commercial formulations using the FIA procedure were in good agreement with those obtained by using a comparative method.

Analysis of homatropine methylbromide dosage forms.[Pubmed:576237]

J Pharm Sci. 1977 Jan;66(1):123-4.

A stability-indicating method of analysis of Homatropine Methylbromide in pharmaceutical formulations was developed. This method is based on the formation of a picric acid-quaternary ammonium complex, which is adsorbed on acid-washed diatomaceous earth in alkaline media followed by on-column chloroform extraction. The picrate complex is measured spectrophotometrically at 365 nm. The method was selective for Homatropine Methylbromide in that there was no interference from its major hydrolytic decomposition products, tropinium methylbromide and mandelic acid.

Rectal absorption of homatropine [14C]methylbromide in the rat.[Pubmed:26740]

J Pharm Pharmacol. 1978 May;30(5):284-6.

Homatropine[14C]methylbromide (HMB-14C) was administered to rats by intramuscular injection, oral gavage and rectal suppository. Plasma concentration of 14C were measured over the subsequent 12 h. Peak plasma concentrations were higher and achieved more rapidly after rectal administration than by the other routes whether HMB-14C was administered in a water-soluble suppository base or in aqueous solution. Twelve h after the suppositories were inserted and retained 28% of the 14C had been excreted in the urine while 56% remained in the large intestine. Unlabelled HMB, given in rectal suppositories to anaesthetized rats, caused prompt blockade of the effects of vagal stimulation on pulse rate and of intravenous acetylcholine on blood pressure. These results confirm the rapid rectal absorption of the drug.

Description

Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.

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