Month: August 2013

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Antosiban acetate is commonly researched for its potential in stopping premature labor. The applications and effects of this chemical will vary based on which animals it is being applied to and how it is intended to be used. Most research focuses on applying this peptide to female animals given its natural role in reproductive health within the body.

While this medication is commonly used in European countries to better manage premature labor between the 24-33 weeks of pregnancy by blocking oxytocin in the body, it is not approved nor recommended for this or any other use by individuals in the United States.

While antosiban has been shown to be helpful in managing reproductive health issues it has also been shown to contribute to kidney problems, liver problems, placental abruption, placenta praeia or premature rupture of membranes when applied to animals in research settings. Research is ongoing to better understand what applications of this chemical increase the likelihood of these effects to better understand the workings of this chemical and its potential future medical uses.

Preparing Atosiban Acetate

The following measures should be followed when preparing atosiban acetate for laboratory use.

• Dissolve the product in an aqueous acetonitrile solution using aqueous ammonia and oxidized water filtering to adjust the pH value and purify the substance. You can slowly convert the substance to a salt to obtain the necessary atosiban acetate.
• This method is considered ideal for those that will need to harvest large portions of this chemical because atosiban acetate can be very difficult to dissolve.

This method will also shorten the reaction time to a more reasonable option so it is easy to industrialize the product without compromising the quality or the purity of the product which would be necessary for clinical research.

Visual Compatibility of the Chemical

Many animals exposed to atosiban acetate for research purposes are also exposed to similar chemicals which will need to be presented with care.

• Research for intrauterine infections or endometriosis will often revolve around applying atosiban acetate with amoxicilling clavulanic acid or magnesium sulfate and ketanserin. There is not yet information available about the reactions of this combination.
• Atosiban acetate is typically applied to animals using a sterile aqueous concentrate that is preservative free and contanes acetate sale as well as mannitol to adjust the pH as necessary for the given application.

It is recommended that any solutions with atosiban acetate be applied in a 1:1 ratio. This will allow the solution to retain as much of the original properties of the chemicals as possible during study to ensure accurate and reliable results.

There have been some contradictions regarding the science behind using atosiban acetate in research settings. Some have found that preparations of vitamins may provide a complimentary effect when applied alongside this chemical. However, it has also been found that if this chemical is applied to animals that have also been exposed to known medications containing calcium channel blockers, tocolytic activity or beta mimetics it can produce negative effects that are potentially fatal for the animal.

Sources:

http://patentscope.wipo.int/search/en/WO2012083861
http://www.ajhp.org/content/62/23/2459.extract

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Antide acetate is a peptide which acts as an LHRH antagonist in ‘natural settings’ and can be utilized by an animal’s body to represses FSH and LH releases that stem from the pituitary gland. Synthetic versions of this chemical have been developed as a means of controlling these reactions in a laboratory setting, both as a means to determine a potential medical use for antide acetate and to help researchers better understand the role of this chemical in an animal’s body when it is naturally produced.

Antide acetate that is prepared for use in a laboratory setting is provided in a lyophilized sterile condition that can be reconstituted or diluted with an aqueous solution as necessary for the given application. Researchers are encouraged to seek out a supply that is prepared without additives, to ensure accurate and reliable testing results once the chemical is in use.

Protein quantitation via analysis of the calibrated solution of the chemical or UV spectroscopy set to 280 nm is recommended when applicable.

Potential Application in Inhibiting Liomyoma Extracellular Matrix Production

A recent study worked to determine the effects of GnRH analogues leuprolide acetate as well as cetrorelix acetate on the matrix of the leiomyoma in myometrial cells.

• Leiomyoma cells were exposed to GnRH analogues in varying stages with groups receiving applications for 6, 24 or 120 hours.
• Cells in the initial group saw a decrease in the expression of GnRHR1.
• Those in the 24 hour group saw an increase in the expression of the same GnRHR1 or fibronectin and a versican variant.

Exposing the cells to high concentrations of these chemicals did not increase fibronectin protein production. Protein production in cells that were treated for 120 hours did see an increase in GnRHR1 as well as the virsican variants and fibronectin though only in similar quantities to those in earlier demonstrations.

Potential Oral Delivery System in Vivo

Studies worked to show the potential use of an oral delivery system in vivo that could be used to apply antide or other peptides.

• During this study a sulfhydryl ligand thioglycolic acid was attached to the chitosan for modification and thiol groups of isolated portions of thiolated chitosan were protected by the application of a disulfide bond in intentinal rat mucosa.
• Tablets of each peptide sample were studied ex vivo on the mucosa to determine their rate of absorption within the mucosa.

Results indicated that time release antide incorporated tablets could be seen under a plasma concentration that were comparative to supplying an antide solution directly, implying that this system could improve the bioavailability of select peptides.

It is recommended that researchers reconstitute a lyophilized sample of antide acetate, using 18M of water, though this may vary given the size and methodology used in the preparation of the sample. The concentration of the chemical should be noted on the individualized packaging that was prepared with the product.

This concentration and size may vary based on the lab animals the sample was intended to be used with. Most are prepared for use in rats, so researchers should react accordingly.

Sources:

http://www.sciencedirect.com/science/article/pii/S0015028212018766
http://www.sciencedirect.com/science/article/pii/S0168365912002611

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Click here to view/download the PDF version of this article

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Alarelin acetate is a gondatrophin releasing hormone. Natural forms of alarelin found in animals are used to induce ovulation. Synthetic versions of this product are created using an LH-RH antagonist which is commonly set in larger doses than the natural LH-RH that is typically found in the rat hypophyseal stimulation or the gondatoropin secretions in induced ovulation or in vitro.

This chemical is the acetate form of the natural hypothalamic peptide which is used by an animal’s body to release LH and FSH from the pituitary gland. The peptide alarelin acetate has a single non-glycosylated polypeptide structure that is made up of nine amino acids. This has a molecular mass of 1167.3.

Alarelin is commonly used in research settings both to better understand this peptide’s effects on an animal’s body and to induce conditions that may assist with reproductive research. Samples of this chemical intended for research settings are typically stable for around three weeks at room temperature, and will need to be stored at temperatures below -18 degrees Celsius for long term use.

Most versions of this chemical are shipped as a lyophilized powder that can be reconstituted at a sterile temperature. This chemical may remain stable for up to three weeks at room temperature if it is kept sealed when it is not in use. If this product will be used for long periods of time is should be kept in a freezer with a waterproof sea.

If the mixture has already been reconstituted it can be kept at 40 degrees Celsius for 2-7 days but should be kept at -180 degrees Celsius for longer periods of time. Do not continually refreeze and thaw the product.

Effects on FSH Receptors

A study was performed to determine the effects of alarelin as a GnRH antagonist on the follicle-stimulating hormone receptor of the pituitary gland of ewes.

• Twenty-eight ewes were randomly assigned to groups which were injected with alarelin antigens twice a day, versus a control group that was injected with a solvent.
• Samples of the ovaries were then taken 70 days following this treatment and blood samples were harvested from the jugular vein at even intervals throughout the study following the initial injection.
• Groups that were exposed to alarelin acetate were found to see a higher concentration of GnRH antibodies than those that were in the control group. FSHR cells that were immunostained were found in the ovaries of those that were exposed to this chemical as well.

These increased secretions were found to promote the development of follicles and ovaries within the ewes. This implies that this chemical may have potential in future technique involving superovulation strategies.

Most versions of alarelin acetate are designed to be diluted using an aqueous solution to create the necessary application size for the given experimental setting. It is recommended that alarelin only be reconstituted when it is ready for use. If this product will be in storage for a long period of time it may be necessary to add a carrier protein as a means of protection.

Sources:

http://www.usbio.net/item/A2298-09T
http://www.sciencedirect.com/science/article/pii/S0921448812000776

Click here to view our entire PDF research library

Click here to view/download the PDF version of this article