Taiy Chemical
(D-His2)-LHRH
Synonym (D-His2)-LHRH
Species Human
Protein Accession P01148
Purity Greater than 95%
Endotoxin Level Less than 1 EU/ug
Biological Activity The ED50 as determined by the dose-dependent stimulation of the release of luteinizing hormone from cultured rat pituitary cells is less than 1.0 ng/ml, corresponding to a specific activity of > 1.0 x 10^6 IU/mg.
Expression System E. coli
Fusion Tag No tag
Predicted Molecular Mass 1181 Da
Formulation Lyophilized from a sterile filtered solution of 10 mM HCl
Reconstitution It is recommended to reconstitute the lyophilized (D-His2)-LHRH in sterile 18MΩ-cm H2O not less than 100 µg/ml, which can then be further diluted to other aqueous solutions.
Storage & Stability Lyophilized (D-His2)-LHRH although stable at room temperature for 3 weeks, should be stored desiccated below -18°C. Upon reconstitution (D-His2)-LHRH should be stored at 4°C between 2-7 days and for future use below -18°C.
FAQ
What is (D-His2)-LHRH and how does it function in the body?

(D-His2)-LHRH is a synthetic analogue of the naturally occurring luteinizing hormone-releasing hormone (LHRH or GnRH), which plays a crucial role in regulating the reproductive system. This peptide is a modified version of the hormone with a specific alteration at the second position—where histidine is replaced by its isomer, D-His, to increase its stability and effectiveness. (D-His2)-LHRH is primarily utilized in research settings to better understand how hormonal regulation influences reproductive physiology and related processes.

LHRH is released by the hypothalamus and acts upon the anterior pituitary gland to stimulate the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). These hormones are vital for normal functioning of the ovaries in females and the testes in males. In females, this cascade promotes the maturation of follicles in the ovaries and triggers ovulation. In males, LH stimulates testosterone production while FSH is key for sperm production. Altering the LHRH molecule, as in the case of (D-His2)-LHRH, can affect the responsive hormonal pattern and provides a tool for examining pathway effectiveness under various conditions.

The modified analogue (D-His2)-LHRH can be used to better understand and potentially influence fertility treatments. Researchers can observe how specific changes in LHRH structures alter its interaction with receptors, thus impacting subsequent hormone cascade efficacy. This analogue can also be pivotal in studies aimed at deciphering hormonal dysfunctions or developing methods to manipulate hormone production for therapeutic purposes. For instance, this modified peptide could be explored as a means to proactively control or influence fertility, or even as part of hormone-related cancer research where the suppression of specific hormone activities is crucial. Above all, (D-His2)-LHRH serves as a powerful research tool, aiding scientists in decoding the intricacies of hormonal interactions pertinent to reproduction and broader endocrine health.

How might researchers utilize (D-His2)-LHRH in the context of medical research and treatment development?

Researchers employ (D-His2)-LHRH in various contexts, notably within reproductive medicine and hormone-dependant disease treatments. This analogue serves as a pivotal tool for expanding our understanding of hormonal regulation and offers potential therapeutic avenues. One of the primary areas of employment for (D-His2)-LHRH is in fertility research. By applying this synthetic hormone, scientists can explore distinct physiological responses, testing how it alters the secretion of LH and FSH. This examination can provide insights into ovulatory cycles, spermatogenesis, and more nuanced aspects of reproductive endocrinology, offering enhanced understanding of infertility issues.

Furthermore, (D-His2)-LHRH can be instrumental in developing treatments for hormone-responsive cancers, such as those affecting the prostate or breast. These malignancies often rely on hormonal stimuli for growth and proliferation. Through the adjustment or attenuation of hormone signals, such as those initiated by LHRH, researchers can develop strategies that diminish hormone production or block receptor activation, thereby stunting cancer growth. As a result, (D-His2)-LHRH may pave the way for novel therapeutics that effectively mediate these pathways to provide improved outcomes for patients.

Beyond reproductive health and oncology, (D-His2)-LHRH might offer solutions for managing hormone-related conditions like polycystic ovary syndrome (PCOS) or endometriosis, where hormone regulation plays a critical role in disease management. By manipulating hormonal output, (D-His2)-LHRH presents the possibility of alleviating symptoms or reducing disease severity in such cases.

Furthermore, as scientists continue to expand the application of peptide-based drugs, (D-His2)-LHRH remains at the forefront of innovative peptide therapy development. Its stability and receptor affinity offer significant advantages in preclinical studies aimed at developing targeted therapies, exemplifying its invaluable role in translational research. The research on (D-His2)-LHRH thus extends beyond theoretical exploration, offering practical applicability in therapeutic innovation, which continues to develop as technologies and methodologies improve.

What are the safety considerations and potential side effects associated with the use of (D-His2)-LHRH in research settings?

When using (D-His2)-LHRH in research settings, it is important to consider both the potential biological effects and hazards associated with handling synthetic peptides. As a chemical entity, it must be carefully managed to avoid exposure risks, which are typically mitigated through standard laboratory safety protocols. Protective equipment, such as gloves and safety goggles, should be worn to prevent direct skin contact or accidental ingestion or inhalation, and experiments should be conducted within controlled environments, like laminar flow hoods, to prevent cross-contamination or exposure.

In terms of biological safety, the administration of (D-His2)-LHRH to biological models can elicit a variety of physiological responses, depending on the dosage and method of administration. By imitating natural LHRH, this analogue could potentially alter hormonal balances, leading to side effects similar to those observed with natural hormone therapies. These could include changes in reproductive function, such as altered menstrual cycles or impacts on testosterone production. Experiments need to be designed carefully to monitor these impacts, particularly when working with animal models.

When extrapolating data from animal studies to human applications, researchers must proceed cautiously. Side effects observed in animal models do not always accurately predict human responses due to biological and metabolic differences. Nonetheless, these observations provide a critical foundation for assessing the potential impacts on hormone levels, reproductive cycles, or other physiological parameters.

It's also crucial to consider potential long-term effects and the duration of the hormone alteration. Chronic exposure or improper dosing could lead to sustained hormonal imbalance or negative feedback effects on the hypothalamic-pituitary-gonadal axis, which must be managed through tailored experimental designs.

Moreover, since (D-His2)-LHRH may interact differently with various receptors, understanding receptor-specific activity is key. Detailed receptor binding studies should be carried out to elucidate these interactions, ensuring that the analogue's behavior within biological systems is thoroughly understood. Such investigations aid in anticipating and mitigating unintended effects, reinforcing the importance of established preclinical safety assessments and appropriate dosing regimens.

How does (D-His2)-LHRH differ from other LHRH analogues in terms of stability and efficacy?

(D-His2)-LHRH is distinguished from other LHRH analogues mainly by its structural modification at the second position, where the natural amino acid histidine is replaced with D-His, an isomer of histidine. This specific alteration enhances both the stability and efficacy of the peptide compared to its natural counterpart. The inclusion of D-His impedes enzymatic degradation, thereby extending the analogue's half-life in biological systems. Increased stability allows for a prolonged therapeutic window and reduces the frequency of administration, which can be particularly beneficial in long-term treatment or research contexts.

The efficacy of (D-His2)-LHRH is linked to its ability to maintain biological activity despite its structural modifications. It retains the capacity to bind effectively to LHRH receptors, ensuring that the essential signaling cascade is initiated efficiently. The selective receptor affinity of (D-His2)-LHRH contributes to its role as an effective tool in research settings, enabling precise modulation of reproductive hormones like LH and FSH. This precision is fundamental when investigating cellular responses, testing hypotheses within endocrine research, or exploring novel therapeutic approaches.

Additionally, the unique stability attributes of (D-His2)-LHRH facilitate its use under varying experimental conditions, including those that mimic human physiological environments or altered states in disease models. Its ability to sustain activity over extended periods presents researchers with enhanced flexibility in experimental design and specificity in observing time-dependent hormonal effects.

In contrast, other LHRH analogues might not offer the same level of receptor specificity or stability, which can limit their application or require more frequent dosing. The development of such analogues is multifaceted, focusing on achieving an optimal balance between stability, receptor binding efficiency, and biological impact. The choice among available analogues, therefore, hinges on the specific requirements of a study or treatment, where (D-His2)-LHRH might be preferred for leveraging its distinct attributes that align with desired research or therapeutic outcomes.

What are the potential implications of using (D-His2)-LHRH in the treatment of endocrine disorders?

The application of (D-His2)-LHRH in treating endocrine disorders holds considerable promise due to its ability to modulate hormonal pathways precisely. Endocrine disorders, characterized by dysregulation in hormone production or signaling, often require targeted therapeutic strategies to restore balance. By virtue of its modified peptide structure, (D-His2)-LHRH functions with increased stability and receptor affinity, offering nuanced control over hormone-dependent pathways. This makes it a valuable candidate for addressing disorders such as hypogonadism, polycystic ovary syndrome (PCOS), and hormone-sensitive cancers.

In the treatment of hypogonadism, where patients exhibit insufficient hormone production leading to underdeveloped secondary sexual characteristics or reproductive issues, (D-His2)-LHRH can be utilized to stimulate the pituitary release of gonadotropins (LH and FSH). By doing so, it can promote gonadal function, thereby increasing the production of sex steroids and supporting normal reproductive physiology. This treatment approach could significantly improve quality of life and assist in resolving underlying symptoms associated with hormonal deficiency.

For conditions like PCOS, where hormonal imbalance leads to irregular ovulation and other physical manifestations, (D-His2)-LHRH might offer therapeutic advantages by effectively controlling hormonal outputs that contribute to ovulatory dysfunction. By manipulating the hypothalamic-pituitary-ovarian axis, it might be possible to mitigate the reproductive challenges posed by this syndrome.

Moreover, in the realm of cancer therapy, particularly for hormone-sensitive types like certain prostate and breast cancers, (D-His2)-LHRH might be used to suppress the hormonal signals that fuel cancer cell proliferation. By acting on the LHRH receptors to downregulate gonadotropin release, it can reduce the levels of sex steroids that are often necessary for tumor growth. This mechanism of action presents a non-surgical option drawn from hormonal manipulation, which is less invasive and can be tailored in dosing.

The exploration of (D-His2)-LHRH's potential extends beyond reproductive health into broader endocrine applications, where precision in hormone regulation is critical. As researchers continue to unravel the diverse roles of peptides in clinical settings, (D-His2)-LHRH represents a promising frontier in the ongoing effort to devise effective, targeted therapies for complex endocrine disorders.
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