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Antide is a short peptide, typically consisting of a specific sequence of amino acids that mimics the bioactive region of VIP. This structural similarity allows it to interact with VIP receptors, primarily VPAC1 and VPAC2, which are expressed in various tissues, including the central nervous system (CNS), immune cells, and smooth muscle. By binding to these receptors, it can modulate cellular signaling pathways, leading to a range of physiological responses.
One of the most promising aspects is its neuroprotective properties. Studies have shown that can protect neurons from damage caused by excitotoxicity, oxidative stress, and inflammation. This makes it a potential candidate for the treatment of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and multiple sclerosis. The ability to enhance neuronal survival and promote synaptic plasticity further underscores its therapeutic potential in conditions characterized by neuronal loss or dysfunction.
Customized Bottle Caps & Corks
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Chemical Formula |
C82H108ClN17O14 |
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Exact Mass |
1590 |
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Molecular Weight |
1591 |
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m/z |
1590 (100.0%), 1591 (88.7%), 1592 (38.8%), 1592 (32.0%), 1593 (28.3%), 1594 (12.4%), 1593 (10.4%), 1591 (6.3%), 1592 (5.6%), 1595 (3.6%), 1592 (2.9%), 1593 (2.6%), 1593 (2.4%), 1593 (2.0%), 1594 (2.0%), 1594 (1.8%), 1591 (1.2%), 1594 (1.1%), 1592 (1.1%) |
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Elemental Analysis |
C, 61.89; H, 6.84; Cl, 2.23; N, 14.96; O, 14.08 |
synthesis methods
Method 1
Raw materials: pyrrolidine, acetone, tetrahydrofuran, boric acid, iodomethane, diphenylphosphine, tert butyryl alumina, p-carboxyphenylthiourea, rhodium trichloride, isopropyl lithium
- In tetrahydrofuran, pyrrolidine is reacted with acetone to obtain N-propylpyrrolidine.
- Reduce N-propylpyrrolidine with boric acid to obtain N-propylpyrrolidine borate ester.
- Perform condensation reaction between N-propylpyrrolidone borate and diphenylphosphine in the presence of tert butyryl alumina to obtain N-(2-diphenylphosphineethyl) pyrrolidine.
- Substitution reaction of N-(2-diphenylphosphineethyl) pyrrolidine with p-carboxyphenylthiourea to obtain N-(2-diphenylphosphineethyl) pyrrolidine p-carboxyphenylthiourea imide.
- In the presence of rhodium trichloride, N-(2-diphenylphosphineethyl) pyrrolidine p-carboxyphenylthiourea imide was reduced with isopropyl lithium to obtain antipeptide.
Method 2
Raw materials: 1-methylpyrrolidine, chloro tert butyrate, tetrahydrofuran, NaH, Pd/C, acetic acid, iodomethane
- Use NaH to remove one proton from 1-methylpyrrolidine and obtain the 1-methylpyrrolidine ion.
- In tetrahydrofuran, N-tert butyryl-1-methylpyrrolidine is obtained by substitution reaction between 1-methylpyrrolidine ion and tert butyrate chloride.
- Use Pd/C to reduce N-tert butyryl-1-methylpyrrolidine and acetic acid to N-methyl-1-methylpyrrolidine.
- Substitute N-methyl-1-methylpyrrolidine with iodomethane to obtain N-methyl-2-iodoethylpyrrolidine.
- In tetrahydrofuran, N-methyl-2-iodoethylpyrrolidine is condensed with p-carboxyphenylthiourea to obtain N-(2-hydroxyethyl) pyrrolidine p-carboxyphenylthiourea imide.
- In the presence of Pd/C, N-(2-hydroxyethyl) pyrrolidine p-carboxyphenylthiourea imide was reduced with acetic acid to obtain antipeptide.
It should be noted that the above synthesis methods involve organic synthesis and the treatment of important intermediates, and there are certain risks involved. Personnel with relevant qualifications and high chemical experimental abilities are required to operate in the laboratory. At the same time, in order to ensure the safety and accuracy of the experiment, it is necessary to strictly follow the chemical experiment operating procedures and safety operating standards.
In addition to the above two methods, there are many other methods for synthesizing antide in the laboratory. The following are some commonly used chemical methods:
Amino acid condensation reaction
Various amino acids (such as phenylalanine, tryptophan, etc.) are condensed to obtain peptide fragments. After separation and purification, these fragments can be further connected into complete antipeptide molecules.
Solid phase synthesis method
Using column chromatography technology, the amino acid mixture is adsorbed on a silica gel or polymer carrier, and then the target compound is separated from the carrier through the elution effect of the eluent. This method can improve synthesis efficiency, reduce pollution and the occurrence of side reactions.
Liquid phase synthesis method
Antipeptide is synthesized through chemical reactions and enzyme catalysis in organic solvents such as acetonitrile and methanol. This method requires the use of specific catalysts and enzymes, and requires complex separation and purification steps.
Genetic engineering method
Using DNA recombination technology and transgenic technology, the gene encoding antipeptide is introduced into microbial cells to express the required protein. This method requires specific biotechnology and equipment, and is costly.
Other methods
There are also some other methods that can be used for laboratory synthesis of antipeptide, such as enzymatic synthesis and photosensitization. These methods require specific equipment and conditions, and have certain technical difficulties.
Antide is an anti androgenic drug widely used in the treatment of advanced castration resistant prostate cancer. Its molecular structure contains benzene ring, imidazole ring, and multiple substituents, which endow it with special biological activity. Its molecular formula is C21H16F4N4OS, with a relative molecular weight of 464.44 g/mol. In this chemical structure, we can analyze its various components as follows:
Benzene ring
The main backbone of the antipeptide molecule is a benzene ring. The benzene ring is a cyclic structure composed of six carbon atoms and three double bonds. The benzene ring plays an important role in the stability and hydrophilicity of molecules.
Imidazole ring
Antipeptide molecules also contain an imidazole ring consisting of five atoms (two nitrogen atoms and three carbon atoms). Imidazole ring is a heterocyclic compound commonly found in many bioactive molecules. It plays an important role in the biological activity of Antipeptide.
Substitution group:
The substituent group in the antipeptide molecule includes a nitrile group (C ≡ N) and a thioamidine group (S). Nitrile groups have an impact on the polarity and pharmacological activity of molecules, while thioamidine groups participate in various reactions and interactions.
Professional
Antipeptide molecules also contain a trifluoromethyl group (CF3). Trifluoromethyl is an electron enriched group that can increase the polarity and solubility of molecules, while also affecting their pharmacological activity.
By binding to androgen receptors and inhibiting their activity, antipeptide can block the androgen signaling pathway and inhibit the growth and spread of prostate cancer cells. Its unique molecular structure and various functional groups play an important role in its biological activity and pharmacological effects. These characteristics make Antipeptide an effective therapeutic drug widely used in the treatment of prostate cancer.
Antid is an important drug with wide applications in the pharmaceutical industry. So, in which fields is Antipeptide widely used? This article will introduce you to multiple application areas of Antipeptide.
Firstly, Antipeptide is widely used in the field of reproduction. It is a gonadotropin-releasing hormone (GnRH) antagonist that can be used to treat some gonadotropin-related diseases and symptoms. For example, Antipeptide can be used in assisted reproductive technology (ART) treatments to help regulate ovarian function, promote oocyte development, and facilitate ovulation processes. In addition, Antipeptide can also be used to treat certain gonadotropin-dependent diseases, such as polycystic ovary syndrome (PCOS) and endometriosis.
Secondly, Antipeptide also has important applications in the field of tumor therapy. It is used as an anti estrogen drug and can be used to treat some estrogen receptor positive breast cancer and ovarian cancer. Antipeptide achieves therapeutic effects by inhibiting the action of estrogen, blocking the growth and division of tumor cells. This makes antipeptide a highly important drug choice for the treatment of patients with breast cancer and ovarian cancer.
In addition, Antipeptide is also being used in research and clinical practice in other fields. For example, it may have potential application value in the treatment of prostate diseases, such as prostate hyperplasia and prostate cancer. In addition, Antipeptide has been studied for the treatment of endocrine disorders such as polycystic ovary syndrome and endometriosis.
In summary, Antipeptide has multiple potential applications in the pharmaceutical industry. It is widely used in the field of reproduction for assisted reproductive technology treatment and treatment of gonadotropin-dependent diseases. In addition, antipeptide also plays an important role in tumor treatment, especially in estrogen receptor positive breast cancer and ovarian cancer patients. In addition, Antipeptide has shown potential application value in research and practice in other fields.
Antid, also known as Iturelix or Orf 23541, is an important pharmacological drug whose core function lies in its function as a gonadotropin-releasing hormone (GnRH) antagonist.
Mechanism of action
Antipeptide competitively binds to the GnRH receptor in the anterior pituitary gland, thereby blocking the release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) induced by GnRH. This mechanism of action makes Antipeptide significantly effective in regulating gonadal hormone secretion. Specifically, Antipeptide can inhibit the response of the anterior pituitary gland to GnRH, leading to reduced secretion of LH and FSH, which in turn affects the function of the gonads.
Pharmacokinetic properties
The pharmacokinetic properties of Antipeptide in vivo determine the duration and intensity of its drug action. Generally speaking, Antipeptide can be rapidly absorbed and reach peak plasma concentration after administration. Its distribution volume is relatively small, indicating that the drug is mainly distributed in plasma and tissues. The metabolic pathway of Antipeptide is not fully understood, but it is known to be metabolized and excreted through the liver and kidneys.
In animal experiments, the administration of Antipeptide is usually subcutaneous injection, with a dosage range of 1 to 15 milligrams per kilogram. The experimental results showed that Antipeptide can induce long-term chemical castration in adult male rats and crab eating monkeys, manifested by dose-dependent inhibitory effects on serum LH (rat only) and testosterone concentrations, as well as the weight of testes, prostate, and seminal vesicles. At higher doses, rats achieved persistent castration like effects, while in crab eating monkeys, only the highest dose induced prolonged inhibitory effects, but with a shorter duration.
In addition to its neuroprotective effects, antide also exhibits potent anti-inflammatory properties. It can suppress the production of pro-inflammatory cytokines and chemokines, thereby reducing inflammation in various tissues. This anti-inflammatory action is particularly relevant in autoimmune disorders and chronic inflammatory conditions, where excessive inflammation contributes to tissue damage and disease progression.
The multifaceted actions of antide make it an attractive candidate for the development of novel therapeutics. Its ability to target both neuronal and immune cells offers a unique advantage in treating complex diseases that involve both neuroinflammation and neurodegeneration. Ongoing research aims to further elucidate the mechanisms underlying the effects and to explore its potential in clinical applications.
Adverse reactions
As a medication that requires injection, Antide may cause redness, swelling, pain, or irritation at the injection site. These reactions are usually local and mild in severity, but may affect the patient's medication adherence.
Although rare, any medication can potentially trigger an allergic reaction. Antide may cause rash, itching, urticaria, and even severe anaphylactic shock. Patients who are allergic to GnRH or similar drugs have a higher risk.
Decreased estrogen levels: Antide may rapidly decrease estrogen levels by inhibiting the secretion of gonadotropins. This may lead to symptoms similar to menopause, such as hot flashes, night sweats, vaginal dryness, emotional fluctuations, headaches, or fatigue.
Bone density changes: Long term use of GnRH antagonists may affect bone density, increase the risk of osteoporosis or fractures, especially in cases requiring long-term treatment.
Weight changes: Some patients may experience weight gain or loss, which may be related to changes in hormone levels or metabolic rate.
Dyslipidemia: Decreased estrogen levels may affect lipid metabolism, leading to increased cholesterol or triglyceride levels and an increased risk of cardiovascular disease.
Long term use or individual sensitivity may lead to dizziness, insomnia, or emotional fluctuations, requiring close monitoring.
Menstrual disorders: Female patients may experience irregular menstruation, amenorrhea, or abnormal uterine bleeding.
Ovarian hyperstimulation syndrome (OHSS): In assisted reproductive technology, GnRH antagonists may increase the risk of OHSS, manifested as ovarian enlargement, abdominal pain, abdominal distention or fluid retention.
Frequently Asked Questions
What is lanthanum fluoride used for?
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Lanthanum Fluoride Patinal® (LaF3) is a versatile coating material for applications in the UV, VIS and IR spectral range. Its predominant application is in the UV wavelength range as a high index material for optical multilayer coatings, especially for semiconductor lithography optics.
Is lanthanum harmful to humans?
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Although lanthanum is considered to have relatively low toxicity for humans, prolonged exposure or elevated concentrations in drinking water could raise concerns for overall health.
Why does its half-life "split" into 1.7 days and 14.5 days? What happened inside the body?
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Because it has a biphasic elimination feature. The half-life of the first phase, about 1.7 days, represents the distribution of the drug from the blood to the tissues; The second phase half-life of 14.5 days reflects its slow release from subcutaneous or tissue "reservoirs". Even with a single intravenous injection, it can be detected in the blood for more than 36 days, and this ultra long effect is not due to slow dissociation of receptor binding, but rather a special distribution behavior in the body.
Why can it be taken orally? Aren't peptide drugs all destroyed by stomach acid?
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It is an exception. In animal experiments, an oral dose of 600 μ g can achieve 73% anti ovulation activity, and 1200 μ g can achieve 100%. The oral absorption mechanism is not fully understood, and may be related to specific D-amino acid modifications and side chain structures that enable it to resist gastrointestinal protease degradation, which is very rare in large peptide molecules.
How does it achieve "no histamine release"? What are the issues with early GnRH antagonists?
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This is its design core. The first generation GnRH antagonists (such as azaline B) often cause allergic reactions (flushing, hypotension) due to histamine release. Antide completely avoids this problem through specific D-amino acid substitutions and side chain modifications (such as nicotinyllysine and isopropyllysine), resulting in no local inflammatory response even at high doses in primates.
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