Protirelin (TRH)

The Structure of Protirelin

What is Protirelin?

Protirelin, also known as thyrotropin-releasing factor (TRF), thyroid-stimulating hormone(TRH). It is essentially a thyroid-stimulating hormone.^[1][14] It controls the production of thyroxine and triiodothyronine, hormones that control everything from metabolic rate to neuromuscular function, as well as heart rate and heat production.^[8]

The main function of Protirelin is to stimulate the pituitary gland to release thyroxine. The thyrotropin peptide is responsible for regulating the growth and function of the thyroid gland. Protirelin is responsible for maintaining the health of thyroid hormones and their functions.^[2][6]It has hormones, pararegulatory factors, neurotransmitters, and neuromodulators original effects. It can effectively treat thyroid diseases and has antidepressant and antisuicide functions. Research also suggests that it plays a role in controlling hair growth.^[1][5][9]

Protirelin has also been studied for its possible benefits in the aging process, dietary behavior, reduction of free radicals,and modulation of the autonomic nervous system. Protirelin can be used to test the anterior lobe response of the pituitary gland in people who may have certain thyroid conditions. Using this drug as a test can help find problems or make sure you are using the correct dose of medicine.^[2][7]

Mechanism of action of Protirelin against shock

Protirelin increases the number of β-receptors and DA-receptors, improves the affinity of β-receptors, increases the level of cAMP in important vital organs, and strengthens the role of Iso and DA in promoting calcium influx. Body and DA-receptor, so as to play the role of anti-shock.

The role of δ-opioid receptors and antagonizing β-endorphins can significantly inhibit cardiovascular function and reduce blood flow velocity, while Protirelin can antagonize the cardiovascular effects of β-endorphins and effectively inhibit their effect on the cardiovascular system affect.^[11] It can have an anti-shock effect by down-regulating δ-opioid receptors in the brain, resisting β-endorphin, and inhibiting the cardiovascular effects of shock animals.

Protirelin can increase the activity of endogenous superoxide dismutase in the heart, liver, kidney, lung and intestine of shock organisms, significantly inhibit the excessive oxidation of lipid in injured spinal cord tissue, and improve the mitochondria of liver cells in traumatic shock organisms. It plays a role in reducing lipid peroxidation damage and protecting mitochondrial function during shock.^[4]

Benefits of Protirelin

1. Treat depression.

As early as the 1970s, people realized that Protirelin could reduce suicidal thoughts, and studies have shown that the effect of TRH on depression is more pronounced when taken at night, which may be due to the natural circadian rhythm of TRH itself when taken at night.^[10]

2. Exercise motor memory.^[3]

Motor memory, also known as muscle memory, is a procedural memory that develops through repeated practice of a specific movement. Studies have shown that for some organisms lacking the TRH gene, their learning speed for specific tasks is slow, and exogenous TRH can improve their learning speed.

3. Combating opioid overdose.

Opioids inhibit the respiratory drive in the brainstem and can be fatal in overdose. Protirelin has similar benefits to Naloxone, but with fewer side effects, and their mechanisms of action are different, suggesting they could be used synergistically, or as a backup should the other prove ineffective.^[13] Protirelin promises to be a potential cornerstone in the fight against opioid overdose.

4. Against traumatic shock.

Studies have shown that Protirelin can effectively increase the average arterial blood pressure and respiratory rate, protect the respiratory function of mitochondria, and prevent the decrease of arterial blood oxygen saturation, which is equivalent to the current method for treating acute blood loss, and has become a key component of emergency shock treatment in ambulances part.

5. Affect the aging process.

Protirelin has the potential to protect specific organs from oxidative damage and age-related degeneration.^[12] It reduces the buildup of amyloid plaques in the kidneys, a common factor in decreased kidney function. By inhibiting plaque formation, kidney function may be preserved as the individual ages.

6. Treat narcolepsy.

Protirelin can prevent the reuptake of norepinephrine by nerve endings, and can also be used to treat narcolepsy with cataplexy symptoms.

7. Treatment of children with neurological diseases (including intractable epilepsy).

TRH and its peptide analogs can be used as add-on therapy and monotherapy in the treatment of epileptic disorders, and it is a possible treatment for intractable epilepsy. Unlike traditional epilepsy drugs, TRH may contribute to epileptic network plasticity, similar to its known trophic effects on spinal motor neurons.

8. TRH deficiency is important for disease development.

The researchers noticed that changes in TRH levels were associated with thyroid disease. There is also growing interest in investigating the potential of TRH supplementation to reduce the severity of non-thyroid disease in some cases and as an adjunctive treatment.

9. Accelerate lung maturation.

Protirelin can be used in combination with glucocorticoids before delivery to accelerate fetal lung maturation, thereby reducing the incidence of infant respiratory distress syndrome.

10. Acts as a stimulant.

TRH is a general stimulant that elicits elevated questions when injected intracerebroventricularly, suggesting a role in central thermoregulation. Studies in mice may shed further light on the non-growth-promoting role of TRH.

11. Affect TSH.

TRH can induce the secretion and synthesis of TSH in the pituitary gland. Injecting TRH into the human body will increase the TSH in the body by as much as 22 times within half an hour. It can also affect its biological activity by acting on the glycosylation pattern of TSH.

12. Stimulate the secretion of prolactin.

Protirelin stimulates the pituitary gland to secrete prolactin and induces hyperprolactinemia in some patients with hypothyroidism. Although TRH is dispensable for pregnancy and lactation, it is required for prolactin function.

Synthesis of Protirelin Powder

Protirelin is a synthetic peptide used to treat depression and thyroid disease. Synthesis of Protirelin powder was first produced by Eli Lilly by standard solid-phase peptide synthesis. Eli Lilly and Company published the synthesis method of Protirelin through a patent application, so the large-scale production process of this compound has now been reported. As a result, more and more qualified manufacturers produce Protirelin powder.

Protirelin is a synthetic peptide. It is administered as a subcutaneous injection and is sold on Polypeptide.ltd as a raw powder and as a lyophilized powder.

Protirelin original powder dosage form

Protirelin powder is an active ingredient in powder form. Protirelin raw powder is the raw material for the production of vials of tezepatide freeze-dried powder. It is not ready for personal use. For research purposes only.

Reconstitution (Protirelin finished vial)

Protirelin is available in lyophilized powder form for reconstitution. This lyophilized powder is usually supplied as a vial or a kit of vials. The lyophilized powder is then mixed with a suitable diluent, such as bacteriostatic or sterile water, to form an injection solution. Reconstitution instructions may vary depending on the specific product and manufacturer of Protirelin, so it is important to follow the guidelines provided carefully.

Protirelin Vs Naloxone

Naloxone is an opioid antagonist that can improve a variety of cardiovascular functions in traumatic shock caused by endotoxemia, hemorrhage, anaphylaxis or the spine, and can quickly cross the blood-brain barrier.

Protirelin inhibits side effects on the cardiovascular system by sensitizing adrenergic β-receptors and dopamine receptors, can reduce lipid peroxidation damage during shock, and protect mitochondrial function, which has become a potential cornerstone in the fight against opioids.

Studies have shown that antagonistic morphine analgesics such as Naloxone have side effects such as addiction, immobilization, respiratory depression and death, and in the case of an overdose of opioids, Naloxone will be ineffective or short-acting. In addition, if opioid use disorder occurs, Naloxone can cause immediate withdrawal symptoms, irritability, and possibly even harmful behavior for medical staff. On the contrary, Protirelin has fewer side effects and has a certain regulating effect on the above-mentioned side effects. Although it will lead to faster and deeper breathing and increased gastrointestinal motility, it will not affect the change in heart rate. TRH is an effective one-by-one drug against opioid overdose.

Depression and the circadian rhythm of Protirelin

Researchers studied circadian thyrotropin (TSH) and prolactin (PRL) responses in 35 drug-naive DSM III-R hospitalized patients with major depressive episodes.

Response to synthetic thyrotropin-releasing hormone (protirelin) infusions (200 g IV) at 8 a.m. and 11 p.m. PRL and TSH responses were lower in each group at 8 a.m. than at 11 p.m. The difference between ΔTSH at 11p.m. and ΔJTSH at 8a.m. (ΔTSH) was significantly smaller in depressed patients compared with controls. The PRL response to protirelin was not diminished in depressed patients.

TSH circadian parameters (i.e., median and amplitude) correlated strongly with the response to protirelin in most individuals. 8a.m. TSH and 11p.m. TSH.In addition to ΔΔ PRL, these correlations can also be observed with PRL. In contrast, TSH mesoscale and amplitude were lower in depressed patients. In contrast, there were no significant differences in PRL median and magnitude between diagnostic groups. Thus, ΔΔTSH is a chronobiological improvement of thyroid axis dysfunction in major depressive disorder. TRH receptors for pituitary thyrotropin are blunted in major depressive disorder because of a blunted TSH response to pretirelin.

Other related to Protirelin

Experiments in animals have shown that TRH is dose-dependent, possibly through an interaction with the opioid peptide system. TRH affects motor activity. Indeed, this tripeptide leads to more exploratory activity and spontaneous movement by interacting with the dopaminergic neurotransmitter system at the level of the nucleus accumbens.

The neuropharmacological effects of TRH include arousal and excitability, leading to complete central nervous system depression. This suppression may be natural (e.g., hibernation), pharmacologically induced (e.g., alcohol or barbiturates), or traumatic (e.g., coma). Stimulation of cholinergic neurons in the septal hippocampus as well as TRH-containing terminals in the lateral septum, as well as a particular concentration of TRH receptors in the medial septum and Broca’s diagonal band, are responsible for this excitatory effect. It has also been suggested that TRH, located in the pineal gland, is involved in neuronal arousal mechanisms. Activation and arousal of TRH are associated with plant functions (body temperature, circulation,and gastrointestinal tract) under shock conditions of various origins. The rationale for TRH in the initial treatment of coma induced by traumatic brain injury and in the treatment of endogenous depression is that these stimulating activities stimulate the central nervous system.

The most attractive property of TRH is protection against experimental spinal cord injury leading to neurological deficits, especially spasticity and ataxia. Through electrophysiological experiments, TRH can depolarize motor neurons in the frog spinal cord, thereby enhancing monosynaptic reflexes. TRH is also beneficial in rat fetal spinal cord cultures. On this basis, TRH has been used to treat spinocerebellar degeneration and Charcot syndrome (amyotrophic lateral sclerosis). This therapeutic approach is further supported by the increased density of TRH spinal receptors due to the blockage of spinal afferents in rats. In addition, recent studies have yielded positive results regarding the possible use of TRH in the treatment of Alzheimer’s disease.

The side effects of Protirelin

Common side effects

• flushed skin
• headache, dizziness
• nausea
• stomachache
• dry mouth

Unusual side effects

• anxiety
• drowsiness
• sweating
• stabbing pain

Serious side effects

• Eye symptoms: such as sudden vision loss, blurred vision, narrowed vision, eye pain or swelling, or seeing halos around lights;
• Heart symptoms: such as a fast, irregular, or pounding heartbeat; fluttering in your chest; shortness of breath; sudden dizziness, lightheartedness, or passing out;
• Severe headache, confusion, slurred speech, weakness in arms or legs, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or shaking

Dosage and Administration

Protirelin is given intravenously with the patient in the supine position. After administration as a bolus over 15 to 30 seconds, the patient remains in the supine position until all scheduled blood samples are collected. Blood pressure should be measured periodically before and within 15 minutes of taking Protirelin. You should urinate before injecting Protirelin.

• Adults: 500 micrograms. Dosages range from 200 to 500 mg. 500 mg is considered the best dose for most patients. Doses above 500mg are unlikely to increase TSH.
• Children 6-16 years old: 7 mg/kg, up to a maximum dose of 500 mg;
• Infants and children under 6 years: Inexperienced in this age group, the dose is 7 mg/kg.

A blood sample for TSH assessment should be drawn immediately before Protirelin injection and then another blood sample should be drawn 30 minutes after injection.

When the drug is repeated, the TSH response to Protirelin decreases. Therefore, if the Proterelin test needs to be repeated, it is recommended to do it after 7 days.

Protirelin for sale/Protirelin supplier

Protirelin is a synthetic polypeptide that can alleviate hypoxia and pathological changes in vital organs, and has a good therapeutic effect on severe traumatic shock and depression. It can also regulate the secretion of thyroid hormone and prolactin. In addition, the ability of TRH to induce analgesia is dose-dependent, and studies suggest that this may be achieved through interactions with the opioid peptide system. Recent studies have yielded encouraging results regarding the possible therapeutic use of TRH for the treatment of Alzheimer’s disease.

However, much research is still needed to fully understand and utilize its therapeutic potential of Protirelin. Researchers interested in experimenting with Protirelin want to make sure they are sourcing this material from a reliable supplier. If you are looking to buy Protirelin online, please exercise caution and make sure you are getting the peptide from a reputable and trustworthy manufacturer. Polypeptide.Ltd is a highly reliable manufacturer of pharmaceutical grade peptides.

Summary

Protirelin stimulates the anterior pituitary gland to secrete pituitary thyrotropin and also increases prolactin secretion. It is a synthetic tripeptide, which is structurally considered to be the same as the natural thyrotropin-releasing hormone produced by the hypothalamus. It is a reference indicator for biochemical research and clinical diagnosis of hypothalamus-pituitary thyroid dysfunction.

Protirelin peptide, a small peptide hormone produced by the anterior pituitary gland, is a thyrotropin-releasing hormone. It may be used to test the anterior lobe response of the pituitary gland in some patients with certain thyroid disorders. If you are looking for a professional, top-grade Peptide Protirelin manufacturer or factory, here is the right place for you.

Protirelin is a tripeptide (pyro-glutamyl-histidyl-proline amide) that elicits these effects through interaction with cell surface receptors. It has also been studied for its benefits in the aging process, dietary behaviour, reduction of free radicals and modulation of the autonomic nervous system.

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Q: Is Protirelin safe?

A: Researchers are still studying the safety and effectiveness of protirelin. This fact suggests that the compound should not be considered as a form of treatment for any disease. Larger studies are needed here.

Q: Will Protirelin increase the subject’s body temperature?

A: TRH tartrate dissolved in saline was administered intraperitoneally to male Wistar rats weighing 200-250 g at doses of 1, 5, 10 and 20 mg/kg. An electronic thermistor is inserted 5 cm inside the anus to measure rectal temperature. TRH tartrate causes a dose-dependent transient increase in body temperature.

Q: Where can I buy Protirelin?

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Q: What happens if there is too much thyrotropin-releasing hormone in my body?

A: There are no known cases of thyrotropin-releasing hormone excess.

Q: What happens if my TSH is too low?

A: If a person has too little TSH, they can develop an underactive thyroid (hypothyroidism). This is a rare condition, usually due to an injury or tumor that destroys this area of the hypothalamus. This condition is called secondary or central hypothyroidism.

Q: How is thyrotropin-releasing hormone controlled?

A: As the name suggests, TSH’s main role is to stimulate the pituitary gland to release thyroid-stimulating hormone (also known as thyrotropin). Thyrotropin-releasing hormone is the master regulator of thyroid growth and function (including secretion of the thyroid hormones thyroxine and triiodothyronine). These hormones control the body’s metabolic rate, heat production, neuromuscular function, and heart rate, among other things. If there is not enough thyroid hormone available to the brain, this is detected by the hypothalamus and thyrotropin-releasing hormone is released into the blood supply to the pituitary gland.

Q: What is Protirelin?

A: Protirelin is essentially a thyroid-stimulating hormone. It stimulates the anterior pituitary gland to produce a hormone called thyroid-stimulating hormone, or TSH. Any TSH in turn stimulates the thyroid gland and can be used to test how the anterior pituitary gland responds in people who may have certain disorders involving the thyroid gland. is a diagnostic agent for the evaluation of thyroid, pituitary, or hypothalamic dysfunction.

Q: What is the use of Protirelin?

A: Protirelin is used to test the response of the anterior pituitary gland in people who may have certain disorders involving the thyroid gland. Testing with this drug may help find problems or make sure the correct dose of the drug is being used.

Q: Can TRH increase prolactin?

A: Thyrotropin-releasing hormone (TRH) stimulates prolactin release and 45Ca 2+ efflux in GH3 cells (a clone of rat pituitary cells). Elevation of extracellular K+ also induces prolactin release and increases 45Ca2+ efflux from these cells

Q: Why does Protirelin stimulate prolactin?

A: Protirelin-induced signaling events also include activation of extracellular signal-regulated kinase (ERK) and induction of MAP kinase phosphatase, an inactivator of activated ERK. TRH stimulates prolactin synthesis by activating ERK, which is released through elevated intracellular Ca(2+).