Pyr-His-Pro-NH2
L-pyroglutamyl-L-histidyl-L-prolinamide
CAS: 24305-27-9
Molecular Formula: C16H22N6O4
Pyr-His-Pro-NH2 - Names and Identifiers
| Name | L-pyroglutamyl-L-histidyl-L-prolinamide |
| Synonyms | TRH THR 2-3 THR 1-2 PROTIRELIN Protirelin Pyr-His-Pro-NH2 PYR-HIS-PRO-NH2 PGLU-HIS-PRO-NH2 H-pGlu-His-Pro-NH2 PYROGLU-HIS-PRO NH2 PYR-HIS-PRO-NH2(TRH) PYROGLU-HIS-PRO AMIDE pglu-his-pro amide acetate pglu-his-pro amide free base 5-oxoprolylhistidylprolinamide Thyrotropin releasing hormone (TRH) L-pyroglutamyl-L-histidyl-L-prolinamide |
| CAS | 24305-27-9 |
| EINECS | 246-143-4 |
| InChI | InChI=1/C16H22N6O4/c17-14(24)12-2-1-5-22(12)16(26)11(6-9-7-18-8-19-9)21-15(25)10-3-4-13(23)20-10/h7-8,10-12H,1-6H2,(H2,17,24)(H,18,19)(H,20,23)(H,21,25) |
| InChIKey | ITYONPBTNRIEBA-SRVKXCTJSA-N |
Pyr-His-Pro-NH2 - Physico-chemical Properties
| Molecular Formula | C16H22N6O4 |
| Molar Mass | 362.38 |
| Density | 1.1675 (rough estimate) |
| Melting Point | >143°C (dec.) |
| Boling Point | 494°C (rough estimate) |
| Specific Rotation(α) | -50 (D/25℃) (c=1.5, H2O)-65.5 (D) (c=1.0, H2O) |
| Flash Point | 545.5°C |
| Solubility | H2O: 10mg/mL, clear, colorless |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | powder |
| Color | White to Off-White |
| Merck | 13,9663 |
| BRN | 770238 |
| pKa | 13.05±0.20(Predicted) |
| PH | pH (10g/l, 25℃) : 3.0～4.0 |
| Storage Condition | −20°C |
| Stability | Hygroscopic |
| Refractive Index | 1.6000 (estimate) |
| Physical and Chemical Properties | White dry freeze-dried powder, hygroscopic. Specific optical rotation [α]25D-65.5 °(1%, water). Soluble in water. |
Pyr-His-Pro-NH2 - Risk and Safety
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| WGK Germany | 2 |
| RTECS | TW3580000 |
| FLUKA BRAND F CODES | 10-21 |
Pyr-His-Pro-NH2 - Reference
| Reference Show more | 1. Shan, Tong, et al. "Proteomics Based Mongolian Medicine Modified Sugmul-7 Mechanism of Regulating Endocrine Function in Hyperplasia of the Breast." Clinical Medicine Research 9.1 (2020): 11.doi: 10.11648/j.cmr.20200901.13 |
Pyr-His-Pro-NH2 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.76 ml | 13.798 ml | 27.595 ml |
| 5 mM | 0.552 ml | 2.76 ml | 5.519 ml |
| 10 mM | 0.276 ml | 1.38 ml | 2.76 ml |
| 5 mM | 0.055 ml | 0.276 ml | 0.552 ml |
Last Update：2024-01-02 23:10:35
Pyr-His-Pro-NH2 - Reference Information
| Overview | Protorelin (Protirelin), formerly known as thyrotropin-releasing hormone (Thyrotropin-releasing hormone), is a tripeptide hormone released by the hypothalamus. In the late 2060s, it was first purified and artificially synthesized from the hypothalamic tissues of sheep and pigs. TRH is widely distributed in the central nervous system and some peripheral organs. In addition to endocrine effects, it also plays the role of endogenous excitatory neurotransmitters, which can produce a wide range of central and peripheral effects. It has a certain antagonistic effect of endogenous opioid receptors, but it does not antagonize the analgesic effect of morphine. In 1981, it was first reported that prorelin had an anti-shock effect. |
| pharmacology | experiments have proved that prorelin does not have naloxone to fully antagonize the analgesic, addiction, immobilization, respiratory depression and lethal effects of morphine drugs. In the isolated guinea pig ileum experiment, prorelin is different from naloxone. It does not antagonize DHE and inhibits the contraction response of guinea pig ileum. The concentration response curve shifts slightly to the left. Therefore, prorelin has no antagonistic effect on the μ-opioid receptor that mediates analgesia. Therefore, prorelin is better than naloxone for war trauma shock. Blood pressure slightly increased, while breathing deepened and accelerated, gastrointestinal peristalsis increased, but heart rate had little effect. Luo Ruilin does not antagonize the analgesic effect of morphine, and has a certain excitatory effect on the breathing, circulation and central nervous system of normal animals. |
| Use | In addition to the treatment of shock, protorelin has other uses, such as the treatment of hypothalamic hypothyroidism and central hyperthyroidism in endocrinology. Psychiatry is used to treat depression and schizophrenia. Neurology is used to treat brain and spinal cord injury, coma for various reasons, amyotrophic lateral sclerosis, spinal cerebellar degeneration, senile dementia, epilepsy, etc. The diagnostic aspect is used for the diagnosis of hyperthyroidism. Therefore, protorelin is a drug with good development value and worthy of further research to expand the scope of application. It can stimulate the secretion of thyrotropin from the anterior pituitary gland and cause the release of prolactin. Reference index for biochemical research and clinical diagnosis of hypothalamic pituitary thyroid dysfunction. |
| pharmacokinetics | prorelin is a two-compartment open model, which is widely distributed in various tissues and organs after intravenous injection, with the highest concentration of pituitary gland and kidney, most of which are degraded in blood and mainly excreted by kidney. |
| development prospect | prorelin is a tripeptide hormone in the body. its chemical structure is relatively simple and has been artificially synthesized. freeze-dried powder can be stored for one year at normal temperature, and can be stored for several years at 4 ℃. the price is moderate. Pharmacological dose of protorelin has a clear anti-shock effect, and has a clear therapeutic effect on a variety of circulatory shocks such as hemorrhagic, infectious, traumatic, and spinal shock. The literature reports on anaphylactic shock, platelet activating factor and The hypotension caused by leukotriene also has an anti-shock effect, and its anti-shock effect is superior to commonly used anti-shock drugs in many aspects. For example, compared with vasoconstrictor drugs, the pressure is more moderate, and the pressure is increased at the same time to improve microcirculation. Compared with vasodilators, it does not rely on sufficient volume recovery, and it still has a fairly good effect when used without infusion. Compared with naloxone, it does not antagonize μ-opioid receptors, does not affect the use of morphine, and is especially suitable for traumatic shock. Moreover, the toxicity of prorelin is small, the treatment dose width is large, no teratogenicity, mutagenicity, and lethal effect. Therefore, protorelin may be a promising new type of anti-shock drug. At present, trauma has become a major cause of death after cardiovascular diseases in human beings. More than 30% of trauma died of shock. Shock induced by other causes such as septic shock (mortality rate as high as 30% -50% ), anaphylactic shock and hemorrhagic shock are also common. There are still many shortcomings of anti-shock drugs, so it is very important to develop new anti-shock drugs. |
| application | 1. treatment of shock; 2. treatment of hypothalamic hypothyroidism and central hyperthyroidism in secretory department; 3. treatment of depression and schizophrenia in psychiatric department; 4. treatment of brain and spinal cord injury in neurology department, coma of various causes, amyotrophic lateral sclerosis, spinal cerebellar degeneration, senile dementia, epilepsy, etc; 5. Diagnostic aspects for the diagnosis of hyperthyroidism. |
| References | [1] Hu Deyao, Liu Liangming, Zhou Xuewu, Lu Ruquan, He Fengci, Chen Huisun. Preclinical pharmacology of antishock drug protorelin [J]. Chinese Journal of Pharmacology and Toxicology, 2000(04):241-246. [2] Li Xiangping, Tang Jiyou, Chi Zhaofu. The basis and clinic of thyrotropin-releasing hormone and its analogs in epilepsy [J]. Foreign medicine. Neurology Neurosurgery Volume, 2000(02):82-85. [3] Liu Liangming, Chen Huisun, Hu Deyao, Lu Ruquan. Thyrotropin-releasing hormone antagonizes the inhibitory effect of β-endorphin on cardiovascular system [J]. Journal of the third military medical university, 1994(06):402-404. |
Last Update：2024-04-09 20:52:54
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Product Name: Protirelin Visit Supplier Webpage Request for quotationCAS: 24305-27-9
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Mobile: 86+15671228036
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Product Name: Trh Visit Supplier Webpage Request for quotationCAS: 24305-27-9
Tel: 18301782025
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Mobile: 18021002903
QQ: 3008007409
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Product Name: TRH, Thyroliberin, Protirelin Request for quotation
CAS: 24305-27-9
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QQ: 1761863581Send QQ message
CAS: 24305-27-9
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Email: qilin@cellmano.com
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