Name | Pentagastrin |
Synonyms | ay6608 ici50123 lanineamide Pentagastrin gastrodiagnost aspartyl]-l-phenylalaninamide l-methionyl-l-alpha-aspartyl- boc-beta-ala-try-met-asp-phe(nh2) Boc-.beta.-Ala-Trp-Met-Asp-Phe-NH2 T-BOC-BETA-ALA-TRP-MET-ASP-PHE-NH2 N-T-boc-B-ala-trp-met-asp-phe amide N-(tert-butoxycarbonyl)-beta-alanyltryptophylmethionyl-alpha-aspartylphenylalaninamide N-(tert-butoxycarbonyl)-beta-alanyl-L-tryptophyl-L-methionyl-L-alpha-aspartyl-L-phenylalaninamide |
CAS | 5534-95-2 |
EINECS | 226-889-7 |
InChI | InChI=1/C37H49N7O9S/c1-37(2,3)53-36(52)39-16-14-30(45)41-28(19-23-21-40-25-13-9-8-12-24(23)25)34(50)42-26(15-17-54-4)33(49)44-29(20-31(46)47)35(51)43-27(32(38)48)18-22-10-6-5-7-11-22/h5-13,21,26-29,40H,14-20H2,1-4H3,(H2,38,48)(H,39,52)(H,41,45)(H,42,50)(H,43,51)(H,44,49)(H,46,47)/t26-,27-,28-,29-/m0/s1 |
InChIKey | NEYNJQRKHLUJRU-DZUOILHNSA-N |
Molecular Formula | C37H49N7O9S |
Molar Mass | 767.9 |
Density | 1.303±0.06 g/cm3(Predicted) |
Melting Point | 229-230° (dec) |
Boling Point | 1196.6±65.0 °C(Predicted) |
Specific Rotation(α) | D22 -28.8 ±0.5° (DMF) |
Flash Point | 677.489°C |
Solubility | Practically insoluble in water; soluble in 5M ammonia and in dimethylformamide; slightly soluble in ethanol (96%). |
Vapor Presure | 0mmHg at 25°C |
Appearance | powder |
pKa | 4.19±0.10(Predicted) |
Storage Condition | -20°C |
Refractive Index | 1.604 |
MDL | MFCD00076515 |
Physical and Chemical Properties | Colorless needle crystal; Soluble in dimethyl sulfoxide, DMF, insoluble in ether, ethanol, benzene and water; Decomposition point of 229-230 ℃; specific rotation [α]22D-28 °-29 °(0.5-2.0 mg/ml,DMF). |
Hazard Symbols | T - Toxic |
Risk Codes | R61 - May cause harm to the unborn child R36/38 - Irritating to eyes and skin. R20/21 - Harmful by inhalation and in contact with skin. |
Safety Description | S53 - Avoid exposure - obtain special instructions before use. S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. S22 - Do not breathe dust. |
WGK Germany | 1 |
RTECS | AY2970000 |
Reference Show more | 1. Shi Xinghua, Zheng Zhili, Yu Han, Xu zonying, Gao Yining, Wei Weili, Deng Xiulan. Effect of Dangxian-reinforcing spleen therapy on brain-gut peptide in rats with chronic liver injury [J]. Journal of Modern integrated Chinese and Western medicine, 2020,29(33):3649-3653 3707. |
This product is a synthetic pentapeptide, and the chemical structure of the carboxy terminal tetrapeptide of the peptide chain is completely consistent with that of the natural gastrin. This product is colorless needle-like crystal, odorless. Melting point 229~300 °c (decomposition). Almost insoluble in water, ethanol, ether and benzene, insoluble in chloroform, soluble in dimethylformamide and dilute ammonia. This product can promote the secretion of gastric acid, pepsin and internal factors, its gastric acid secretion is equivalent to 1/4 of the natural gastric secretion, equivalent to 125 times of histamine. Function sustainable 10~40min.
This product consists of five amino acids of synthetic peptides, N-[(1, 1-dimethylethoxy) carbonyl]-B-alanyl-L-crocyl-L-methylthiacyl-L-aspartyl-L-benzenepropionamide. The content of C37H49N709S shall be 97.0% ~ 103.0% calculated as dry product.
take this product, precision weighing, plus N ,N-dimethylformamide dissolved and quantitatively diluted into each lml solution containing lOmg, determination according to law (General 0621), the specific rotation is from one to 25.0 ° to one to 29.0 °.
Nausea, abdominal spasm, flushing, Head Pain, dizziness, hypotension and so on. Pancreas, liver, biliary tract disease patients with caution. Allergic patients and patients with severe gastric ulcer should not use.
take this product, add hydrochloric acid solution (1-2), after hydrolysis at 110°C for 24 hours, according to the appropriate amino acid analysis method, containing alanine should be 11.0% ~ 12.2%, aspartic acid is 16.4% to 18.2%, methionine is 18.4% to 20.4%, and phenylalanine is 20.4% to 22.6%.
The ratio of the absorbance at the wavelength of 280nm to 0401 NM should be 1.12 to 1.22 as determined by ultraviolet-visible spectrophotometry (general) of the solution under the content measurement item.
take this product, put it in a phosphorus pentoxide dryer, dry it at room temperature and under reduced pressure for 24 hours, and the weight loss shall not exceed 0.5% (General rule 0831).
take this product, add methanol-concentrated ammonia solution (24:1) mixed solution to dissolve and dilute to prepare a solution containing 5mg per 1ml as a test solution; 1ml was precisely weighed, placed in a 50ml measuring flask, and diluted to a scale with the above mixed solution to serve as a control solution. According to the thin layer chromatography (General 0502) test, absorb the above two solutions each 1UL, respectively point on the same silica gel G thin layer plate, with ether-glacial acetic acid-water (10:2:1) for development, expand, dry, dry at 100°C for 2 minutes, spray with P-dimethylamine benzaldehyde solution [take p-dimethylamino benzaldehyde lg, add methanol-hydrochloric acid (3:1) mixed to dissolve], heat to color development at 100°C. Test solution such as impurity spots, compared with the control solution of the main spot, not deeper (2.0%).
take an appropriate amount of this product, precision weighing, add 0.Ol mol / L ammonia solution to dissolve and quantitatively dilute to make a solution containing about 50ug per 1 ml, the absorbance was measured at a wavelength of 280mn according to ultraviolet-visible spectrophotometry (General rule 0401 ), and the absorption coefficient of C37H49N709S was calculated as 70.
diagnostic medication.
light shielding, sealed storage.
This product is a sterilized aqueous solution of pentagastrin. The content of pentagastrin (C37H49N709S) should be 90.0% to 110.0% of the labeled amount.
This product is colorless and clear liquid.
take the product, according to the five peptide gastrin under the identification (1) test, showed the same results.
precision: take an appropriate amount of this product (about 0.75mg equivalent to pentagastrin) and dilute it quantitatively with 0.01mol / L ammonia solution to make a solution containing about 50ug per 1 ml, that's right.
Same as pentagastrin.
2ml : 400ug
light shielding, closed, stored in cold place.
Overview | pentagastrin, also known as pentapeptide, Peptavlon. It is a synthetic pentapeptide, which can promote the secretion of gastric acid, pepsin and internal factors. Its gastric acid secretion is equivalent to 1/4 of natural gastrin, but stronger than Histamine phosphate and ammonia hydrochloride. It is clinically used for examination of gastric secretory function and pancreatic function. |
preparation method | with tert-butoxycarbonyl-β-alanine, tryptophan, methionine, aspartic acid, after protecting the side chain with a protective agent, the side chain is condensed with a condensing agent, and then the protective agent is removed and purified to obtain pentagastrin. |
pharmacological effects | pentagastrin can promote the secretion of gastric acid, pepsin and internal factors, its role in promoting gastric acid secretion is equivalent to the 1/4 of endogenous gastrin, but stronger than Histamine phosphate and hydrochloric acid, the effect can last 10 to 40 minutes. |
function and use | pentagastrin is a kind of synthetic gastrin polypeptide. After injection, it can produce a similar effect to gastrin, increase gastrointestinal peristalsis, promote the secretion of gastric acid, pepsin, etc., and the peak secretion time is 10~40 minutes. The role of this product is stronger than histamine and betazol, systemic reaction less. Now gradually to the goods instead of histamine for gastric secretion function test, and try to severe atrophic gastritis, can improve its symptoms. |
usage and dosage | subcutaneous injection or intramuscular injection: 6 μg/kg, or the same dose plus 0.9% sodium chloride injection diluted in 1 hours after intravenous infusion. |
adverse reaction | was mild, with occasional Nausea, abdominal spasm, skin flushing, Head Pain, somnolence, dizziness and hypotension. |
note | 1. Allergic to this product, allergic history, acute peptic ulcer disease patients disabled, active pancreas, liver, gallbladder disease patients with caution. 2. Smoking can reduce the effect of this product. |
Main references | / [1] Ren Juanqing, editor-in-chief. Practical Drug Handbook. Jinan: Shandong Science and Technology Publishing House. 2012. Page 1881. [2] Liu Fuqiang and other editors. Physician's Desk medication reference. Beijing: Chinese Medicine Press. 2012. |
Use | is used for biochemical research and clinical diagnosis. |
production method | with tert-butoxycarbonyl-β-alanine, tryptophan, methionine, aspartic acid, phenylpropionamide as raw materials, after protecting its side chain with a protective agent, it is condensed with a condensing agent in turn, and then purified by removing the protective agent. |
toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |