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药品详细

Pentagastrin(五肽胃泌素)

化学结构式图
中文名
五肽胃泌素
英文名
Pentagastrin
分子式
C37H49N7O9S
化学名
(3S)-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}-3-[(2S)-2-[(2S)-3-(1H-indol-3-yl)-2-(3-{[(2-methylpropoxy)carbonyl]amino}propanamido)propanamido]-4-(methylsulfanyl)butanamido]propanoic acid
分子量
Average: 767.891
Monoisotopic: 767.331246891
CAS号
5534-95-2
ATC分类
V04C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid. [PubChem]

生产厂家
  • Wyeth ayerst laboratories
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Weintraub HS, Rudolph A: Combination Therapy for Managing Difficult-to-Treat Patients With Stage 2 Hypertension: Focus on Valsartan-Based Combinations. Am J Ther. 2010 Jun 9. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Polypeptides
  • Tryptamines and Derivatives
Substructures
  • Polypeptides
  • Ethers
  • Hydroxy Compounds
  • Acetates
  • Indoles and Indole Derivatives
  • Carbamates and Derivatives
  • Amino Ketones
  • Pyrroles
  • Benzene and Derivatives
  • Carboxylic Acids and Derivatives
  • Tryptamines and Derivatives
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Phenylpropylamines
  • Keto-Acids
  • Amphetamines
适应症
药理
Indication Used as a diagnostic aid for evaluation of gastric acid secretory function
Pharmacodynamics Pentagastrin is indicated as a diagnostic aid for evaluation of gastric acid secretory function. It is effective in testing for anacidity (achlorhydria) in patients with suspected pernicious anemia, atrophic gastritis, or gastric carcinoma. It is also effective in determining the reduction in acid output after operations for peptic ulcer, such as vagotomy or gastric resection.
Mechanism of action The exact mechanism by which pentagastrin stimulates gastric acid, pepsin, and intrinsic factor secretion is unknown; however, since pentagastrin is an analogue of natural gastrin, it is believed that it excites the oxyntic cells of the stomach to secrete to their maximum capacity. Pentagastrin stimulates pancreatic secretion, especially when administered in large intramuscular doses. Pentagastrin also increases gastrointestinal motility by a direct effect on the intestinal smooth muscle. However, it delays gastric emptying time probably by stimulation of terminal antral contractions, which enhance retropulsion.
Absorption Rapidly absorbed after parenteral administration.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Primarily hepatic
Route of elimination Not Available
Half life 10 minutes or less
Clearance Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 229 dec °C PhysProp
logP 1.6 Not Available
Predicted Properties
Property Value Source
water solubility 3.09e-03 g/l ALOGPS
logP 1.57 ALOGPS
logP 1.24 ChemAxon
logS -5.4 ALOGPS
pKa (strongest acidic) 4 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 8 ChemAxon
hydrogen donor count 8 ChemAxon
polar surface area 250.91 ChemAxon
rotatable bond count 23 ChemAxon
refractivity 199.97 ChemAxon
polarizability 80.96 ChemAxon
药物相互作用
食物相互作用
Not Available

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