Pentagastrin, >=95% (HPLC), powder

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 肽模拟物
• 英文名称: Pentagastrin, >=95% (HPLC), powder
• 英文别名: 4-[(1-amino-1-oxo-3-phenylpropan-2-yl)amino]-3-[[2-[[3-(1H-indol-3-yl)-2-[3-[(2-methylpropan-2-yl)oxycarbonylamino]propanoylamino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-oxobutanoic acid
• 化学式: C₃₇H₄₉N₇O₉S
• 分子量: 767.9
• InChiKey: NEYNJQRKHLUJRU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  54
• 可旋转键数：
  22
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  276
• 氢给体数：
  8
• 氢受体数：
  10

ADMET

毒理性

• 相互作用

盐酸雷尼替丁抑制了15名十二指肠溃疡患者的五肽胃泌素刺激的胃分泌。

RANITIDINE HYDROCHLORIDE INHIBITED PENTAGASTRIN STIMULATED GASTRIC SECRETION IN 15 PT WITH DUODENAL ULCERATION.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

副作用是轻微和短暂的。这些可能包括恶心、眩晕、晕厥、潮红和温暖感。

...SIDE EFFECTS ARE MINOR & TRANSIENT. THESE MAY INCL NAUSEA, DIZZINESS, FAINTNESS, FLUSHING, & SENSATION OF WARMTH.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

在给一名56岁的男性患者输注不超过40微克的五肽胃泌素时，患者突然晕倒，变得冰冷且面色苍白，3分钟内无法触及桡动脉脉搏。一旦脉搏恢复，患者的脉搏降至每分钟35次，出现严重心动过缓。

NOT MORE THAN 40 UG OF PENTAGASTRIN HAD BEEN INFUSED WHEN 56-YR-OLD MALE PT FAINTED & BECAME COLD & WHITE WITH NO RADIAL PULSE PALPABLE FOR 3 MIN. ONCE PULSE RETURNED PT HAD SEVERE BRADYCARDIA OF 35/MIN.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 人类毒性摘录

患者在服用胃泌素后，弥漫性食管痉挛发展成了强烈的、自发的、不规则的收缩。

PT WITH DIFFUSE ESOPHAGEAL SPASM DEVELOPED POWERFUL, SPONTANEOUS, IRREGULAR CONTRACTIONS FOLLOWING ADMIN OF PENTAGASTRIN.

来源:Hazardous Substances Data Bank (HSDB)

毒理性

• 非人类毒性值

LD50 大鼠 静脉注射 160-170 毫克/千克

LD50 RATS INTRAVENOUS 160-170 MG/KG

来源:Hazardous Substances Data Bank (HSDB)

吸收、分配和排泄

口服五肽胃泌素的活动通过其对4名健康受试者、2名十二指肠溃疡患者和1名伴有十二指肠溃疡的环形胰腺患者的胃酸刺激作用来确定。

ACTIVITY OF ORAL PENTAGASTRIN WAS DETERMINED BY ITS ACTION AS GASTRIC ACID STIMULANT IN 4 HEALTHY SUBJECTS, 2 PT WITH DUODENAL ULCERS, & 1 PT WITH ANNULAR PANCREAS IN ASSOC WITH DUODENAL ULCER.

来源:Hazardous Substances Data Bank (HSDB)

文献信息

• Pharmaceutical compositions of drug-oligomer conjugates and methods of treating diseases therewith
  申请人：——

  公开号：US20030069170A1

  公开（公告）日：2003-04-10

  Pharmaceutical compositions that include a drug-oligomer conjugate, a fatty acid component, and a bile salt component are described. The drug is covalently coupled to an oligomeric moiety. The fatty acid component and the bile salt component are present in a weight-to-weight ratio of between 1:5 and 5:1. Methods of treating diseases in a subject in need of such treatment using such pharmaceutical compositions are also provided, as are methods of providing such pharmaceutical compositions.

  描述了包括药物-寡聚物共轭物、脂肪酸成分和胆盐成分的药物组合物。药物以共价键连接到寡聚物基团上。脂肪酸成分和胆盐成分以1:5至5:1的重量比存在。还提供了利用这种药物组合物治疗需要此类治疗的受试者的方法，以及提供这种药物组合物的方法。
• Calcium salts of 1,5-benzodiazepine derivatives, process for producing the salts and drugs containing the same
  申请人：——

  公开号：US20030096809A1

  公开（公告）日：2003-05-22

  Provided are calcium salts of a 1,5-benzodiazepine derivative represented by the following formula (I): 1 (wherein, R 1 represents a lower alkyl group, R 2 represents a phenyl or cyclohexyl group, and Y represents a single bond or a lower alkylene group); a process for preparing the salts; and drugs containing the same as the active ingredient. The compounds exhibit a potent inhibitory activity against the secretion of gastric acid and potent antagonism against gastrin and/or CCK-B receptor.

  提供的是以下公式（I）所代表的1,5-苯二氮䓬啉衍生物的钙盐： （其中，R1代表较低的烷基，R2代表苯基或环己基，Y代表单键或较低的烷基烯基）；一种制备这些盐的方法；以及含有它们作为活性成分的药物。 这些化合物表现出对胃酸分泌的强效抑制活性，以及对胃泌素和/或CCK-B受体的强效拮抗作用。
• [EN] 4-SUBSTITUTED BENZIMIDAZOLES AND THEIR USE AS INHIBITORS OF GASTRIC SECRETION<br/>[FR] BENZIMIDAZOLES SUBSTITUES EN POSITION 4 ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA SECRETION GASTRIQUE
  申请人：ALTANA PHARMA AG

  公开号：WO2004054984A1

  公开（公告）日：2004-07-01

  The invention relates to 6-substituted benzimidazoles of formula 1, in which X is O (oxygen) or NH and Y has either the meaning -CH2-Ar wherein Ar is a mono- or bicyclic aromatic residue, or Y denotes the group gp, formula (gp) wherein Z has the meaning -CHR8- or -CHR8-CHR9-. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.

  这项发明涉及式1中的6-取代苯并咪唑，其中X为O（氧）或NH，Y具有以下含义之一：-CH2-Ar，其中Ar是单环或双环芳香基团；或Y表示群gp，式（gp），其中Z具有含义-CHR8-或-CHR8-CHR9-。这些化合物具有抑制胃酸分泌和优异的胃肠保护作用特性。
• Mixtures of drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same
  申请人：——

  公开号：US20030228275A1

  公开（公告）日：2003-12-11

  A non-polydispersed mixture of conjugates in which each conjugate in the mixture comprises a drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may result in less inter-subject variability than polydispersed mixtures of similar conjugates.

  披露了一种非多分散混合物，其中混合物中的每个共轭物包括与包含聚乙二醇基团的寡聚物偶联的药物。该混合物可能表现出比类似共轭物的多分散混合物更高的体内活性。该混合物可能比类似共轭物的多分散混合物更有效地在体外模拟肠道消化模型中存活。该混合物可能导致比类似共轭物的多分散混合物更少的受试者间变异性。
• [EN] BENZODIAZEPINE DERIVATIVES AS CCK2/GASTRIN RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS DE BENZODIAZÉPINE À TITRE D'ANTAGONISTES DES RÉCEPTEURS DE CCK2/GASTRINE
  申请人：TRIO MEDICINES LTD

  公开号：WO2016020698A1

  公开（公告）日：2016-02-11

  The invention relates to benzodiazepine derivatives of formula (A) useful as CCK2/gastrin receptor antagonists, their preparation and their use in the treatment or prevention of disorders associated with CCK2/gastrin receptors, disorders caused by or associated with hypergastrinaemia, and gastric acid-related disorders.

  这项发明涉及一种公式（A）的苯二氮卓衍生物，可用作CCK2/胃泌素受体拮抗剂，其制备以及在治疗或预防与CCK2/胃泌素受体相关的疾病、由高胃泌素血症引起或相关的疾病以及胃酸相关疾病中的使用。