A pharmaceutical preparation comprising an angiotension II2 type receptor agonist, and use thereof

An angiotensin and receptor agonist technology, applied to pharmaceutical preparations containing angiotensin II type 2 receptor agonists and its application fields, can solve unstable blood pressure regulation, increase allergic performance and upper airway stimulation Hazardousness, accumulation, etc.

Inactive Publication Date: 2001-04-11
法玛克有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] However, the use of ACE inhibitors in the treatment of intestinal diseases is hampered by the fact that they are nonspecific enzyme inhibitors that lead to the accumulation of several vasoa...

Method used

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  • A pharmaceutical preparation comprising an angiotension II2 type receptor agonist, and use thereof
  • A pharmaceutical preparation comprising an angiotension II2 type receptor agonist, and use thereof
  • A pharmaceutical preparation comprising an angiotension II2 type receptor agonist, and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] In this in vivo example, the peptide purchased from SIGMA, the angiotensin II type 2 receptor agonist p-aminophenylalanine 6 - Angiotensin II (Product No. A1811). The agonist was administered intravenously to rats anesthetized with chloralose, prepared for the in situ measurement of base secretion in the duodenal mucosa (Flemstrom et al. in Am. J. Physiol. ) 1982, 243: the method described in G348). As a result, it was found that increasing the infusion rate of the compound significantly stimulated mucosal base secretion in a dose-dependent manner, as shown in the table below.

[0032] To further exemplify the receptor specificity of this agonist, it was also administered in the presence of a specific angiotensin II type 2 receptor antagonist (PD123319, 200 μg / kg iv), with positive effects on systemic parameters such as mean Arterial blood pressure did not have any significant side effects. The alkali secretion of the mucous membrane is counteracted. This is also il...

Embodiment 2

[0036] In this in vivo example, use is purchased from NEOSYSTEM S. A. , a peptide from France, the selective angiotensin II type 2 receptor agonist CGP 42112A (N-α-nicotinoyl-Tyr-(N-α-CZB-Arg)Lys-His-Pro-Ile-OH)( Product No. SC431). The agonist was administered intravenously as described in Example 1 to chloralose-anesthetized rats prepared for in situ measurement of base secretion in the duodenal mucosa.

[0037] As a result, it was found that, as shown in Table 2 below, a single dose of CGP 42112A (0.1 µg / kg x min) increased duodenal mucosal bicarbonate secretion. As shown in the table below, co-administration with the specific angiotensin II type 1 receptor antagonist losartan (10 mg / kg iv) had no effect on the stimulation response.

[0038] To further illustrate the receptor specificity of this agonist, CGP 42112A was also administered together with the specific angiotensin II type 2 receptor antagonist PD123319 (200 [mu]g / kg iv). The alkali secretion of the duodenal m...

Embodiment 3

[0041] In this in vivo example, angiotensin II, the endogenous ligand for the angiotensin II receptor, purchased from SIGMA, was used. The agonist was administered intravenously as described in Example 1 to rats anesthetized with chloralose prepared for in situ assays.

[0042] As a result, it was found that, as shown in Table 3 below, the administration of angiotensin II alone could not increase the base secretion of the duodenal mucosa.

[0043] Following pretreatment with the specific angiotensin II type 1 receptor antagonist losartan (10 mg / kg iv), infusion of angiotensin II stimulated base secretion in the duodenal mucosa as described in the table below.

[0044] Co-administration with the specific angiotensin II type 2 receptor antagonist PD123319 (200 μg / kg intravenously) effectively counteracted this stimulatory response as described in the table below.

[0045] Agonist dose

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PUM

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Abstract

A pharmaceutical preparation comprising an angiotensin II type 2 receptor agonist, which can be either a peptide or a peptide mimetic, said preparation being useful for treatment and prophylaxis of disorders of the alimentary tract, such as dyspepsia, irritable bowel syndrome and multiple organ failure. Use of an angiotensin II type 2 receptor agonist for the manufacture of a medicament for treatment and/or prophylaxis of disorder of the alimentary tract, such as dyspepsia, irritable bowel syndrome and multiple organ failure. A method for treatment and/or prevention of a condition selected from the group consisting of disorders of the alimentary tract, such as dyspepsia, irritable bowel syndrome and multiple organ failure in a patient, wherein an effective amount of an angiotensin II type 2 receptor agonist is administered to the patient.

Description

technical field [0001] The present invention relates to pharmaceutical formulations containing angiotensin II type 2 receptor agonists, and methods for the prevention and treatment of digestive tract disorders such as dyspepsia, irritable bowel syndrome and multiple organ failure. Background technique [0002] Gastrointestinal dysfunction is a very common disorder characterized by the absence of symptoms of organic diseases such as peptic ulcer and ulcerative colitis. This symptom characteristic may be due to an organic disease such as peptic ulcer disease, or more generally, the symptom may not have any known origin, that is, an organic disease in the bowel that is not proven by various diagnostic methods. Pathological changes. In clinical practice, this syndrome of symptoms is usually divided into 2 categories: "dyspepsia" ("non-ulcer dyspepsia", "functional dyspepsia", "nonorganic dyspepsia") or "irritable bowel Syndrome", which is divided according to whether the sympt...

Claims

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Application Information

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IPC IPC(8): A61K38/00A61K45/00A61K38/08A61K45/06A61P1/00A61P43/00
CPCA61K38/085A61K38/08A61P1/00A61P1/04A61P43/00
Inventor L·芬德里克斯A·彼得松A·哈尔贝里
Owner 法玛克有限公司
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