Novel medicinal application of CB2 receptor stimulant

Abstract

The invention relates to the technical field of novel medicinal application, and particularly relates to novel medicinal application of a CB2 receptor stimulant. An endocannabinoid signal system can be used for maintaining the energy balance and glucose homeostasis in a body; when fat and skeletal muscle cells are subjected to glucose deprivation, the messenger-ribonucleic acid (RNA) expression profile of the signal system changes, and ECS has the effects of mediating insulin resistance and regulating diabetes mellitus, obesity and other metabolic diseases. Animal tests of SER 601 in the CB2 receptor stimulant prove that the CB2 receptor stimulant has a remarkable effect for improving pancreas islet function, improving insulin sensitivity and improving accumulation of whole body fat, especially abdominal fat. The CB2 receptor stimulant can be used for reducing the content of fat in a body while improving the insulin sensitivity, preventing / treating diabetes mellitus patients, especially patients with type 2 diabetes mellitus, and preventing / treating obesity, lipodystrophy, weight and fat reduction and other diseases.

Description

technical field [0001] The invention belongs to the technical field of new uses of medicines, and in particular relates to a new medicines use of a cannabinoid CB2 receptor agonist SER601. Background technique [0002] Cannabinoids (English: Cannabinoids), also known as anandamide, are found in Indian hemp (Cannabissativa) and naturally exist in the nervous and immune systems of animals. The extension of cannabinoids includes a group of substances that are structurally related to THC or bind to cannabinoid receptors. The endogenous cannabinoid signaling system (ECS) consists of cannabinoid receptors, its endogenous ligands, also known as endogenous cannabinoids, and lipase responsible for the metabolism of endogenous cannabinoids. Intracellular and cell-to-cell signal transduction. [0003] The three known cannabinoid receptors belong to the Gprotein-coupled receptors (GPCRs) superfamily, which are called cannabinoid1 (CB1) receptor, cannabinoid2 (CB2) receptor and atypica...

AI Technical Summary

Problems solved by technology

The hypoglycemic mechanism of sulfonylureas is mainly to stimulate insulin secretion, which only works on patients with certain islet functions; the main mechanism of biguanides to hypoglycemic is to increase the utilization of glucose by peripheral tissues and increase the anaerobic glycolysis of glucose. Reduce the absorption of glucose in the gastrointestinal tract and reduce weight; such as metformin (metformin), although it can improve the body's sensitivity to insulin, but its effect in reducing fat is not good, and there are certain side effects, and it does not have the ability to stimulate insulin at the same time secrete, increase insulin sensitivity, and reduce fat; Chinese patent CN103550219A discloses "Treatment of Diabetes in Patients Not Suitable for Metformin Treatment", which discloses the disadvantages of metformin drugs: Metformin treatment is accompanied by side effects, such as: gastrointestinal Symptoms or (sometimes) serious side effects, lactic acidosis (which can be fatal), recognized risk factors are reduced renal function

In addition, metformin is largely eliminated by the kidneys through glomerular filtration and tubular secretion without change, so it is contraindicated in patients with renal disease or renal impairment, and is not suitable for those who are intolerant or contraindicated to metformin

Long-term use of the above-mentioned drugs will lead to obesity, and easily induce the risks of cardiovascular disease and heart failure, especially for patients with type Ⅱ diabetes who develop insulin resistance, the above-mentioned traditional drugs have no therapeutic effect

[0007] In view of the close relationship between obesity and type 2 diabetes, the existing drugs used to treat diabetes cannot simultaneously improve the body's sensitivity to insulin and reduce body fat. Drugs for body fat bring good news to the majority of patients with type 2 diabetes

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