{"title":"谷氨酸受体对胰岛素释放和糖尿病神经病变的影响","authors":"Enza Palazzo, Ida Marabese, Federica Ricciardi, Francesca Guida, Livio Luongo, Sabatino Maione","doi":"10.1016/j.pharmthera.2024.108724","DOIUrl":null,"url":null,"abstract":"<div><p>Diabetes causes macrovascular and microvascular complications such as peripheral neuropathy. Glutamate regulates insulin secretion in pancreatic β-cells, and its increased activity in the central nervous system is associated with peripheral neuropathy in animal models of diabetes. One strategy to modulate glutamatergic activity consists in the pharmacological manipulation of metabotropic glutamate receptors (mGluRs), which, compared to the ionotropic receptors, allow for a fine-tuning of neurotransmission that is compatible with therapeutic interventions. mGluRs are a family of eight G-protein coupled receptors classified into three groups (I-III) based on sequence homology, transduction mechanisms, and pharmacology. Activation of group II and III or inhibition of group I represents a strategy to counteract the glutamatergic hyperactivity associated with diabetic neuropathy. In this review article, we will discuss the role of glutamate receptors in the release of insulin and the development/treatment of diabetic neuropathy, with particular emphasis on their manipulation to prevent the glutamatergic hyperactivity associated with diabetic neuropathy.</p></div>","PeriodicalId":402,"journal":{"name":"Pharmacology & Therapeutics","volume":"263 ","pages":"Article 108724"},"PeriodicalIF":12.0000,"publicationDate":"2024-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S016372582400144X/pdfft?md5=240c691a52afc25d35d265a343409431&pid=1-s2.0-S016372582400144X-main.pdf","citationCount":"0","resultStr":"{\"title\":\"The influence of glutamate receptors on insulin release and diabetic neuropathy\",\"authors\":\"Enza Palazzo, Ida Marabese, Federica Ricciardi, Francesca Guida, Livio Luongo, Sabatino Maione\",\"doi\":\"10.1016/j.pharmthera.2024.108724\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Diabetes causes macrovascular and microvascular complications such as peripheral neuropathy. Glutamate regulates insulin secretion in pancreatic β-cells, and its increased activity in the central nervous system is associated with peripheral neuropathy in animal models of diabetes. One strategy to modulate glutamatergic activity consists in the pharmacological manipulation of metabotropic glutamate receptors (mGluRs), which, compared to the ionotropic receptors, allow for a fine-tuning of neurotransmission that is compatible with therapeutic interventions. mGluRs are a family of eight G-protein coupled receptors classified into three groups (I-III) based on sequence homology, transduction mechanisms, and pharmacology. Activation of group II and III or inhibition of group I represents a strategy to counteract the glutamatergic hyperactivity associated with diabetic neuropathy. In this review article, we will discuss the role of glutamate receptors in the release of insulin and the development/treatment of diabetic neuropathy, with particular emphasis on their manipulation to prevent the glutamatergic hyperactivity associated with diabetic neuropathy.</p></div>\",\"PeriodicalId\":402,\"journal\":{\"name\":\"Pharmacology & Therapeutics\",\"volume\":\"263 \",\"pages\":\"Article 108724\"},\"PeriodicalIF\":12.0000,\"publicationDate\":\"2024-09-18\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.sciencedirect.com/science/article/pii/S016372582400144X/pdfft?md5=240c691a52afc25d35d265a343409431&pid=1-s2.0-S016372582400144X-main.pdf\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmacology & Therapeutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S016372582400144X\",\"RegionNum\":1,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmacology & Therapeutics","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S016372582400144X","RegionNum":1,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
摘要
糖尿病会引起大血管和微血管并发症,如周围神经病变。谷氨酸可调节胰岛β细胞的胰岛素分泌,其在中枢神经系统中的活性增加与糖尿病动物模型中的周围神经病变有关。调节谷氨酸能活动的一种策略是对代谢型谷氨酸受体(mGluRs)进行药理学操作,与离子型受体相比,mGluRs 可对神经传递进行微调,从而与治疗干预措施相兼容。激活 II 组和 III 组或抑制 I 组是对抗与糖尿病神经病变相关的谷氨酸能亢进的一种策略。在这篇综述文章中,我们将讨论谷氨酸受体在胰岛素释放和糖尿病神经病变的发生/治疗中的作用,特别强调操纵谷氨酸受体以防止与糖尿病神经病变相关的谷氨酸能亢进。
The influence of glutamate receptors on insulin release and diabetic neuropathy
Diabetes causes macrovascular and microvascular complications such as peripheral neuropathy. Glutamate regulates insulin secretion in pancreatic β-cells, and its increased activity in the central nervous system is associated with peripheral neuropathy in animal models of diabetes. One strategy to modulate glutamatergic activity consists in the pharmacological manipulation of metabotropic glutamate receptors (mGluRs), which, compared to the ionotropic receptors, allow for a fine-tuning of neurotransmission that is compatible with therapeutic interventions. mGluRs are a family of eight G-protein coupled receptors classified into three groups (I-III) based on sequence homology, transduction mechanisms, and pharmacology. Activation of group II and III or inhibition of group I represents a strategy to counteract the glutamatergic hyperactivity associated with diabetic neuropathy. In this review article, we will discuss the role of glutamate receptors in the release of insulin and the development/treatment of diabetic neuropathy, with particular emphasis on their manipulation to prevent the glutamatergic hyperactivity associated with diabetic neuropathy.
期刊介绍:
Pharmacology & Therapeutics, in its 20th year, delivers lucid, critical, and authoritative reviews on current pharmacological topics.Articles, commissioned by the editor, follow specific author instructions.This journal maintains its scientific excellence and ranks among the top 10 most cited journals in pharmacology.