This is a working overview of glucagon receptor, written for readers who want more than a one-paragraph summary but less than a textbook.
This page was last updated on 2025-09-24 and is reviewed periodically as new material appears.
瑞他鲁肽是一种在研合成肽，同时作用于胰高血糖素样肽-1、葡萄糖依赖性促胰岛素多肽和胰高血糖素受体。该分子属于多受体激动剂类别，尚未获得任何监管机构的上市批准。当前临床开发主要针对肥胖和2型糖尿病，研究代号为LY3437943。已确立的信息包括受体靶点和部分中期试验结果；最终疗效、长期安全性和适用人群仍属开放问题。
开发进程从早期单次和多次给药研究推进至大规模后期试验。公开报告显示，参与者在体重和相关代谢指标上出现变化，但完整数据需经同行评审并接受独立复核。试验设计通常包括随机、双盲和对照设置，以区分药物效应与行为干预。监管提交和标签范围尚未确定；长期维持效果与心血管结局仍是开放问题。
与仅靶向单一受体的同类药物相比，瑞他鲁肽增加胰高血糖素受体成分，理论上可提高能量消耗并改变脂肪分布。临床中观察到的体重变化是否主要来自该额外机制，目前尚无定论。胃肠道反应是该类药物常见不良事件，试验中通过剂量递增和监测进行管理。停药后体重反弹、个体差异和长期耐受性仍需更多数据。
Pharmacologically, retatrutide acts as a triple agonist at the glucagon-like peptide-1 receptor, the glucose-dependent insulinotropic polypeptide receptor, and the glucagon receptor. Activation of the first two receptors is associated with improved insulin secretion and reduced appetite. The glucagon receptor component is thought to increase energy expenditure, a mechanism that distinguishes this molecule from dual-agonist compounds. Researchers continue to investigate how the three activities interact and whether the combined profile offers advantages that justify additional clinical testing.
Several questions about the compound remain unresolved. The durability of weight reduction after treatment stops, the frequency of gastrointestinal side effects, and the long-term cardiovascular profile are topics of ongoing study. Regulatory submissions and phase 3 trial outcomes have not been fully reported in the public literature. Because most available data come from controlled trials rather than general-population use, conclusions about effectiveness outside study settings are provisional. The distinction between established findings and open questions matters when interpreting early coverage of the drug.
Retatrutide is an investigational peptide developed by a pharmaceutical company as a multi-receptor agonist for treating obesity and type 2 diabetes. The compound emerged from research into gut-hormone analogues that act on several receptors simultaneously rather than on a single target. Early preclinical work examined how combined activity at three distinct receptors might produce greater metabolic effects than single-receptor compounds. Published phase 2 results have described substantial reductions in body weight among participants, although the compound remains unapproved in most jurisdictions as of the mid-2020s.
| Property | Value | Notes |
|---|---|---|
| 研究代号 | LY3437943 | 文献中常用的实验标识 |
| 药物类别 | 三重受体激动剂 | 靶向GLP-1、GIP与胰高血糖素受体 |
| 开发状态 | 后期临床研究 | 尚未获批上市 |
| 主要研究人群 | 肥胖与2型糖尿病 | 入组条件依试验方案而定 |
| 常见同义词 | 瑞他鲁肽；LY3437943 | 名称拼写可能因语言和出版物而异 |
Development has progressed through early- and mid-stage human studies in adults with obesity and with type 2 diabetes. Published phase 2 data reported reductions in body weight and improvements in glycemic markers over the treatment period. No regulatory agency has approved the compound for any indication, and it remains available only within controlled research settings. Whether benefits observed in trials translate into durable outcomes after treatment stops is not yet established.
Retatrutide is an investigational synthetic peptide that acts as an agonist at three distinct G protein-coupled receptors. It combines activity at the glucagon-like peptide-1 receptor, the glucose-dependent insulinotropic polypeptide receptor, and the glucagon receptor within a single molecule. This multi-receptor profile distinguishes it from earlier incretin-based compounds that engage one or two of these pathways. Researchers designed the molecule to test whether simultaneous activation produces greater metabolic effects than single or dual agonism alone.
The peptide backbone is chemically modified to resist rapid enzymatic breakdown in the body. A fatty acid side chain promotes binding to serum albumin, which slows renal clearance and supports an extended circulation time. These modifications allow less frequent administration than would be possible with an unmodified peptide. The precise contribution of glucagon receptor activation to the overall metabolic effect remains an area of active investigation, because glucagon raises glucose while also increasing energy expenditure.
Retatrutide is an investigational peptide studied for obesity and type 2 diabetes. It is a single synthetic molecule designed to activate three metabolic receptors simultaneously. The compound belongs to the incretin mimetic family, a group of peptides that imitate gut hormones involved in appetite and glucose control. Its research code is LY3437943, and it remains under clinical study rather than cleared for routine medical use.
Acting as a triple agonist, the molecule binds the GLP-1, GIP, and glucagon receptors. GLP-1 activity slows gastric emptying and dampens appetite, while GIP signaling contributes to insulin sensitivity and fat metabolism. Glucagon receptor engagement raises energy expenditure and encourages fat breakdown, although it can also elevate blood glucose. Combining three pathways is intended to yield larger weight reduction than single or dual agonists, and researchers continue to examine how the balance among them shapes tolerability.
==== Canada ==== As of 11 April 2020, access in Canada was available only through clinical trials. Health Canada approved requests to treat twelve people with remdesivir under the department's special-access program (SAP). Additional doses of remdesivir are not available through the SAP except for pregnant women or children with confirmed COVID‑19 and severe illness. In June 2020, Health Canada received an application from Gilead for the use of remdesivir for treating COVID‑19. On 27 July 2020, Health Canada conditionally approved the application. In September 2020, Minister of Public Services and Procurement Anita Anand announced that Canada had entered into a deal to obtain up to 150,000 vials of remdesivir from Gilead starting in October. As of 8 October, remdesivir was still not widely available in Alberta, because Alberta Health Services was undertaking a "formulary review" to be completed by mid-November.
Genotypic AMR characterisation methods are, however, being increasingly used in combination with machine learning algorithms in research to help better predict phenotypic AMR from organism genotype. Optical techniques such as phase contrast microscopy in combination with single-cell analysis are another powerful method to monitor bacterial growth. In 2017, scientists from Uppsala University in Sweden published a method that applies principles of microfluidics and cell tracking, to monitor bacterial response to antibiotics in less than 30 minutes overall manipulation time. This invention was awarded the 8M£ Longitude Prize on AMR in 2024. Recently, this platform has been advanced by coupling microfluidic chip with optical tweezing to isolate bacteria with altered phenotype directly from the analytical matrix. Rapid diagnostic methods have also been trialled as antimicrobial stewardship interventions to influence the healthcare drivers of AMR. Serum procalcitonin measurement has been shown to reduce mortality rate, antimicrobial consumption and antimicrobial-related side-effects in patients with respiratory infections, but impact on AMR has not yet been demonstrated. Similarly, point of care serum testing of the inflammatory biomarker C-reactive protein has been shown to influence antimicrobial prescribing rates in this patient cohort, but further research is required to demonstrate an effect on rates of AMR. Clinical investigation to rule out bacterial infections are often done for patients with pediatric acute respiratory infections.
=== Cyst stage === To endure harsh environmental conditions, trophozoites transform into microbial cysts, spherical, single-layered structures about 7–15 μm in diameter, enclosing a single cell nucleus. Acting as a resilient capsule, the cyst enables the amoeba to withstand adverse circumstances. Factors triggering cyst formation include food scarcity, overcrowding, desiccation, waste accumulation, and cold temperatures. When conditions improve, the amoeba can emerge through the pore or ostiole at the center of the cyst. N. fowleri has been observed to encyst at temperatures below 10 °C (50 °F).
==== Anticancer properties ==== Some cecropins (e.g. cecropin A, and cecropin B) have anticancer properties and are called anticancer peptides (ACPs). Hybrid ACPs based on Cecropin A have been studied for anticancer properties. The fruit fly Defensin prevents tumour growth, suspected to bind to tumour cells owing to cell membrane modifications common to most cancer cells, such as phosphatidylserine exposure.
Sources: en.wikipedia.org
=== Antibiotics created from 6-APA === There are three major groups of other semi-synthetic antibiotics related to the penicillins. They are synthesised by adding various side-chains to the precursor 6-APA, which is isolated from penicillin G. These are the antistaphylococcal antibiotics, broad-spectrum antibiotics and antipseudomonal antibiotics.
According to the contract, the RDIF as a seller is not liable for any adverse events following administering of the vaccine, nor its effectiveness. According to the Slovak lawyers, the contract is explicitly disadvantageous for Slovakia. On 8 May 2021, the Russian Direct Investment Fund sent a letter to the Denník N newspaper requesting the removal of the statements of the drug regulator, calling them "unsubstantiated and false" and "fake news". RDIF threatened the newspaper with legal action if they didn't comply with the demand by 9 May. The newspaper's editors refused. After the samples were sent to the EU-certified laboratory in Hungary and it was stated that "the results were satisfactory", the Slovak government approved the vaccine, and announced that vaccination with Sputnik V would begin in June 2021, despite the negative review by Slovakia's drug regulator. Vaccinations started on 7 June, but without significant interest in the Sputnik V vaccine. Slovakia had no plans to order new batches and planned to sell or donate unused vaccines to Balkans countries. The registrations for vaccination were closed on 30 June. In July 2021, 160,000 doses of the vaccine from the first batch of 200,000 were shipped back to Russia. Temporary government approval for Sputnik V expired on 31 August 2021. In total, 18,500 people have been vaccinated. The purchase of Sputnik V, which led to a political crisis and contributed to a fall of Igor Matovič's Cabinet was investigated by Slovak Police Force with the investigation levered against Marek Krajčí.
== Medical Significance == Pathogenic mutations in this gene have been associated with a number of diseases, including Developmental and epileptic encephalopathy 71 (DEE71), CASGID syndrome, and Global developmental delay, progressive ataxia, and elevated glutamine (GDPAG).
Since its founding in 1517 on the orders of François I, Le Havre has continued to grow: today it measures 27 km (17 mi) from east to west, about 5 km (3 mi) from north to south with an area of 10,000 hectares (24,711 acres). The last big project called Port 2000 increased the handling capacity for containers. The port provides 16,000 direct jobs to the Le Havre region, to which must be added indirect jobs in industry and transport. With approximately 3,000 employees in 2006, the activities of distribution and warehousing provide more jobs, followed by road transport (2,420 jobs) and handling (2,319 jobs). In 2011, 715,279 passengers passed through the port of Le Havre and there were 95 visits by cruise ships carrying 185,000 passengers. The port expects 110 cruise ship calls in 2012. Created in 1934, the leisure boat harbour of Le Havre is located to the west and is the largest French boat harbour in the Channel with a capacity of 1,160 moorings. Finally, there is a small fishing port in the Saint-François district and a Hawker centre.
== Discoveries made using egg extracts == Purification of M-phase promoting factor (MPF) Elucidation of the role of synthesis and degradation of cyclin B in cell cycle progression Discovery that degradation of a protein(s) other than cyclin B is necessary for initiating chromosome segregation Discovery of a mechanism of spindle assembly that depends on chromatin, but not centrosomes Proposal of a DNA replication licensing system and identification of its responsible factor Identification of importin α/β responsible for nuclear transport Discovery of the condensin complex essential for mitotic chromosome assembly Identification of the cohesin complex essential for sister chromatid cohesion More recently, the egg extracts have been used to study reprogramming of differentiated nuclei, physical properties of spindles and nuclei, and theoretical understanding of cell cycle control.
Sources: en.wikipedia.org
尚未。它仍处于临床研究阶段，任何监管批准都取决于正在进行的试验结果和提交审评。可公开获取的信息以试验注册和会议摘要为主。
司美格鲁肽主要靶向GLP-1受体，而瑞他鲁肽同时作用于GLP-1、GIP和胰高血糖素受体。这种三重机制旨在产生不同的代谢效应，但临床差异仍需头对头研究确认。
长期心血管结局、停药后维持效果、罕见不良事件和不同人群中的获益风险比尚未完全确定。完整三期数据和监管审评将影响结论。
It is designed as a triple agonist acting on the GLP-1, GIP, and glucagon receptors. This combination is intended to influence appetite, insulin secretion, and energy expenditure. Single-receptor and dual-receptor compounds act on a narrower set of targets.