Ifenprodil Tartrate

脑卒中（中风）是严重威胁人类生命健康的重大疾病，其高致残率与高死亡率给社会和家庭带来沉重负担。当前针对缺血性卒中的一线治疗手段，如重组组织型纤溶酶原激活剂静脉溶栓，受限于严格的时间窗（通常为发病后4.5小时内）及潜在的颅内出血风险，临床获益人群有限。与此同时，创新药物研发周期漫长、投入巨大，使得“老药新用”策略成为卒中治疗领域极具吸引力的替代路径。在此背景下，如何系统性地从基因层面发掘可靠的治疗靶点，并快速筛选出能作用于该靶点的已有药物，是卒中转化医学研究亟需解决的关键科学问题。 2026年6月，由首都医科大学基础医学院与航天中心医院神经内科联合团队在《Journal of the American Heart Association》上发表了题为“Systematic Identification of Therapeutic Targets and Repurposed Drugs for Stroke: From Genome Causal Analysis to Multilevel Validation”的研究论文。该研究整合了大规模人群的多组学数据，系统评估了5859个可成药基因的表达调控与卒中风险之间的因果关系。研究成功锁定GGCX基因作为极具潜力的治疗靶点，并通过细胞与动物模型验证了该靶点的神经保护功能。在此基础上，研究进一步筛选出已上市药物Ifenprodil，并在多个临床前模型中证实了其通过上调GGCX表达发挥抗缺血损伤效应的可行性。该成果为缺血性卒中的靶向治疗提供了高质量的遗传学证据和候选药物方案。 迈维代谢为本研究提供了Ultra-Fast定量蛋白组检测服务。 本研究采用“遗传筛查→功能验证→机制解析→药物筛选”的递进式策略。首先，整合脑组织和血液的eQTL数据，以孟德尔随机化评估5859个可成药基因表达与卒中的因果关联，并通过共定位与全表型分析锁定GGCX并筛查潜在副作用。其次，在缺血卒中模型中验证GGCX表达改变及过表达的保护效应，并运用蛋白质组学解析其调控的通路网络。最后，通过分子对接筛选靶向GGCX的已有药物，在体内外模型中验证候选药物疗效及其与靶点的作用关系。 1. GGCX基因表达水平与卒中风险之间存在因果关联，其高表达具有保护作用孟德尔随机化分析结果显示，无论是脑组织还是血液中，由遗传因素决定的GGCX基因表达水平越高，个体发生卒中的风险就越低。这一保护效应在缺血性卒中中尤为明确。共定位分析进一步确认，影响GGCX表达与影响卒中风险的遗传变异来自同一来源，而非偶然的统计关联。Steiger方向性检验确认了GGCX表达到卒中风险的单向因果关系。该遗传学证据确立了GGCX作为卒中保护性靶点的因果基础。 ■ ■ ■ ■ ■ 图1. 脑组织（PsychENCODE、GTEx）与外周血（eQTLGen、GTEx）中候选基因表达水平与卒中及缺血性卒中风险的孟德尔随机化估计值 2. 缺血性卒中模型中GGCX表达呈病理性下调，过表达GGCX通过调控蛋白稳态与炎症代谢通路发挥神经保护效应 在卒中患者的血液、缺氧复氧处理的神经元以及缺血再灌注小鼠的脑组织中，GGCX的表达均出现显著下降，说明缺血本身就是导致该基因下调的原因。为阐明GGCX的保护机制，研究者在细胞模型中过表达该基因，对正常对照、氧糖剥夺/复氧及GGCX过表达三组细胞进行了蛋白质组学检测，并鉴定出3419个差异表达蛋白。聚类分析与通路富集显示，GGCX过表达所上调的蛋白显著富集于蛋白质稳态维持、代谢修复等通路，下调的蛋白则富集于炎症反应相关通路。该结果揭示了GGCX的保护功能远超越其经典的凝血辅助作用，而是通过系统性地重塑多条细胞存活通路来抵抗缺血损伤。 ■ ■ ■ ■ ■ 图2. GGCX在不同缺血性卒中模型中的表达下调及过表达的保护效应 ■ ■ ■ ■ ■ 图3. GGCX过表达后蛋白稳态、炎症和代谢等相关通路的系统性变化 3. 已上市药物Ifenprodil通过恢复GGCX表达在动物和细胞模型中均显示出治疗潜力 研究通过分子对接筛选出能与GGCX蛋白结合的已有药物，并重点验证了Ifenprodil的疗效。在缺血再灌注小鼠模型中，该药物能显著缩小脑梗死范围、改善运动协调能力和空间记忆功能。在细胞模型中，Ifenprodil同样能提高缺氧复氧后神经元的存活率。机制上，该药物能逆转缺血导致的GGCX表达下降，将其恢复至正常水平。当细胞已预先过表达GGCX后，药物不再产生额外效果，提示Ifenprodil正是通过GGCX通路发挥作用。该结果证实靶向GGCX的药物重定位策略可行，且Ifenprodil作为已上市药物，安全性已知，具备快速进入临床验证的优势。 ■ ■ ■ ■ ■ 图4. Ifenprodil的临床前药效学数据 4. GGCX上调策略在展现治疗潜力的同时，其心血管系统安全性需在后续研究中审慎评估 全表型遗传分析对GGCX可能影响的各类疾病进行了系统性筛查。结果显示，遗传性升高GGCX表达除了与卒中风险降低相关外，还与部分心血管疾病的风险升高存在一定关联。GGCX的已知功能包括参与肝脏中凝血因子的活化，因此系统性增强其活性理论上可能打破凝血-抗凝平衡。这一发现并不否定GGCX作为卒中靶点的价值，但提示未来的干预策略需要设计得更为精准，例如通过局部给药或靶向中枢的方式，避免对外周凝血系统产生不必要的干扰，在疗效和安全性之间取得最佳平衡。 ■ ■ ■ ■ ■ 图5. GGCX、ALDH16A1和SLC33A1的全表型孟德尔随机化分析结果 本研究通过遗传学因果推断、蛋白质组学机制解析及多模型药效验证的整合策略，确立了GGCX基因作为缺血性卒中治疗靶点的科学基础。遗传分析表明该基因高表达与卒中风险降低存在因果关联；蛋白质组学揭示其过表达通过协调蛋白稳态、炎症抑制和代谢修复等多条通路发挥保护效应；药物筛选证实Ifenprodil可通过恢复缺血所致的GGCX下调，在体内外模型中显著减轻脑损伤并改善神经功能。该研究为卒中治疗提供了一个兼具遗传学证据与机制理解的新靶点，并为Ifenprodil的临床转化开辟了新适应症。 迈维蛋白队列研究3大技术优势： 测得稳：自动化前处理+全流程质控标准+规范操作体系，保障大样本队列从采集到产出的长期稳定性与可重复性。 批间比较：自研AI算法结合高质量质控策略，有效降低跨平台、跨批次、跨中心的系统误差，实现跨平台跨中心数据比较。 测的多：整合Astral、SomaSeq、Olink三大平台及超60台质谱仪，实现从高通量筛选到高灵敏度靶向验证的完整能力，支撑队列样本的深度覆盖与多维度解析。 文章含有部分AI生成内容，如有错漏/侵权，请联系作者删除。

NOT FOR DISTRIBUTION TO U.S. NEWSWIRE SERVICES OR FOR DISSEMINATION IN THE UNITED STATES VANCOUVER, British Columbia, May 25, 2026 (GLOBE NEWSWIRE) -- Grey Matters Health Inc. (the “Company” or “Grey Matters”) (CSE: GREY) (FRANKFURT: AGW0) (OTCQB: AGNPF), a Canadian healthcare company, is pleased to announce that it has amended the warrant terms of its recently announced non-brokered private placement, removing the acceleration feature and extending the warrant exercise period to 3 years. All other terms remain unchanged. Summary of Amended Offering Terms The Company recently announced a non-brokered private placement for gross proceeds of CAD $1,000,000 of units at an issue price of CAD $0.40 per Unit. Each Unit will consist of one Class A common share in the capital of the Company (a “Common Share”) and one Common Share purchase warrant (a “Warrant”). Each Warrant will entitle the holder to acquire one Common Share (a “Warrant Share”) at an exercise price of CAD $0.60 (the “Exercise Price”) per Warrant Share for a period of 36 months from the issuance date (the “Expiry Date”). The Company will use the proceeds of the Offering to advance its Alzheimer’s Disease program towards the opening of its first U.S. brain-specific neuroimaging clinic, general and administrative expenses, and for working capital purposes. The securities issued and issuable, described in this news release, will be subject to a statutory hold period of four months plus a day from the date of issuance in accordance with applicable Canadian securities legislation. The securities have not been and will not be registered under the United States Securities Act of 1933, as amended (the “U.S. Securities Act”), or any state securities laws, and may not be offered or sold within the United States or to, or for the account or benefit of, “U.S. persons” (as such term is defined in Regulation S under the U.S. Securities Act) absent registration under the U.S. Securities Act and applicable state securities laws, or an exemption from such registration. Christopher J. Moreau CEO Grey Matters Health Inc. 604.398.4175 Ext 701 cjmoreau@greymatters-health.com info@greymatters-health.com www.greymatters-health.com About Grey Matters Grey Matters is a Canadian healthcare company focused on the provision of brain specific PET scanning services through a planned network of new neuroimaging clinics in the U.S. for the early-stage detection of Alzheimer’s Disease, and other forms of dementia, as well as epilepsy, neuro-oncology, and movement disorders including Parkinson’s disease. Grey Matters has a program for Repirinast, a repurposed drug for CKD, and is also the parent company of Algernon NeuroScience, a wholly owned subsidiary, that has been advancing a psychedelic program investigating a proprietary form of DMT for stroke and traumatic brain injury recovery. The Company’s chronic cough drug Ifenprodil, which works by stopping cough in the brain, was sold for USD $2M cash and a 20% equity position in Seyltx, a private U.S. based drug development company that continues to advance research on the drug. Neither the Canadian Securities Exchange nor its Market Regulator (as that term is defined in the policies of the CSE) accepts responsibility for the adequacy or accuracy of this release. CAUTIONARY DISCLAIMER STATEMENT: This news release contains forward-looking statements that are not historical facts. Forward-looking statements are often identified by terms such as “will”, “may”, “should”, “anticipate”, “expects” and similar expressions. All statements other than statements of historical fact, included in this release are forward-looking statements that involve risks and uncertainties. There can be no assurance that such statements will prove to be accurate and actual results and future events could differ materially from those anticipated in such statements. Important factors that could cause actual results to differ materially from the Company’s expectations include the failure to satisfy the conditions of the relevant securities exchange(s) and other risks detailed from time to time in the filings made by the Company with securities regulations. The reader is cautioned that assumptions used in the preparation of any forward-looking information may prove to be incorrect. Events or circumstances may cause actual results to differ materially from those predicted, as a result of numerous known and unknown risks, uncertainties, and other factors, many of which are beyond the control of the Company. The reader is cautioned not to place undue reliance on any forward-looking information. Such information, although considered reasonable by management at the time of preparation, may prove to be incorrect and actual results may differ materially from those anticipated. Forward-looking statements contained in this news release are expressly qualified by this cautionary statement. The forward-looking statements contained in this news release are made as of the date of this news release and the Company will update or revise publicly any of the included forward-looking statements as expressly required by applicable law.