关键词: PET/CT TRPV1 cancer pain transient receptor potential cation channel subfamily V member 1

Mesh : Humans Capsaicin / metabolism Pain / drug therapy Positron-Emission Tomography TRPV Cation Channels / chemistry genetics metabolism

来  源:   DOI:10.1093/jjco/hyad194

Abstract:
Transient receptor potential cation channel subfamily V member 1 (TRPV1) was identified using capsaicin, a pungent compound that is present in red pepper. The activation of TRPV1 induces an influx of calcium ions into cells and causes excitation of sensory neurons, associating with thermal sensing, sweating and pain. TRPV1 is also identified in various types of cancer cells. The expression of TRPV1 in cancer cells depends on the type of cancer and the stage of the disease. Therefore, TRPV1 has been considered a potential target of medicinal chemistry for drug development, and blocking its activation may lead to cancer therapy and pain relief. However, the details of the pathophysiological function of TRPV1 in vivo are still unclear. To explore practical use of TRPV1, we focused on positron emission tomography imaging and developed a 11C-radiolabeled tracer to visualize TRPV1.
摘要:
使用辣椒素鉴定瞬时受体电位阳离子通道亚家族V成员1(TRPV1),红辣椒中的刺激性化合物。TRPV1的激活诱导钙离子流入细胞并引起感觉神经元的兴奋,与热传感相关,出汗和疼痛。TRPV1也在各种类型的癌细胞中被鉴定。TRPV1在癌细胞中的表达取决于癌症的类型和疾病的阶段。因此,TRPV1已被认为是药物开发的药物化学的潜在目标,阻断其激活可能导致癌症治疗和疼痛缓解。然而,TRPV1在体内的病理生理功能细节尚不清楚.为了探索TRPV1的实际使用,我们专注于正电子发射断层扫描成像,并开发了11C放射性标记的示踪剂来可视化TRPV1。
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