Synthetic derivatives of capsaicin and gingerols as analgesics acting at the vanilloid receptor

辣椒素和姜辣素的合成衍生物作为作用于香草素受体的镇痛剂。本项目旨在制备作用于香草素（VR 1）受体的α-羟基酮和姜辣素衍生物，具有潜在的镇痛活性。将测试这些化合物激活VR 1受体、使受体脱敏和释放与疼痛通路相关的神经肽的能力。这些新型化合物的开发将有助于了解VR 1受体激活的机制，并提供有关VR 1受体如何调节的信息。我们将确定和比较这些化合物的神经毒性辣椒素，这是已知的具有神经毒性活性。该项目的结果可能会导致更好的疼痛管理的有效药物。R\n

Synthetic derivatives of capsaicin and gingerols as analgesics acting at the vanilloid receptor. This project aims to prepare alpha-hydroxyketones and gingerol derivatives acting at vanilloid (VR1) receptor with potential analgesic activity. These compounds will be tested for their ability to activate the VR1 receptor, desensitize the receptor and release neuropeptides associated with pain pathways. The development of these novel compounds will contribute towards understanding the mechanisms of VR1 receptor activation and provide information on how the VR1 receptor is regulated. We will determine and compare neurotoxicity of these compounds to capsaicin which is known to possess neurotoxic activity. The outcome of this project may result in effective agents for better pain management.\r\n