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首页> 外文期刊>The journal of clinical investigation >Retinoids activate the irritant receptor TRPV1 and produce sensory hypersensitivity
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Retinoids activate the irritant receptor TRPV1 and produce sensory hypersensitivity

机译：类维生素A激活刺激性受体TRPV1并产生感觉超敏反应

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Retinoids are structurally related derivatives of vitamin A and are required for normal vision as well as cell proliferation and differentiation. Clinically, retinoids are effective in treating many skin disorders and cancers. Application of retinoids evokes substantial irritating side effects, including pain and inflammation; however, the precise mechanisms accounting for the sensory hypersensitivity are not understood. Here we show that both naturally occurring and synthetic retinoids activate recombinant or native transient receptor potential channel vanilloid subtype 1 (TRPV1), an irritant receptor for capsaicin, the pungent ingredient of chili peppers. In vivo, retinoids produced pain-related behaviors that were either eliminated or significantly reduced by genetic or pharmacological inhibition of TRPV1 function. These findings identify TRPV1 as an ionotropic receptor for retinoids and provide cellular and molecular insights into retinoid-evoked hypersensitivity. These findings also suggest that selective TRPV1 antagonists are potential therapeutic drugs for treating retinoid-induced sensory hypersensitivity.
机译：类视黄醇是维生素A的结构相关衍生物，是正常视力以及细胞增殖和分化所必需的。在临床上，类视黄醇可有效治疗许多皮肤疾病和癌症。使用类维生素A会引起严重的刺激性副作用，包括疼痛和炎症。然而，尚不清楚引起感觉超敏反应的确切机制。在这里，我们显示天然存在的和合成的类维生素A均能激活重组或天然瞬时受体电位通道香草样亚型1（TRPV1），辣椒素的刺激性成分辣椒素的刺激性受体。在体内，类维生素A产生的疼痛相关行为被遗传或药理抑制TRPV1功能消除或明显减轻。这些发现将TRPV1识别为类维生素A的离子受体，并为类维生素A引起的超敏反应提供了细胞和分子方面的见识。这些发现还表明选择性TRPV1拮抗剂是用于治疗类维生素A诱导的感觉超敏反应的潜在治疗药物。

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