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A Randomised Trial Evaluating the Effects of the TRPV1 Antagonist SB705498 on Pruritus Induced by Histamine and Cowhage Challenge in Healthy Volunteers

机译:评估TRPV1拮抗剂SB705498对组胺诱导的瘙痒的影响以及健康志愿者的母牛皮挑战的随机试验。

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摘要

BackgroundTransient receptor potential vanilloid type 1 (TRPV1) is a non-selective cation channel widely expressed in skin tissues, and peripheral sensory nerve fibres. Activation of TRPV1 releases neuropeptides; the resulting neurogenic inflammation is believed to contribute to the development of pruritus. A TRPV1 antagonist has the potential to perform as an anti-pruritic agent. SB705498 is a TRPV1 antagonist that has demonstrated in vitro activity against cloned TRPV1 human receptors and when orally administered has demonstrated pharmacodynamic activity in animal models and clinical studies.
机译:背景瞬态受体电位类香草素1型(TRPV1)是在皮肤组织和周围感觉神经纤维中广泛表达的非选择性阳离子通道。 TRPV1的激活释放神经肽;据信产生的神经源性炎症有助于瘙痒的发展。 TRPV1拮抗剂具有用作止痒药的潜力。 SB705498是TRPV1拮抗剂,已证明其对克隆的TRPV1人受体具有体外活性,并且在动物模型和临床研究中口服给药时已证明其药效活性。

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