Crotamiton 是一种抗疥疮药，可抑制感觉神经元中组胺和氯喹诱导的瘙痒通路，并减轻小鼠的抓挠,Biomolecules & Therapeutics

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Crotamiton 是一种抗疥疮药，可抑制感觉神经元中组胺和氯喹诱导的瘙痒通路，并减轻小鼠的抓挠
Biomolecules & Therapeutics ( IF 3.0 ) Pub Date : 2020-11-01 , DOI: 10.4062/biomolther.2020.063
Da-Som Choi _{1,

2} , Yeounjung Ji _{1,

2} , Yongwoo Jang ₃ , Wook-Joo Lee _{1,

2} , Won-Sik Shim _{1,

2}

Affiliation

克罗米通是一种抗疥疮药物，但最近发现克罗米通还能抑制小鼠的非疥疮性瘙痒。然而，其潜在机制在很大程度上尚不清楚。因此，本研究的目的是探讨克罗米通对非疥疮性瘙痒的止痒作用机制。组胺和氯喹用作非疥疮性瘙痒剂。在 HEK293T 细胞和原代培养的背根神经节 (DRG) 神经元中，使用荧光细胞内钙测定法确定了克罗米通的作用。进一步的体内效果通过抓挠行为测试进行评估。Crotamiton 强烈抑制 HEK293T 细胞中组胺诱导的钙内流，表达组胺受体 1 (H1R) 和瞬时受体电位香草素 1 (TRPV1)，作为组胺诱导的瘙痒模型。相似地，它还阻止了氯喹诱导的 HEK293T 细胞中的钙内流，表达了 Mas 相关 G 蛋白偶联受体 A3 (MRGPRA3) 和瞬时受体电位 A1 (TRPA1)，作为组胺非依赖性瘙痒的模型。此外，克罗米通还抑制组胺和氯喹诱导的小鼠 DRG 原代培养物中的钙内流。此外，克罗米通强烈抑制组胺和氯喹诱导的小鼠抓挠。总体而言，发现克罗米通通过组胺和氯喹对非疥疮性瘙痒具有止痒作用。因此，克罗米通可用作一般的止痒剂，而与疥疮的存在无关。作为非组胺瘙痒的模型。此外，克罗米通还抑制组胺和氯喹诱导的小鼠 DRG 原代培养物中的钙内流。此外，克罗米通强烈抑制组胺和氯喹诱导的小鼠抓挠。总体而言，发现克罗米通通过组胺和氯喹对非疥疮性瘙痒具有止痒作用。因此，克罗米通可用作一般的止痒剂，而与疥疮的存在无关。作为非组胺瘙痒的模型。此外，克罗米通还抑制组胺和氯喹诱导的小鼠 DRG 原代培养物中的钙内流。此外，克罗米通强烈抑制组胺和氯喹诱导的小鼠抓挠。总体而言，发现克罗米通通过组胺和氯喹对非疥疮性瘙痒具有止痒作用。因此，克罗米通可用作一般的止痒剂，而与疥疮的存在无关。发现克罗米通通过组胺和氯喹对非疥疮性瘙痒具有止痒作用。因此，克罗米通可用作一般的止痒剂，而与疥疮的存在无关。发现克罗米通通过组胺和氯喹对非疥疮性瘙痒具有止痒作用。因此，克罗米通可用作一般的止痒剂，而与疥疮的存在无关。

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Crotamiton, an Anti-Scabies Agent, Suppresses Histamine- and Chloroquine-Induced Itch Pathways in Sensory Neurons and Alleviates Scratching in Mice

Crotamiton is an anti-scabies drug, but it was recently found that crotamiton also suppresses non-scabietic itching in mice. However, the underlying mechanism is largely unclear. Therefore, aim of the study is to investigate mechanisms of the anti-pruritic effect of crotamiton for non-scabietic itching. Histamine and chloroquine are used as non-scabietic pruritogens. The effect of crotamiton was identified using fluorometric intracellular calcium assays in HEK293T cells and primary cultured dorsal root ganglion (DRG) neurons. Further in vivo effect was evaluated by scratching behavior tests. Crotamiton strongly inhibited histamine-induced calcium influx in HEK293T cells, expressing both histamine receptor 1 (H1R) and transient receptor potential vanilloid 1 (TRPV1), as a model of histamine-induced itching. Similarly, it also blocked chloroquine-induced calcium influx in HEK293T cells, expressing both Mas-related G-protein-coupled receptor A3 (MRGPRA3) and transient receptor potential A1 (TRPA1), as a model of histamine-independent itching. Furthermore, crotamiton also suppressed both histamine- and chloroquine-induced calcium influx in primary cultures of mouse DRG. Additionally, crotamiton strongly suppressed histamine- and chloroquine-induced scratching in mice. Overall, it was found that crotamiton has an anti-pruritic effect against non-scabietic itching by histamine and chloroquine. Therefore, crotamiton may be used as a general anti-pruritic agent, irrespective of the presence of scabies.

更新日期：2020-11-01

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