更新于：2024-11-01

κ opioid receptor x TRPA1 x TRPM8

更新于：2024-11-01

基本信息

关联

项与 κ opioid receptor x TRPA1 x TRPM8 相关的药物

Ibuprofen/Levomenthol

布洛芬/左旋薄荷醇

靶点

COX x TRPA1 x TRPM8 x κ opioid receptor

作用机制

COX抑制剂 [+3]

在研机构

The Mentholatum Co.

原研机构

The Mentholatum Co.

在研适应症-

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区

英国

首次获批日期1998-08-06

Levomenthol

左旋薄荷醇

靶点

TRPA1 x TRPM8 x κ opioid receptor

作用机制

TRPA1抑制剂 [+2]

在研机构

Fuji Pharma Co., Ltd.

原研机构

University Hospitals Cleveland Medical Center

在研适应症-

非在研适应症

肠道疾病

最高研发阶段批准上市

首次获批国家/地区

日本

首次获批日期1986-01-20

Crotamiton/Lidocaine/Levomenthol/Bifonazole/Glycyrrhetinic Acid

联苯苄唑/克罗米通/利多卡因/甘草次酸/左旋薄荷醇

靶点

11β-HSD1 x CYP51A1 x SCNA x TRPA1 x TRPM8 x fungal CYP51A1 x κ opioid receptor

作用机制

11β-HSD1抑制剂 [+6]

在研机构-

原研机构-

在研适应症

足癣

非在研适应症-

最高研发阶段批准上市

首次获批国家/地区-

首次获批日期1800-01-20

项与 κ opioid receptor x TRPA1 x TRPM8 相关的临床试验

NCT05888597 / Recruiting临床2期

Effect of L-menthol on Breathlessness and Exercise Capacity in Chronic Obstructive Pulmonary Disease: a Randomized

The purpose of this study is to assess the effect of L-menthol on breathlessness in patients with chronic obstructive pulmonary disease (COPD).

开始日期2023-05-24

申办/合作机构

Region Skåne Holding AB

[+1]

RBR-7tgfwmk / Not yet recruitingN/AIIT

Use of L-menthol solution as an esophageal antispasmodic in Upper Digestive Endoscopy: pilot project

开始日期2021-08-01

申办/合作机构-

JPRN-jRCTs031200400 / Completed临床2期IIT

Effects of olfactory stimulation by L-menthol on dyspnea on exertion in chronic lung disease: A pilot study

开始日期2021-04-14

申办/合作机构-

100 项与 κ opioid receptor x TRPA1 x TRPM8 相关的临床结果

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100 项与 κ opioid receptor x TRPA1 x TRPM8 相关的转化医学

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0 项与 κ opioid receptor x TRPA1 x TRPM8 相关的专利（医药）

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项与 κ opioid receptor x TRPA1 x TRPM8 相关的文献（医药）

Frontiers in Molecular Neuroscience

The distinctive role of menthol in pain and analgesia: Mechanisms, practices, and advances

Review

作者: Zhang, Haoyue ; Zhang, Linlin ; Li, Ziping ; Li, Yize ; Wang, Yigang ; Li, Qing

Menthol is an important flavoring additive that triggers a cooling sensation. Under physiological condition, low to moderate concentrations of menthol activate transient receptor potential cation channel subfamily M member 8 (TRPM8) in the primary nociceptors, such as dorsal root ganglion (DRG) and trigeminal ganglion, generating a cooling sensation, whereas menthol at higher concentration could induce cold allodynia, and cold hyperalgesia mediated by TRPM8 sensitization. In addition, the paradoxical irritating properties of high concentrations of menthol is associated with its activation of transient receptor potential cation channel subfamily A member 1 (TRPA1). Under pathological situation, menthol activates TRPM8 to attenuate mechanical allodynia and thermal hyperalgesia following nerve injury or chemical stimuli. Recent reports have recapitulated the requirement of central group II/III metabotropic glutamate receptors (mGluR) with endogenous κ-opioid signaling pathways for menthol analgesia. Additionally, blockage of sodium channels and calcium influx is a determinant step after menthol exposure, suggesting the possibility of menthol for pain management. In this review, we will also discuss and summarize the advances in menthol-related drugs for pathological pain treatment in clinical trials, especially in neuropathic pain, musculoskeletal pain, cancer pain and postoperative pain, with the aim to find the promising therapeutic candidates for the resolution of pain to better manage patients with pain in clinics.