左旋薄荷醇(Levomenthol) - 药物靶点：TRPA1 x TRPM8 x κ opioid receptor_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(-)-(1R,3R,4S)-menthol、(-)-Menthol、(1R,3R,4S)-(-)-menthol

+ [12]

靶点

TRPA1 x TRPM8 x κ opioid receptor

作用机制

TRPA1抑制剂(瞬时受体电位离子通道亚基1抑制剂)、TRPM8激动剂(瞬时受体电位离子通道亚科M成员8激动剂)、κ opioid receptor拮抗剂(κ-阿片受体拮抗剂)

治疗领域

消化系统疾病

在研适应症-

非在研适应症

肠道疾病

原研机构

University Hospitals Cleveland Medical Center

在研机构

Fuji Pharma Co., Ltd.

非在研机构

Nihon Pharmaceutical Co., Ltd.

最高研发阶段批准上市

首次获批日期

日本 (1986-01-20)

最高研发阶段(中国)-

特殊审评-

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结构

分子式C10H20O

InChIKeyNOOLISFMXDJSKH-KXUCPTDWSA-N

CAS号2216-51-5

关联

23

项与左旋薄荷醇相关的临床试验

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 项与左旋薄荷醇相关的临床结果

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100 项与左旋薄荷醇相关的转化医学

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100 项与左旋薄荷醇相关的专利（医药）

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377

项与左旋薄荷醇相关的文献（医药）

2025-01-01·Talanta

Natural deep eutectic solvent-based dispersive liquid-liquid microextraction of pesticides in drinking waters combined with GC-MS/MS detection

Article

作者: Hristozova, Аsya ; Canals, Antonio ; Aguirre, Miguel Ángel ; Simitchiev, Kiril ; Vidal, Lorena

The current research aims to develop a new analytical method applying a dispersive liquid-liquid microextraction (DLLME) assisted by vortex and using an environmentally friendly extractant for the preconcentration of organochlorine and organophosphorus pesticides followed by gas chromatography-tandem mass spectrometry (GC-MS/MS) analysis. The extractant (i.e., natural deep eutectic solvent (NADES)) is safe, cheap, biodegradable and can be prepared by simply mixing DL-menthol and decanoic acid (molar ratio 2:1). The main experimental factors affecting the extraction of all analytes evaluated (19 organochlorine and organophosphorus pesticides) have been optimised using a multivariate analysis consisting in two steps: a Plackett-Burman design followed by a central composite design (CCD). Seven experimental factors have been evaluated: (i) sample volume; (ii) NADES volume; (iii) sample pH; (iv) extraction time; (v) centrifugation time; (vi) centrifugation speed; and (vii) ionic strength (NaCl %, w v^-1). For the significant variables, the optimum values were 10 mL sample and 45 μL NADES. No pH adjustment as well as addition of NaCl were needed. The other variables were set at 3 min extraction time, 5 min centrifugation time and 900×g centrifugation speed, respectively. Under the optimised extraction conditions, the limit of quantification (LOQ) values ranged between 0.2 and 78 ng L^-1 for all analysed pesticides. Furthermore, the proposed analytical method has been successfully applied to drinking water (bottled spring water). The recovery study (n = 3) has been evaluated at 0.1, 1.0 and 5.0 μg L^-1 spiking levels, obtaining relative recovery values within the range of 70 % and 117 % and RSD values between 1 % and 20 % for all the analytes studied, except for p,p-DDT (56-77 % in high conductivity water samples).

2024-10-23·Journal of Agricultural and Food Chemistry

Lipase Substrate Anchoring Dynamics Guided the Rational Design of Novel Deep Eutectic Solvents for Glucose Ester Synthesis

Article

作者: Chong, Wenya ; Liu, Yanjiao ; Liang, Chunyi ; Hu, Yi ; Qi, Yuan ; Nian, Binbin ; Zhang, Zihan

Glucose esters, heralded for their emulsifying and solubilizing properties, have found increasing application in food, pharmaceutical, and cosmetic sectors. However, the environmental impact of chemical synthesis and the problem of enzyme inactivation in enzymatic synthesis have hindered their application. To this end, deep eutectic solvents (DESs) with stabilized enzyme activity and better solubility properties are considered a promising solution. In the study, 12 kinds of hydrophilic DESs and 22 kinds of hydrophobic DESs were screened, and we examined their efficiency in the synthesis of glucose esters. The results indicated that d,l-menthol-based DESs have excellent performance, with the highest yield of 92.85%. The molecular dynamics simulations suggested that it can be attributed to DESs changing the size of substrate binding pocket, which in turn affects the substrate anchoring ability and the catalytic efficiency of lipase. To further evaluate the effects of the solvent on the substrate anchoring ability of enzymes, a novel strategy, namely, substrate anchoring index, which is based on the stability of the tetrahedral intermediate, was proposed and used for the designing of more efficient DESs. Fortunately, novel DESs based on cyclohexanone (menthol analogues) were successfully developed with a yield of 98.85%.

2024-10-01·Neurogastroenterology & Motility

The combination of L‐menthol and caraway oil does not affect gastric function but increases hunger in healthy subjects

Article

作者: Mori, Hideki ; Tackoen, Julie ; Ruilova Sosoranga, Emily ; Van Oudenhove, Lukas ; Masuy, Imke ; Verbeure, Wout ; Tack, Jan

AbstractBackgroundThe heterogeneous character of functional gastrointestinal disorders, recently renamed into disorders of gut‐brain interaction, makes finding effective treatment options challenging. Compared to synthetic drugs, phytotherapy can have broader pharmacological effects and is often better tolerated. This study aimed to investigate the effect of peppermint oil and caraway oil (POCO) on gastric function and symptom levels in 32 healthy subjects in a single‐blinded, placebo‐controlled, randomized, parallel design.MethodsGastric emptying rate was assessed using a 13C‐breath test. Intragastric pressure was measured using high‐resolution manometry in fasted state and during intragastric infusion of a nutrient drink (350 mL or until full satiation). GI symptoms were rated on a 100 mm VAS. Data were analyzed using linear mixed models.Key ResultsPOCO had no effect on intragastric pressure in fasted or fed state (p > 0.08 for all). No significant differences in gastric emptying rate were observed (p = 0.54). In the fasted state, a stronger increase in hunger and decrease in satiety were observed following POCO (p = 0.016 and p = 0.008, respectively). No differences in hunger and satiety were observed in the fed state (p > 0.31 for all). POCO induced less epigastric burning, bloating, and fullness (p < 0.05 for all).ConclusionsAcute POCO administration did not affect gastric function in healthy subjects, but increased fasted hunger ratings. The effects of POCO on gastric function and hunger sensations in patients with disorders of gut‐brain interaction, and the contribution to symptom improvement, needs to be elucidated in future studies.

100 项与左旋薄荷醇相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	左旋薄荷醇	-	DB00825

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
肠道疾病	药物发现	日本	Nihon Pharmaceutical Co., Ltd.	2014-10-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


UEGW	N/A	-	-	Menthol infusion	淵網鬱構夢糧廠鹽選糧(築醖夢壓窪網醖醖壓鹹) = 選選糧餘廠獵淵餘鬱積淵築積製獵鬱鑰獵繭襯 (憲憲選廠製鹽築憲憲積, 116.2) 更多	-	2017-10-01
UEGW	N/A	-	-	L-Menthol (Baseline recording)	淵網鬱構夢糧廠鹽選糧(築醖夢壓窪網醖醖壓鹹) = 鬱獵鹽襯鹽醖製觸醖範淵築積製獵鬱鑰獵繭襯 (憲憲選廠製鹽築憲憲積, 126.2) 更多	-	2017-10-01
NCT01687101 (CTgov)	N/A	偏头痛 \| 头痛	32	STOPAIN topical gel	糧願選膚糧簾鑰構膚顧(醖糧網鑰鹹齋夢淵製簾) = 齋壓壓鹹鹽醖窪膚鹽選簾鹽遞壓廠衊壓鹽構壓 (鏇製觸繭鏇艱顧憲顧衊, 範鹹淵餘積選廠鏇願壓 ~ 顧壓齋築糧夢衊鹹衊淵) 更多	-	2015-04-27