586-60-7
Chemical Structure
Dyclonine
Synonym(s): Dyclocaine
- CAS No.: 586-60-7
- Formula:C18H27NO2
- Molecular Weight:289.41
InChIKey: BZEWSEKUUPWQDQ-UHFFFAOYSA-N
SMILES: O=C(CCN1CCCCC1)C2=CC=C(C=C2)OCCCC
Biological Activity: Dyclonine (Dyclocaine) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis[1][2][3][4].
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Dyclonine | Dyclonine (Dyclocaine) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis. | |||||||||||||||||||||
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References
- [1]. Bailly C, et al. A new horizon for the anesthetic drug dyclonine. Biochemical pharmacology. 2026 Feb;244:117569. [Content Brief]
- [2]. Sahdeo S, et al. Dyclonine rescues frataxin deficiency in animal models and buccal cells of patients with Friedreich's ataxia. Human molecular genetics. 2014 Dec 20;23(25):6848-62. [Content Brief]
- [3]. Liu Q, et al. Therapeutic inhibition of keratinocyte TRPV3 sensory channel by local anesthetic dyclonine. eLife. 2021 Apr 20;10:e68128. [Content Brief]
