1679-76-1
Chemical Structure
Drofenine
Synonym(s): Cycloadiphene; Hexahydroadiphenine
- CAS No.: 1679-76-1
- Formula:C20H31NO2
- Molecular Weight:317.47
IUPAC Name: 2-(diethylamino)ethyl 2-cyclohexyl-2-phenylacetate
InChIKey: AGJBLWCLQCKRJP-UHFFFAOYSA-N
SMILES: O=C(OCCN(CC)CC)C(C1CCCCC1)C2=CC=CC=C2
Biological Activity: Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm[1][2][3][4].
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Drofenine | Drofenine (Cycloadiphene; Hexahydroadiphenine) is an brain-penetrant antispasmodic agent. Drofenine is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine ameliorates diabetic peripheral neuropathy -like pathology. Drofenine can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm. | |||||||||||||||||||||
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- [1]. Lu J, et al. Drofenine as a Kv2.1 inhibitor alleviated AD-like pathology in mice through Aβ/Kv2.1/microglial NLRP3/neuronal Tau axis. Acta Pharm Sin B. 2025;15(1):371-391. [Content Brief]
- [2]. Xu X, et al. Antispasmodic Drug Drofenine as an Inhibitor of Kv2.1 Channel Ameliorates Peripheral Neuropathy in Diabetic Mice. iScience. 2020;23(10):101617. Published 2020 Sep 28. [Content Brief]
- [3]. Bodur E, et al. Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. Arch Biochem Biophys. 2001;386(1):25-29. [Content Brief]
- [4]. Deering‐Rice C E, et al. Drofenine: a 2‐APB analog with improved selectivity for human TRPV3[J]. Pharmacology research & perspectives, 2014, 2(5): e00062. [Content Brief]
Keywords
