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<p>The endogenous cannabinoid palmitoylethanolamide (PEA) has shown efficacy in the treatment of a wide range of diseases, including parkinsonism, Alzheimer’s disease, epilepsy, depression, stroke, traumatic brain injury, cognitive and behavioral disorders, oncology, and diseases caused by bacteria and viruses. Clinical trials of PEA showed the absence of any significant side effects. The disadvantage of PEA is the lack of a dosage form for injection (it is used only orally) because of its insolubility in water. Nine water-soluble analogs of PEA, particularly IEM-1875, were obtained by us by replacing the terminal OH group of PEA with an NH<sub>2</sub> group. IEM-1875 in animal experiments showed pharmacological properties like PEA, in particular, analgesic, anticonvulsant, neuroprotective, antihypoxic, and antiparkinsonian properties with acute toxicity ≥2 g/kg (when administered parenterally). IEM-1875 potentiated the effects of mono- and dicationic glutamate blockers, including memantine, allowing their effective doses to be reduced by an order of magnitude or more.</p>

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Water-Soluble Analogs of Palmitoylethanolamide and Its Combination with Adamantane- and Phenylcyclohexyl-Containing Glutamate Blockers

  • 期刊论文

  • 发表日期：

    2025年4月1日

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  • V. E. Gmiro,
  • S. E. Serdyuk

摘要

The endogenous cannabinoid palmitoylethanolamide (PEA) has shown efficacy in the treatment of a wide range of diseases, including parkinsonism, Alzheimer’s disease, epilepsy, depression, stroke, traumatic brain injury, cognitive and behavioral disorders, oncology, and diseases caused by bacteria and viruses. Clinical trials of PEA showed the absence of any significant side effects. The disadvantage of PEA is the lack of a dosage form for injection (it is used only orally) because of its insolubility in water. Nine water-soluble analogs of PEA, particularly IEM-1875, were obtained by us by replacing the terminal OH group of PEA with an NH2 group. IEM-1875 in animal experiments showed pharmacological properties like PEA, in particular, analgesic, anticonvulsant, neuroprotective, antihypoxic, and antiparkinsonian properties with acute toxicity ≥2 g/kg (when administered parenterally). IEM-1875 potentiated the effects of mono- and dicationic glutamate blockers, including memantine, allowing their effective doses to be reduced by an order of magnitude or more.