Produces 5-HT2A Receptor Antagonism in a Subject, Enabling the Development of Potential Antipsychotic and/or Antischizophrenic Treatments
This compound, Atheliapyrrolidine A, produces 5-HT2A receptor antagonism for treating psychiatric disorders. The 5-HT2A receptor (5-HT2AR) is one of 14 genetically encoded 5-HT serotonin receptors in humans. Antagonists are chemicals blocking the uptake of specific neurotransmitters, in this case, serotonin, by their corresponding receptor, stymieing the brain activity the neurotransmitter would typically produce. Many medications for the treatment of various types of psychosis, such as schizophrenia, major depressive disorder, post-traumatic stress disorder, or obsessive-compulsive disorder, are serotonin antagonists. However, there is a need for additional 5-HT2AR antagonist drugs.
The genus Athelia is a Basidiomycota fungus that produces sclerotia structures mimicking the appearance of termite eggs, also known as “termite balls.” Termite balls are brown, with a similar size and different shape to termite eggs. The fungal sclerotia may protect the eggs in a termite nest from putative pathogens and termites appear to recognize the sclerotia and care for them like their eggs. Details on this specific mutualistic symbiotic relationship are currently under investigation.
Researchers at the University of Florida, elucidating the chemical interactions between termites and Athelia termite balls, have discovered atheliapyrrolidine A, a 5-HT2A receptor antagonist. By selectively blocking the 5-HT2A receptor, this compound isolated from Athelia termite balls can potentially treat multiple psychotic disorders.
Application
5-HT2A receptor antagonist to develop antipsychotic and antischizophrenic drugs, treating psychotic disorders
Advantages
- Atheliapyrrolidine exhibits antagonistic activity against the 5-HT2A receptor with no agonist properties, constituting a specific antipsychotic therapeutic
- Targets the 5-HT2A receptor in humans and other mammals, expanding its potential antipsychotic therapeutic for a spectrum of subjects
- Different administration strategies include oral, sublingually, intranasally, rectally, topically, intradermally, and intravenously, enabling tailoring of administration according to specific needs
Technology
Researchers at the University of Florida have isolated atheliapyrrolidine, a 5-HT2A receptor (5-HT2AR) antagonist, from termite egg-mimicking root structures formed by Athelia fungus, also known as sclerotia. More specifically, atheliapyrrolidine isolates from the TMB strain T5 sclerotia from the genus Athelia. Blockading the 5-HT2A receptor is a conventional strategy for the treatment of multiple psychotic disorders, including schizophrenia, obsessive-compulsive disorder, major depressive disorder, Autism, and PTSD, making atheliapyrrolidine a potential antipsychotic drug. This compound in vitro exhibits selective antagonistic activity like conventional 5-HT2AR antagonists, such as clozapine, with no agonist properties, making it a specific antipsychotic therapeutic.
