Identification of Psychoplastogenic Tropanes Lacking Muscarinic Activity

J Med Chem. 2024 Jul 25;67(14):12410-12427. doi: 10.1021/acs.jmedchem.4c01204. Epub 2024 Jul 9.

Abstract

Tropane-containing small molecules like scopolamine are a promising class of psychoplastogens. However, their potent antagonism of all muscarinic receptor subtypes presents the potential for undesirable anticholinergic side effects. In an effort to decouple their neuroplasticity-promoting effects from their muscarinic activity, we performed phenotypic structure-activity relationship studies across a variety of structurally distinct subclasses of tropanes. We discovered several novel tropanes capable of significantly increasing cortical neuronal growth while exhibiting drastically reduced activity at all muscarinic receptor subtypes compared to scopolamine.

MeSH terms

  • Animals
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism
  • Humans
  • Mice
  • Muscarinic Antagonists / chemistry
  • Muscarinic Antagonists / pharmacology
  • Neurons / drug effects
  • Neurons / metabolism
  • Rats
  • Receptors, Muscarinic* / chemistry
  • Receptors, Muscarinic* / metabolism
  • Scopolamine / pharmacology
  • Structure-Activity Relationship
  • Tropanes* / chemistry
  • Tropanes* / metabolism
  • Tropanes* / pharmacology

Substances

  • Tropanes
  • Receptors, Muscarinic
  • Scopolamine
  • Muscarinic Antagonists