Where do we go next in antidepressant drug discovery? A new generation of antidepressants: a pivotal role of AMPA receptor potentiation and mGlu2/3 receptor antagonism

Expert Opin Drug Discov. 2022 Oct;17(10):1131-1146. doi: 10.1080/17460441.2022.2111415. Epub 2022 Aug 22.

Abstract

Introduction: Major depressive disorder remains a prevalent world-wide health problem. Currently available antidepressant medications take weeks of dosing, do not produce antidepressant response in all patients, and have undesirable ancillary effects.

Areas covered: The present opinion piece focuses on the major inroads to the creation of new antidepressants. These include N-methyl-D-aspartate (NMDA) receptor antagonists and related compounds like ketamine, psychedelic drugs like psilocybin, and muscarinic receptor antagonists like scopolamine. The preclinical and clinical pharmacological profile of these new-age antidepressant drugs is discussed.

Expert opinion: Preclinical and clinical data have accumulated to predict a next generation of antidepressant medicines. In contrast to the current standard of care antidepressant drugs, these compounds differ in that they demonstrate rapid activity, often after a single dose, and effects that outlive their presence in brain. These compounds also can provide efficacy for treatment-resistant depressed patients. The mechanism of action of these compounds suggests a strong glutamatergic component that involves the facilitation of AMPA receptor function. Antagonism of mGlu2/3 receptors is also relevant to the antidepressant pharmacology of this new class of drugs. Based upon the ongoing efforts to develop these new-age antidepressants, new drug approvals are predicted in the near future.

Keywords: AMPA receptors; AMPAkines; Depression; NMDA receptors; hallucinogens; ketamine; mGlu2/3 antagonists; psychedelics; scopolamine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antidepressive Agents / pharmacology
  • Antidepressive Agents / therapeutic use
  • Depression / drug therapy
  • Depressive Disorder, Major* / drug therapy
  • Humans
  • Ketamine* / pharmacology
  • Receptors, AMPA
  • Receptors, N-Methyl-D-Aspartate
  • Scopolamine / therapeutic use

Substances

  • Receptors, AMPA
  • Antidepressive Agents
  • Ketamine
  • Scopolamine
  • Receptors, N-Methyl-D-Aspartate