intended rapid antidepressant effect

Every compound in the sci-wiki that affects intended rapid antidepressant effect; the ones you can source are floated to the front, then the reference-only entries. Tap any for the full entry, mechanism, and outlets.

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NMDA Modulator

Apimostinel

Apimostinel (NRX-1074) is the understudy in the rapastinel story: developed by the same company, Naurex, using the same core idea of gently boosting NMDA receptor signaling at the glycine co-agonist site rather than blocking the channel like ketamine does. Naurex called this class of drugs Stinels, framing them as neuroplastogens meant to trigger rapid synaptic strengthening and antidepressant effects without dissociation. Allergan acquired Naurex in 2015 largely to get the entire Stinel franchise, including apimostinel as a potentially more potent follow-on to rapastinel, and moved it into Phase I/II testing. But when rapastinel, the lead compound and more advanced sibling, failed its own Phase III depression trials, Allergan shut down the whole glycine-site NMDA program in 2019, and apimostinel never got the chance to run its own late-stage trial.

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NMDA Modulator

AV-101

AV-101 is an oral prodrug, not an active drug in the blood; once it crosses into the brain, astrocytes convert it into 7-chlorokynurenic acid, a potent blocker of the glycine co-agonist site on the NMDA receptor. The pitch from VistaGen Therapeutics was a ketamine-like antidepressant you could take as a pill with none of the dissociation, since the parent compound itself does nothing until it's converted locally in brain tissue. Early studies, including a neurophysiology trial in veterans, confirmed it does engage NMDA receptor signaling in humans exactly as designed. But the pivotal Phase II depression trial did not separate from placebo, and VistaGen shifted its psychiatric pipeline toward other candidates, leaving AV-101 as a mechanistically elegant idea that worked at the target but not at the endpoint.

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