resterons

Resterons are a class of synthetic small molecules used to modulate receptor signaling in biological systems. They function as positive or negative allosteric modulators of G protein-coupled receptors (GPCRs) and have been reported to bias signaling toward specific downstream pathways, enabling selective pharmacology with potentially fewer side effects.

The term remaining in use within pharmacology reflects their role in allosteric modulation and was first described in the mid-2010s by researchers exploring receptor-biased signaling in GPCRs.

Resterons typically feature a heteroaryl-alkyl framework with a chiral center; molecules range 250–450 daltons; they display moderate lipophilicity (logP 2–4) and high receptor affinity in the nanomolar range for targeted GPCRs; enantiomeric pairs may show distinct activity.

They are used as research tools to study receptor signaling and biased agonism, with potential therapeutic applications in pain, mood disorders, and metabolic diseases. They are not currently approved for clinical use and require extensive safety profiling.

Synthesis often relies on modular cross-coupling strategies and is typically performed at multi-gram scales for research purposes; compounds are handled under standard laboratory safety guidelines.

As of now, research is mainly preclinical, with several groups reporting selective modulators for serotonin and dopamine receptors. Development of pharmacokinetic and selectivity data remains an area of active investigation.