Other aminergic G protein-coupled receptors

Other aminergic G protein-coupled receptors (GPCRs) represent a diverse subgroup of Class A (rhodopsin-like) receptors that are activated by biogenic amines, including dopamine, serotonin, histamine, and trace amines (Alexander et al., 2023). This classification often encompasses the trace amine-associated receptors (TAARs) and various orphan receptors that bind biogenic amines but do not fit into the primary neurotransmitter subfamilies like the adrenoceptors or muscarinic receptors (Gainetdinov et al., 2018). These receptors are critical for signal transduction within the central and peripheral nervous systems, where they regulate mood, cognition, and autonomic functions by acting as rheostats for classical neurotransmitter systems (Sexton et al., 2019). They are among the most significant therapeutic targets in pharmacology, with a wide range of drugs such as antipsychotics, antidepressants, and novel TAAR1 agonists acting upon them (UniProt, 2024). A major challenge in drug development for this group is the high structural homology between different aminergic receptors, which frequently leads to off-target effects and safety concerns such as cardiotoxicity or metabolic disturbances (Alexander et al., 2023). Recent therapeutic strategies involve the development of highly selective ligands and biased agonists to improve the safety profile of treatments for psychiatric and neurological disorders (Sexton et al., 2019).

Other names

Aminergic GPCRsBiogenic amine receptorsTrace amine-associated receptorsTAARsNon-classical aminergic GPCRs

These receptors function as molecular switches that translate the binding of biogenic amines into intracellular signals via G proteins or beta-arrestins, modulating various physiological responses (Sexton et al., 2019).