Topic: positive allosteric modulators

Ionotropic glycine receptors (GlyRs) are chloride-permeable ligand-gated ion channels expressed in neurons of the central nervous system. These receptors play a key role in regulating neuronal membrane potential, impacting various physiological processes, including motor control, respiratory rhythm, and pain modulation. Consistent with its relevance, positive allosteric modulators (PAMs) of GlyRs have shown analgesic effects in chronic pain models. A promising group of glycinergic PAMs are the tricyclic sulfonamides (TS), such as AM-1488, which has been majorly studied using biochemical and hi

Y-Aminobutyric acid type A (GABA-A) receptors are GABA-gated ion channels that are assembled of 5 (out of a set of 19) subunits, with six possible different alpha subunits. These differently assembled subunits lead to receptors with unique pharmacological and physiological properties that also show unique anatomical distribution. Animal models of several neuropsychiatric conditions suggest that compounds selectively activating, or positively modulating, cerebellar alpha6-containing GABA-A receptors can have highly beneficial effects on different diseases. For the case of essential tremor, flum