Mechanism of analgesia by gabapentinoid drugs: Involvement of modulation of synaptogenesis and trafficking of glutamate-gated ion channels
G Varadi - Journal of Pharmacology and Experimental …, 2024 - ASPET
Gabapentinoids have clinically been used for treating epilepsy, neuropathic pain, and
several other neurologic disorders for> 30 years; however, the definitive molecular …
several other neurologic disorders for> 30 years; however, the definitive molecular …
EMC chaperone–CaV structure reveals an ion channel assembly intermediate
Voltage-gated ion channels (VGICs) comprise multiple structural units, the assembly of
which is required for function,. Structural understanding of how VGIC subunits assemble and …
which is required for function,. Structural understanding of how VGIC subunits assemble and …
Structural biology of voltage-gated calcium channels
Voltage-gated calcium (Cav) channels mediate Ca2+ influx in response to membrane
depolarization, playing critical roles in diverse physiological processes. Dysfunction or …
depolarization, playing critical roles in diverse physiological processes. Dysfunction or …
Naturally inspired molecules for neuropathic pain inhibition—effect of mirogabalin and cebranopadol on mechanical and thermal nociceptive threshold in mice
Background: Neuropathic pain is drug-resistant to available analgesics and therefore novel
treatment options for this debilitating clinical condition are urgently needed. Recently, two …
treatment options for this debilitating clinical condition are urgently needed. Recently, two …
Towards Multitargeted Ligands as Pain Therapeutics: Dual Ligands of the Cavα2δ‐1 Subunit of Voltage‐Gated Calcium Channel and the μ‐Opioid Receptor
A Wegert, M Monnee, W de Graaf, F van Holst… - …, 2024 - Wiley Online Library
The synthesis and pharmacological activity of a new series of dual ligands combining
activities towards the α2δ‐1 subunit of voltage‐gated calcium channels (Cavα2δ‐1) and the …
activities towards the α2δ‐1 subunit of voltage‐gated calcium channels (Cavα2δ‐1) and the …
[HTML][HTML] Determinants of interactions of a novel next-generation gabapentinoid NVA1309 and mirogabalin with the Cavα2δ-1 subunit
NVA1309 is a non-brain penetrant next-generation gabapentinoid shown to bind Cavα2δ at
R243 within a triple Arginine motif forming the binding site for gabapentin and pregabalin. In …
R243 within a triple Arginine motif forming the binding site for gabapentin and pregabalin. In …