Overview
- Bulaj, G. et al. (2008) J. Med. Chem. 51, 8038.
- White, H.S. et al. (2009) Neurotherapeutics 6, 372.
Alomone Labs NAX-5055 activates GalR2 receptor-mediated Ca2+ mobilization in CHO-K1-Gα16-mt-Aequorin cells.Dose response of normalized NAX-5055 (#N-360) activation of GalR2 receptor-mediated Ca2+ mobilization, measured as aequorin-derived fluorescence following NAX-5055 application (EC50 = 6.12 nM).
NAX-5055 is an active analog of the endogenous neuropeptide galanin that acts as a galanin receptor 1 (GalR1) and galanin receptor 2 (GalR2) agonist. NAX-5055 demonstrates high affinity for the receptors and was shown to prevent seizures in mouse model of epilepsy following intraperitoneal administration1.
NAX-5055 is a systemically-active, metabolically stable galanin analog that can penetrate the blood-brain-barrier and displays a potent anticonvulsant activity2,3.
Galanin is widely expressed throughout the central and peripheral nervous systems. Galanin receptors belong to the family of G-protein coupled receptors. Studies show that galanin and its receptors are involved in the transmission and modulation of nociception in the central nervous system, at spinal cord levels and in the brain4.
