Inhibition of NMDA receptors and other ion channel types by membrane-associated drugs DOI Creative Commons

Elizabeth G. Neureiter,

M. Quincy Erickson-Oberg,

Aparna Nigam

et al.

Frontiers in Pharmacology, Journal Year: 2025, Volume and Issue: 16

Published: April 30, 2025

N-methyl-D-aspartate receptors (NMDARs) are ligand-gated ion channels present at most excitatory synapses in the brain that play essential roles cognitive functions including learning and memory consolidation. However, NMDAR dysregulation is implicated many nervous system disorders. Diseases involve pathological hyperactivity of NMDARs can be treated clinically through inhibition by channel blocking drugs. block occur via two known mechanisms. First, traditional block, charged drug molecules enter directly from extracellular solution after activation opening. Second, uncharged hydrophobic plasma membrane, upon membrane-associated transit into a fenestration within NMDAR. This mechanism action called membrane to (MCI) not well understood despite clinical importance Intriguingly, route access for drugs unique NMDARs. Our review will address other consider how path may affect drug’s therapeutic potential.

Language: Английский

A Bright Future for Photopharmaceuticals Addressing Central Nervous System Disorders: State of the Art and Challenges Toward Clinical Translation DOI
Rudolf L. Z. Ganzoni, Sofie S. Bournons, Erick M. Carreira

et al.

Medicinal Research Reviews, Journal Year: 2025, Volume and Issue: unknown

Published: April 5, 2025

ABSTRACT Photopharmacology is an innovative approach that uses light to activate drugs. This method offers the potential for highly localized and precise drug activation, making it particularly promising treatment of neurological disorders. Despite enticing prospects photopharmacology, its application treat human central nervous system (CNS) diseases remains be demonstrated. In this review, we provide overview prominent strategies design activation photopharmaceutical agents in field neuroscience. Photocaged photoswitchable drugs bioactive molecules are discussed, instructive list examples provided highlight compound strategies. Special emphasis placed on photoactivatable compounds modulation glutamatergic, GABAergic, dopaminergic, serotonergic neurotransmission conditions, as well various photoresponsive with improved pain management. Compounds holding promise clinical translation discussed in‐depth their future applications assessed. Neurophotopharmaceuticals have yet achieve breakthrough clinic, both delivery not reached full maturity. However, by describing current state art providing illustrative case studies, offer a perspective opportunities neurophotopharmacology focused addressing CNS

Language: Английский

Citations

0
Inhibition of NMDA receptors and other ion channel types by membrane-associated drugs DOI Creative Commons

Elizabeth G. Neureiter,

M. Quincy Erickson-Oberg,

Aparna Nigam

et al.

Frontiers in Pharmacology, Journal Year: 2025, Volume and Issue: 16

Published: April 30, 2025

N-methyl-D-aspartate receptors (NMDARs) are ligand-gated ion channels present at most excitatory synapses in the brain that play essential roles cognitive functions including learning and memory consolidation. However, NMDAR dysregulation is implicated many nervous system disorders. Diseases involve pathological hyperactivity of NMDARs can be treated clinically through inhibition by channel blocking drugs. block occur via two known mechanisms. First, traditional block, charged drug molecules enter directly from extracellular solution after activation opening. Second, uncharged hydrophobic plasma membrane, upon membrane-associated transit into a fenestration within NMDAR. This mechanism action called membrane to (MCI) not well understood despite clinical importance Intriguingly, route access for drugs unique NMDARs. Our review will address other consider how path may affect drug’s therapeutic potential.

Language: Английский

Citations

0