Structure, function, and pharmacology of glutamate receptor ion channels
Many physiologic effects of l-glutamate, the major excitatory neurotransmitter in the
mammalian central nervous system, are mediated via signaling by ionotropic glutamate …
mammalian central nervous system, are mediated via signaling by ionotropic glutamate …
Therapeutic potential of N-methyl-D-aspartate receptor modulators in psychiatry
Abstract N-methyl-D-aspartate (NMDA) receptors mediate a slow component of excitatory
synaptic transmission, are widely distributed throughout the central nervous system, and …
synaptic transmission, are widely distributed throughout the central nervous system, and …
Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead …
MAM Subbaiah, J Rautio, NA Meanwell - Chemical Society Reviews, 2024 - pubs.rsc.org
The delivery of a drug to a specific organ or tissue at an efficacious concentration is the
pharmacokinetic (PK) hallmark of promoting effective pharmacological action at a target site …
pharmacokinetic (PK) hallmark of promoting effective pharmacological action at a target site …
A comprehensive description of GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists
W Liu, X Jiang, Y Zu, Y Yang, Y Liu, X Sun, Z Xu… - European journal of …, 2020 - Elsevier
Abstract l-glutamate is an excitatory neurotransmitter in the central nervous system (CNS),
which can activate ionotropic receptors (iGluRs) and metabotropic (mGluRs) receptors. N …
which can activate ionotropic receptors (iGluRs) and metabotropic (mGluRs) receptors. N …
Highly enantioselective iridium-catalyzed coupling reaction of vinyl azides and racemic allylic carbonates
M Han, M Yang, R Wu, Y Li, T Jia, Y Gao… - Journal of the …, 2020 - ACS Publications
The iridium-catalyzed enantioselective coupling reaction of vinyl azides and allylic
electrophiles is presented and provides access to β-chiral carbonyl derivatives. Vinyl azides …
electrophiles is presented and provides access to β-chiral carbonyl derivatives. Vinyl azides …
Drug development in channelopathies: Allosteric modulation of ligand-gated and voltage-gated ion channels
Y Zhang, K Wang, Z Yu - Journal of medicinal chemistry, 2020 - ACS Publications
Ion channels have been characterized as promising drug targets for treatment of numerous
human diseases. Functions of ion channels can be fine-tuned by allosteric modulators …
human diseases. Functions of ion channels can be fine-tuned by allosteric modulators …
Discovery of novel tryptamine derivatives as GluN2B subunit-containing NMDA receptor antagonists via pharmacophore-merging strategy with orally available …
J Quan, H Yang, F Qin, Y He, J Liu, Y Zhao… - European Journal of …, 2023 - Elsevier
A series of tryptamine derivatives has been designed and synthesized as novel GluN2B
subunit-containing NMDA receptor (GluN2B-NMDAR) antagonists, which could …
subunit-containing NMDA receptor (GluN2B-NMDAR) antagonists, which could …
Ifenprodil rapidly ameliorates depressive-like behaviors, activates mTOR signaling and modulates proinflammatory cytokines in the hippocampus of CUMS rats
Y Yao, P Ju, H Liu, X Wu, Z Niu, Y Zhu, C Zhang… - …, 2020 - Springer
Rationale The rapid-onset and long-lasting antidepressant properties of ketamine have
prompted investigations into a variety of agents that target N-methyl-D-aspartate receptors …
prompted investigations into a variety of agents that target N-methyl-D-aspartate receptors …
Prodrug Strategy to Address Impaired Oral Absorption of a Weakly Basic TYK2 Inhibitor Caused by a Gastric Acid-Reducing Agent
M AM Subbaiah, T Ramar, M Reddy… - Journal of Medicinal …, 2024 - ACS Publications
The pH-dependent solubility of the weakly basic TYK2 inhibitor 1 posed a risk to its
advancement, given that drugs with such profiles have exhibited drug–drug interaction (DDI) …
advancement, given that drugs with such profiles have exhibited drug–drug interaction (DDI) …
Phosphate prodrugs: an approach to improve the bioavailability of clinically approved drugs
The phosphate prodrug approach has emerged as a viable option for increasing the
bioavailability of a drug candidate with low hydrophilicity and poor cell membrane …
bioavailability of a drug candidate with low hydrophilicity and poor cell membrane …