Discovery of subtype-selective NMDA receptor ligands: 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists.

doi:10.1016/S0960-894X(99)00482-5

Paper

DOI: 10.1016/S0960-894X(99)00482-5

Discovery of subtype-selective NMDA receptor ligands: 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists.

Published Oct 4, 1999 · J. Wright, T. Gregory, P. Boxer

Bioorganic & medicinal chemistry letters

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4-Benzyl-1-[4-(1 H -imidazol-4-yl)but-3-ynyl)but-3-ynyl]piperidine is a potent antagonist of the NR1A/2B subtype of NMDA receptor, potentiating L-

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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References

DOI: 10.1021/JM990148X

Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.

4-benzyl-1-(4-phenyl-3-butynyl)piperidine (8) is a moderately potent and selective antagonist of the NR1A/2B subtype of NMDA receptors, with hydroxyl propyne (48) and butyne (23)

1999·34citations·J. Wright et al.·Journal of medicinal chemistry

Journal of medicinal chemistry

DOI: 10.1021/JO971572D

A Practical and Efficient Synthesis of the Selective Neuronal Acetylcholine-Gated Ion Channel Agonist (S)-(−)-5-Ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine Maleate (SIB-1508Y)

This study presents a practical and efficient synthetic procedure for the preparation of the novel neuronal acetylcholine-gated ion channel agonist (S)-()-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (

1998·71citations·L. Bleicher et al.·Journal of Organic Chemistry

Journal of Organic Chemistry

DOI: 10.1016/0040-4020(96)00823-X

Palladium catalysed coupling of imidazoles to alkynyl and vinyl substrates

Palladium-catalyzed coupling of imidazoles to alkynyl and vinyl substrates can produce 4-substituted imidazoles under Stille conditions.

1996·17citations·M. Cliff et al.·Tetrahedron

Tetrahedron

DOI: 10.1038/358036A0

Molecular diversity of the NMDA receptor channel

The molecular diversity of the subunit family underlies the functional heterogeneity of the NMDA receptor channel, with distinct agonist affinities and sensitivities in heteromeric heteromers.

1992·1339citations·T. Kutsuwada et al.·Nature

Nature

DOI: 10.1038/354031A0

Molecular cloning and characterization of the rat NMDA receptor

The rat NMDA receptor, with its characteristic electrophysiological and pharmacological properties, has been cloned and characterized, with its expression in neuronal cells throughout the brain.

1991·1778citations·K. Moriyoshi et al.·Nature

Nature

Citations

DOI: 10.1016/j.ejmech.2020.112447

A comprehensive description of GluN2B-selective N-methyl-D-aspartate (NMDA) receptor antagonists.

GluN2B-selective NMDA antagonists show potential as effective treatments for various CNS diseases, with two main categories: prototypical and atypical antagonists.

2020·51citations·Wen-wu Liu et al.·European journal of medicinal chemistry

European journal of medicinal chemistry

DOI: 10.1070/RC2014v083n06ABEH004418

C-Ethynylpyrroles: synthesis and reactivity

C-ethynylpyrroles show high reactivity, particularly in cycloaddition and intramolecular cyclization reactions, which can form new pyrrole systems.

2014·21citations·L. N. Sobenina et al.·Russian Chemical Reviews

Russian Chemical Reviews

DOI: 10.2174/187152709789824606

Glutamate receptors as therapeutic targets for Parkinson's disease.

Modulating glutamate receptors may alleviate Parkinson's disease symptoms and slow disease progression by delaying dopamine neuron degeneration.

2009·238citations·Kari A. Johnson et al.·CNS & neurological disorders drug targets

CNS & neurological disorders drug targets

DOI: 10.1517/13543776.15.4.389

NR2B subtype-selective NMDA receptor antagonists: 2001 – 2004

NR2B-selective NMDA antagonists show potential for improved therapeutic outcomes due to reduced CNS side effects and increased structural diversity.

2005·26citations·J. Mccauley·Expert Opinion on Therapeutic Patents

Expert Opinion on Therapeutic Patents

DOI: 10.1016/S0960-894X(03)00713-3

1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists.

This study identified a novel class of potent and selective NMDA receptor blockers, NR1/2B subtype, through screening of the Roche compound depository.

2003·21citations·A. Alanine et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

DOI: 10.1016/S0960-894X(03)00007-6

2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.

2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines are a novel class of NR1/2B subtype selective NMDA receptor antagonists with high affinity and in vivo activity.

2003·19citations·B. Büttelmann et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters

DOI: 10.1016/S0960-894X(02)00470-5

4-Aminoquinolines as a novel class of NR1/2B subtype selective NMDA receptor antagonists.

4-aminoquinoline 4 is a novel, highly potent, and in vivo active NMDA receptor antagonist, discovered through screening of the Roche compound library.

2002·25citations·E. Pinard et al.·Bioorganic & medicinal chemistry letters

Bioorganic & medicinal chemistry letters