Kainic Acid-Based Agonists of Glutamate Receptors: SAR Analysis and Guidelines for Analog Design.

Animals Excitatory Amino Acid Agonists / pharmacology Kainic Acid / analogs & derivatives Receptors, Kainic Acid / metabolism Structure-Activity Relationship
domoic acid kainate receptors kainic acid kainoids structure−activity relationship

Journal

ACS chemical neuroscience
ISSN: 1948-7193
Titre abrégé: ACS Chem Neurosci
Pays: United States
ID NLM: 101525337

Informations de publication

Date de publication:
16 10 2019
Historique:
pubmed: 25 9 2019
medline: 5 9 2020
entrez: 25 9 2019
Statut: ppublish

Résumé

A comprehensive survey of kainic acid analogs that have been tested for their biological activity is presented. Specifically, this review (1) gathers and compares over 100 kainoids according to a relative activity scale, (2) exposes structural features required to optimize affinity for kainate receptors, and (3) suggests design rules to create next-generation KA analogs. Literature SAR data are analyzed systematically and combined with the most recent crystallographic studies. In view of the renewed interest in neuroactive molecules, this review aims to help guide the efforts of organic synthesis laboratories, as well as to inform newcomers to KA/GluK research.

Identifiants

DOI: 10.1021/acschemneuro.9b00349 PMID: 31550120
pubmed: 31550120
doi: 10.1021/acschemneuro.9b00349
doi:

Substances chimiques

Excitatory Amino Acid Agonists 0
Receptors, Kainic Acid 0
Kainic Acid SIV03811UC

Types de publication

Journal Article Research Support, Non-U.S. Gov't Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

4190-4198

Auteurs

Zhenlin Tian (Z)

Department of Chemistry , University of British Columbia , Kelowna , BC V1V 1V7 , Canada.

Brianna L M Clark (BLM)

Department of Chemistry , University of British Columbia , Kelowna , BC V1V 1V7 , Canada.

Frederic Menard (F)

Department of Chemistry , University of British Columbia , Kelowna , BC V1V 1V7 , Canada.
ORCID: 0000-0002-4135-4417

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Kainic Acid-Based Agonists of Glutamate...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Agents neuromédiateurs › Agents des acides aminés excitateurs › Agonistes des acides aminés excitateurs › Kainic Acid-Based Agonists of Glutamate...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Pyrrolidines › Acide kaïnique › Kainic Acid-Based Agonists of Glutamate...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Récepteurs de surface cellulaire › Récepteurs aux neuromédiateurs › Récepteurs aux acides aminés › Récepteurs au glutamate › Récepteurs ionotropes du glutamate › Récepteurs kaïnate › Kainic Acid-Based Agonists of Glutamate...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Kainic Acid-Based Agonists of Glutamate...