Structural determinants of substrates and inhibitors : Probing glutamate transporters with 2,4-methanopyrrolidine-2,4-dicarboxylate

Using an intramolecular [2 + 2] photocyclization, 2,4-methanopyrrolidine-2,4-dicarboxylate was prepared as a conformationally locked analogue of glutamate. This compound, in combination with two other pyrrolidine dicarboxylates, has been used to define the structural elements that differentiate subs...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-11, Vol.8 (21), p.3101-3106
Hauptverfasser:	ESSLINGER, C. S, KOCH, H. P, KAVANAUGH, M. P, PHILIPS, D. P, CHAMBERLIN, A. R, THOMPSON, C. M, BRIDGES, R. J
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Transport System X-AG Animals ATP-Binding Cassette Transporters - antagonists & inhibitors Biological and medical sciences Dicarboxylic Acids - chemical synthesis Glutamatergic system (aspartate and other excitatory aminoacids) Glutamic Acid - analogs & derivatives Male Medical sciences Molecular Conformation Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyrrolidines - chemical synthesis Rats Rats, Sprague-Dawley
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	Using an intramolecular [2 + 2] photocyclization, 2,4-methanopyrrolidine-2,4-dicarboxylate was prepared as a conformationally locked analogue of glutamate. This compound, in combination with two other pyrrolidine dicarboxylates, has been used to define the structural elements that differentiate substrate and nonsubstrate inhibitors of a high-affinity, sodium-dependent glutamate transporter.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00560-5