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

4-Benzyl-1-[4-(1H-imidazol-4-yl)but-3-ynyl]piperidine (8) has been identified as a potent antagonist of the NR1A/2B subtype of the NMDA receptor. When dosed orally, this compound potentiates the effects of L-DOPA in the 6-hydroxydopamine-lesioned rat, a model of Parkinson's disease.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1999-10, Vol.9 (19), p.2815-2818
Hauptverfasser:	WRIGHT, J. L, GREGORY, T. F, WHITTEMORE, E. R, WOODWARD, R. M, YANG, K. C, ZHOU, Z.-L, BOXER, P. A, MELTZER, L. T, SERPA, K. A, WISE, L. D, HONG-BAE, S, HUANG, J. C, KONKOY, C. S, UPASANI, R. B
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Disease Models, Animal Glutamatergic system (aspartate and other excitatory aminoacids) Imidazoles - chemical synthesis Imidazoles - pharmacology Levodopa - agonists Levodopa - pharmacology Ligands Medical sciences Molecular Structure Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oxidopamine Parkinsonian Disorders - metabolism Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - pharmacology Pyrazoles - chemical synthesis Pyrazoles - pharmacology Pyrroles - chemical synthesis Pyrroles - pharmacology Rats Receptors, N-Methyl-D-Aspartate - antagonists & inhibitors
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Beschreibung
Zusammenfassung:	4-Benzyl-1-[4-(1H-imidazol-4-yl)but-3-ynyl]piperidine (8) has been identified as a potent antagonist of the NR1A/2B subtype of the NMDA receptor. When dosed orally, this compound potentiates the effects of L-DOPA in the 6-hydroxydopamine-lesioned rat, a model of Parkinson's disease.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00482-5