2-Aryl indole NK1 receptor antagonists : Optimisation of indole substitution

The synthesis and biological evaluation of a series of 2-aryl indoles with high affinity for the human neurokinin-1 (hNK1) receptor are reported, concentrating on optimisation of the indole substitution.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-05, Vol.11 (9), p.1233-1236
Main Authors: COOPER, Laura C, CHICCHI, Gary G, WATT, Alan P, WILLIAMS, Angela R, SWAIN, Christopher J, DINNELL, Kevin, ELLIOTT, Jason M, HOLLINGWORTH, Gregory J, KURTZ, Mare M, LOCKER, Karen L, MORRISON, Denise, SHAW, Duncan E, TSAO, Kwei-Lan
Format: Article
Language:English
Subjects:
Animals
Behavior, Animal
Binding, Competitive - drug effects
Biological and medical sciences
Brain Chemistry
CHO Cells
Cricetinae
Gerbillinae
Indicators and Reagents
Indoles - chemical synthesis
Indoles - pharmacokinetics
Indoles - pharmacology
Medical sciences
Neurokinin-1 Receptor Antagonists
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Rats
Structure-Activity Relationship
Substance P - metabolism
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Description
Summary:The synthesis and biological evaluation of a series of 2-aryl indoles with high affinity for the human neurokinin-1 (hNK1) receptor are reported, concentrating on optimisation of the indole substitution.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00182-2