ISSN:
1573-3904
Keywords:
neurokinin A
;
substance P
;
tachykinins
;
tetrahydrocarbazole
;
tetrahydro-β-carboline
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Abstract Chemical modifications on the NK1 competitive antagonist L-732,138, with a view to creating a dual NK1/NK2 ligand, led to the tryptophan derivative 1 possessing the protected Gly-Leu sequence of the C-terminus of substance P and neurokinin A. Modifications in the nature of the carbamate function increased the selectivity for the NK1 receptor, whereas the inclusion of the indole moiety in β-carboline or carbazole rings decreased the affinity for both receptors. Free indolylmethyl and Cbz carbamate groups were shown to be essential for NK2 affinity.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1023/A:1008844323931
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