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Three new cyclic substance P analogues were prepared to examine the possible role of a pseudocyclic turn structure for receptor recognition. In the guinea pig isolated ileum [Cys5, Cys11]-SP5-11-NH2 and [Cys6, Cys11]-SP5-11-NH2 were inactive at concentrations up to 100 microM, while [Cys5, Cys6, Nle11]-SP was a weak agonist. The order of relative affinities on the rat brain radioreceptor assay was as follows: [Cys5, Cys6, Nle11]-SP greater than [Cys5, Cys11]-SP5-11-NH2 greater than [Cys6, Cys11]-SP5-11-NH2. We interpret these results to indicate that a pseudocyclic structure of the 5-11 sequence may not be an important factor involved in the receptor recognition of substance P.
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
October 1992,
Journal of medicinal chemistry,
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
November 2007,
Bioorganic & medicinal chemistry letters,
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
August 2009,
The Journal of organic chemistry,
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
August 2000,
Chemistry (Weinheim an der Bergstrasse, Germany),
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
August 1998,
Bioorganic & medicinal chemistry letters,
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
January 2004,
Acta biochimica Polonica,
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
July 2007,
Journal of medicinal chemistry,
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
February 2002,
Bioorganic & medicinal chemistry,
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
April 1977,
Journal of medicinal chemistry,
P S Darman, and
G C Landis, and
J R Smits, and
L D Hirning, and
K Gulya, and
H I Yamamura, and
T F Burks, and
V J Hruby
September 1983,
Biochimica et biophysica acta,
