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Conformationally restricted cyclic analogues of substance P: insight into the receptor binding process

Darman, P.S.; Landis, G.C.; Smits, J.R.; Hirning, L.D.; Gulya, K.; Yamamura, H.I.; Burks, T.F.; Hruby, V.J.

Biochemical and Biophysical Research Communications 127(2): 656-662

1985

ISSN/ISBN: 0006-291X
PMID: 2579658
Document Number: 260152
Three new cyclic substance P analog were prepared to examine the possible role of a pseudocyclic turn structure for receptor recognition. In the guinea pig isolated ileum .**GRAPHIC**. and .**GRAPHIC**. were inactive at concentrations up to 100 .mu.M, while .**GRAPHIC**. was a weak agonist. The order of relative affinities on the rat brain radioreceptor assay was as follows: .**GRAPHIC**. > .**GRAPHIC**. > .**GRAPHIC**. Apparently, a pseudocyclic structure of the 5-11 sequence may not be an important factor involved in the receptor recognition of substance P.

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