TY - JOUR
T1 - Synthesis and biological activity of Substance P C‐terminal hexapeptide and heptapeptide analogues
AU - STAVROPOULOS, GEORGE
AU - KARAGIANNIS, KOSTAS
AU - CORDOPATIS, PAUL
AU - HALLE, DAVID
AU - GILON, CHAIM
AU - BAR‐AKIVA, GIORA
AU - SELINGER, ZVI
AU - CHOREV, MICHAEL
PY - 1991/3
Y1 - 1991/3
N2 - The analogues [Glu(OBzl)11]SP6–11 and [Glu(OBzl)11]SP5–11 of the C‐terminal hexapeptide and heptapeptide of Substance P have been synthesized by conventional solution methods. In each analogue the SCH3 group of Met11 is replaced by the COOCH2C6H5 group. The in vitro activity of both analogues has been determined on three biological preparations: guinea pig ileum (GPI), rat vas deferens (RVD), and rat portal vein (RPV). The selectivity for the different receptors has been studied by utilizing atropine‐treated guinea pig ileum (GPI + At). The results showed that both analogues are mainly active on GPI through the NK‐1 receptor and that both analogues are equipotent to Substance P.
AB - The analogues [Glu(OBzl)11]SP6–11 and [Glu(OBzl)11]SP5–11 of the C‐terminal hexapeptide and heptapeptide of Substance P have been synthesized by conventional solution methods. In each analogue the SCH3 group of Met11 is replaced by the COOCH2C6H5 group. The in vitro activity of both analogues has been determined on three biological preparations: guinea pig ileum (GPI), rat vas deferens (RVD), and rat portal vein (RPV). The selectivity for the different receptors has been studied by utilizing atropine‐treated guinea pig ileum (GPI + At). The results showed that both analogues are mainly active on GPI through the NK‐1 receptor and that both analogues are equipotent to Substance P.
KW - guinea pig ileum assay
KW - methionine replacement
KW - NK‐1 receptor
KW - Substance P
KW - Substance P C‐terminal analogues
UR - http://www.scopus.com/inward/record.url?scp=0025980085&partnerID=8YFLogxK
U2 - 10.1111/j.1399-3011.1991.tb00268.x
DO - 10.1111/j.1399-3011.1991.tb00268.x
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C2 - 1714423
AN - SCOPUS:0025980085
SN - 0367-8377
VL - 37
SP - 180
EP - 184
JO - International Journal of Peptide and Protein Research
JF - International Journal of Peptide and Protein Research
IS - 3
ER -