Synthesis and biological activity of Substance P <i>C</i>‐terminal hexapeptide and heptapeptide analogues

Wiley - Tập 37 Số 3 - Trang 180-184 - 1991
George Stavropoulos1, KOSTAS KARAGIANNIS1, Paul Cordopatis2, David Halle3, Chaim Gilon4, Giora Bar-Akiva3, Zvi Selinger3, Michael Chorev5
1Department of Chemistry, University of Patras, Patras, Greece
2Department of Pharmacy, University of Patras, Patras, Greece
3Department of Biological, The Hebrew University of Jerusalem, Jerusalem, Israel
4Department of Organic, The Hebrew University of Jerusalem, Jerusalem, Israel
5Department of Pharmaceutical Chemistry, The Hebrew University of Jerusalem, Jerusalem, Israel

Tóm tắt

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.

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Wiley

Tập 37 Số 3

180-184

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