Synthesis and biological activity of substance P C-terminal hexapeptide and heptapeptide analogues.
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.
Stavropoulos
G
G
Department of Chemistry, University of Patras, Greece.
Karagiannis
K
K
Cordopatis
P
P
Halle
D
D
Gilon
C
C
Bar-Akiva
G
G
Selinger
Z
Z
Chorev
M
M
D000595:Amino Acid Sequence; D000818:Animals; D006168:Guinea Pigs; D007082:Ileum / Q000378:metabolism; D066298:In Vitro Techniques; D008297:Male; D008969:Molecular Sequence Data; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D010446:Peptide Fragments / Q000138:chemical synthesis* / Q000494:pharmacology; D011169:Portal Vein / Q000378:metabolism; D011761:Pyrrolidonecarboxylic Acid / Q000031:analogs & derivatives; D051381:Rats; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter / Q000187:drug effects; D013373:Substance P / Q000138:chemical synthesis* / Q000494:pharmacology; D014649:Vas Deferens / Q000378:metabolism
D010446:Peptide Fragments; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter; D013373:Substance P; C032292:substance P (6-11); C031661:substance P (5-11); D011761:Pyrrolidonecarboxylic Acid