Structural requirements for mast cell triggering by substance P-like peptides.
Experiments were based on the hypothesis that the histamine releasing action of substance P and some other neuropeptides is not due to the interaction of the neuropeptide with a specific membrane receptor. Rather, this may be a property of many amphiphilic compounds having a minimal number of positives charges and a hydrophobic chain which is not necessarily a peptide. According to this hypothesis, 18 substance P derivatives and fragments were synthesized and tested on rat and hamster peritoneal mast cells, among them five compounds which contain a non-peptide chain instead of the C-terminal substance P heptapeptide. The results are in accord with the above hypothesis.
Repke
H
H
Institute of Drug Research, Academy of Sciences of the GDR, Berlin.
Bienert
M
M
D000818:Animals; D006224:Cricetinae; D006636:Histamine Release / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D008407:Mast Cells / Q000187:drug effects* / Q000276:immunology; D009479:Neuropeptides / Q000494:pharmacology; D010446:Peptide Fragments / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013373:Substance P / Q000031:analogs & derivatives / Q000494:pharmacology*
D009479:Neuropeptides; D010446:Peptide Fragments; D013373:Substance P