PMID- 6188072 OWN - NLM STAT- MEDLINE DCOM- 19830527 LR - 20190726 IS - 0028-3908 (Print) IS - 0028-3908 (Linking) VI - 22 IP - 2 DP - 1983 Feb TI - Structure-activity relationship in the mast cell degranulating capacity of neurotensin fragments. PG - 197-201 AB - The mast cell degranulating capacity of neurotensin and three of its fragments was examined. In Tyrode solution (137 mM NaCl, 2.7 mM KCl, 0.4 mM NaH2PO4, 1.4 mM CaCl2, 1 mM MgCl2, 10 mM Hepes, 5.6 mM glucose, pH 7.4), neither intact neurotensin nor its C-terminal tripeptide (Tyr-Ile-Leu) caused any release of histamine. Concentrations of neurotensin exceeding 10(-4)M did cause histamine release but through lysis of the cells. The C-terminal hexa- and octapeptides of neurotensin (Arg-Arg-Pro-Tyr-Ile-Leu and Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu, respectively) induced a non-cytolytic release of histamine with the latter peptide being more active (ED50 = 90 microM for the hexapeptide and 13 microM for the octapeptide). This release was not affected by the C-terminal tripeptide. It was found to be calcium-dependent and was inhibited by the anti-allergic drug, disodium cromoglycate. Phosphatidylserine did not enhance release of histamine and saturation of the immunoglobulin E (IgE) receptors did not inhibit it. FAU - Sagi-Eisenberg, R AU - Sagi-Eisenberg R FAU - Ben-Neriah, Z AU - Ben-Neriah Z FAU - Pecht, I AU - Pecht I FAU - Terry, S AU - Terry S FAU - Blumberg, S AU - Blumberg S LA - eng PT - Journal Article PL - England TA - Neuropharmacology JT - Neuropharmacology JID - 0236217 RN - 0 (Peptide Fragments) RN - 0 (Phosphatidylserines) RN - 37341-29-0 (Immunoglobulin E) RN - 39379-15-2 (Neurotensin) RN - EC 1.1.1.27 (L-Lactate Dehydrogenase) RN - SY7Q814VUP (Calcium) SB - IM MH - Animals MH - Calcium/physiology MH - Cytoplasmic Granules/*drug effects MH - Histamine Release/drug effects MH - Immunoglobulin E/pharmacology MH - In Vitro Techniques MH - L-Lactate Dehydrogenase/metabolism MH - Male MH - Mast Cells/*ultrastructure MH - Neurotensin/*analogs & derivatives/pharmacology MH - Peptide Fragments/pharmacology MH - Phosphatidylserines/pharmacology MH - Rats MH - Rats, Inbred Strains MH - Structure-Activity Relationship EDAT- 1983/02/01 00:00 MHDA- 1983/02/01 00:01 CRDT- 1983/02/01 00:00 PHST- 1983/02/01 00:00 [pubmed] PHST- 1983/02/01 00:01 [medline] PHST- 1983/02/01 00:00 [entrez] AID - 10.1016/0028-3908(83)90009-6 [doi] PST - ppublish SO - Neuropharmacology. 1983 Feb;22(2):197-201. doi: 10.1016/0028-3908(83)90009-6.