WeightNameValue
1000 Titel
  • Structure activity studies of mast cell activation and hypotension induced by neuropeptide Y (NPY), centrally truncated and C-terminal NPY analogues
1000 Autor/in
  1. Cross, L.J. Mark |
  2. Beck-Sickinger, Annette G. |
  3. Bienert, Michael |
  4. Gaida, Wolfram |
  5. Jung, Günther |
  6. Krause, Ebehard |
  7. Ennis, Madeleine |
1000 Erscheinungsjahr 2012
1000 LeibnizOpen
1000 Publikationstyp
  1. Artikel |
1000 Online veröffentlicht
  • 2012-07-19
1000 Erschienen in
1000 Quellenangabe
  • 117(2): 325-332
1000 FRL-Sammlung
1000 Verlagsversion
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1909254/ |
  • http://doi.org/10.1111/j.1476-5381.1996.tb15194.x |
1000 Publikationsstatus
1000 Begutachtungsstatus
1000 Sprache der Publikation
1000 Abstract/Summary
  • 1. Neuropeptide-induced histamine release is thought to occur via receptor-independent mechanisms, with net charge and lipophilicity being important factors. 2. In this study, the histamine releasing ability of neuropeptide Y (NPY), two C-terminal segments of NPY and 13 centrally truncated NPY analogues was examined. These results were compared with the ability of the peptides to bind to the Y2 receptor in the rabbit kidney membrane model and with their hypotensive actions in the anaesthetized-rat model. 3. All analogues tested, with the exception of [Glu4,25,33,35]-NPY(1–4)-Ahx-(25–36) and [Asp4,25,33,35]NPY(1–4)-Ahx-(25–36) which were devoid of histamine releasing activity, evoked a dose-dependent histamine release but there were marked differences between the peptides. The native peptide was the least active. 4. Histamine release was not linked to the ability of the peptides to displace NPY from Y2 receptors. There was a statistical correlation between the hypotensive effects expressed as ED10 values (μmol kg−1, which induced a blood pressure decrease of 10 mmHg) and the EC25 for histamine release (r = 0.62, P = 0.04), although histamine release may not be the sole determinant of the alterations in blood pressure. 5. There was a strong negative correlation between EC25 for histamine release and net positive charge (r = −0.93, P = 5.7 × 10−7), i.e. increasing the net positive charge caused greater histamine release. However, there was a 12 fold difference in activity amongst the most positively charged analogues (+ 5). Helicity did not correlate with histamine releasing ability. 6. In the development of NPY-related drugs the avoidance of compounds with net positive charge is recommended.
1000 Sacherschließung
lokal histamine liberation
lokal structure-activity relationships
lokal neuropeptide Y
lokal anaesthetized rat
lokal Mast cells
1000 Fächerklassifikation (DDC)
1000 Liste der Beteiligten
  1. https://frl.publisso.de/adhoc/creator/Q3Jvc3MsIEwuSi4gTWFyaw==|https://frl.publisso.de/adhoc/creator/QmVjay1TaWNraW5nZXIsIEFubmV0dGUgRy4=|https://frl.publisso.de/adhoc/creator/QmllbmVydCwgTWljaGFlbA==|https://frl.publisso.de/adhoc/creator/R2FpZGEsIFdvbGZyYW0=|https://frl.publisso.de/adhoc/creator/SnVuZywgR8O8bnRoZXI=|https://frl.publisso.de/adhoc/creator/S3JhdXNlLCBFYmVoYXJk|https://frl.publisso.de/adhoc/creator/RW5uaXMsIE1hZGVsZWluZQ==
1000 Label
1000 Förderer
  1. Department of Education for Northern Ireland |
1000 Fördernummer
  1. -
1000 Förderprogramm
  1. -
1000 Förderung
  1. 1000 joinedFunding-child
    1000 Förderer Department of Education for Northern Ireland |
    1000 Förderprogramm -
    1000 Fördernummer -
1000 Objektart article
1000 Beschrieben durch
1000 @id frl:6405176.rdf
1000 Erstellt am 2017-10-25T13:36:38.380+0200
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1000 Bearbeitet von 288
1000 Zuletzt bearbeitet Wed Mar 31 07:47:26 CEST 2021
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1000 Vgl. frl:6405176
1000 Oai Id
  1. oai:frl.publisso.de:frl:6405176 |
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