(N-stearyl, Norleucine17)VIPhybrid is a broad spectrum vasoactive intestinal peptide receptor antagonist

Terry W. Moody, Robert T. Jensen, Mati Fridkin, Illana Gozes

Research output: Contribution to journalArticlepeer-review

Abstract

The effects of a (N-stearyl, Norleucine17) vasoactive intestinal peptide hybrid ((SN)VIPhybrid) on cells stably transfected with VPAC1, VPAC2, or PAC1 receptors were investigated. (SN)VIPhybrid inhibited specific 125I-VIP binding to membranes derived from CHO cells transfected with VPAC1 or VPAC2 receptors with high affinity (IC50 = 30 and 50 nM). (SN)VIPhyb inhibited specific 125I-PACAP-27 binding to membranes derived from NIH/3T3 cells transfected with PAC1 receptors with high affinity (IC50 = 65 nM). PACAP-27 caused cAMP elevation in NIH/3T3 cells transfected with PAC1 receptors and the increase cAMP caused by pituitary adenylated cyclase (PACAP) was inhibited by (SN)VIPhyb. Also, the increase in cAMP caused by VIP using CHO cells transfected with VPAC1 or VPAC2 receptors was antagonized by (SN)VIPhyb. These results indicate that (SN)VIPhyb is an antagonist for VPAC1, VPAC2, and PAC1 receptors.

Original languageEnglish
Pages (from-to)29-35
Number of pages7
JournalJournal of Molecular Neuroscience
Volume18
Issue number1-2
DOIs
StatePublished - 2002

Keywords

  • Antagonist
  • Binding
  • Cyclic AMP (cAMP)
  • PACAP receptors
  • VIP receptors

Fingerprint

Dive into the research topics of '(N-stearyl, Norleucine17)VIPhybrid is a broad spectrum vasoactive intestinal peptide receptor antagonist'. Together they form a unique fingerprint.

Cite this