Pituitary adenylate cyclase-activating polypeptide (pacap)/vasoactive intestinal peptide (vip) receptor subtypes in rat tissues: Investigation of receptor binding, a. novel vip receptor antagonist and chemical cross-linking

Masahiko Sone, David M. Smith, Mohammad A. Ghatei, Illana Gozes, Douglas E. Brenneman, Mati Fridkin, Stephen R. Bloom

Research output: Contribution to journalArticlepeer-review

Abstract

Receptors for pituitary adenylate cyclase-activating polypeptide (PACAP) have been subdivided into type I. receptors and II receptors. Using rat brain stem as a tissue containing type I. receptors and rat lung as a tissue containing type II receptors, we investigated the binding of 125I-labelled PACAP, vasoactive intestinal peptide (VIP) and the related peptide, heloderrnin to these and, by chemical cross-linking, the relative molecular weight of the receptors. Type I. receptors showed an Mr of 58,000 and type II an Mr of 54,000. After deglycosylation type I. receptors showed an Mr of 49,000 and type II receptors an Mr of 41,000 demonstrating a high degree of glycosylation of both subtypes. This compares with the predicted (unglycosylated) Mrs of the recently cloned rat braintype I. receptor and rat lung type II receptor of 56,000 and49,000, respectively. We also studied a hybrid VIP receptor antagonist (VIP-neurotensin) and showed it was unable to displace 125I-PACAP from type I. receptors (Ki>10, µM) but was effective at type II receptors and propose that this peptide could be used to differentiate between PACAP effects at the two receptor subtypes.

Original languageEnglish
Pages (from-to)145-153
Number of pages9
JournalBiomedical Research
Volume15
Issue number3
DOIs
StatePublished - 1994

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