PACAP hybrid: A new PACAP receptor antagonist

J. R. Pisegna, J. Leyton, T. Coelho, T. Hida, S. Jakowlew, M. Birrer, M. Fridkin, I. Gozes, T. W. Moody

Research output: Contribution to journalArticlepeer-review

Abstract

The effects of pituitary adenylate cyclase activating polypeptide (PACAP) hybrid, a synthetic antagonist, was investigated on NIH/3T3 cells containing PACAP receptor (R) splice variants (SVs). PACAPhybrid inhibited 125I-PACAP-27 binding to NIH/3T3 cells stably expressing PACAP-R basic, SV-1, SV-2 or SV-3 with an IC50 of 1000 nM. PACAPhybrid antagonized the ability of PACAP-27 to elevate cAMP regardless of the PACAP-R SV used. PACAP was more efficacious at increasing cytosolic Ca2+ in NIH/3T3 cells containing PACAP-R SV-2 than PACAP-R basic, SV-1 or SV-3. PACAPhybrid antagonized the increase in cytosolic Ca2+ caused by PACAP-27 regardless of the PACAP-R SV used. PACAP was more potent at elevating c-fos mRNA using NIH/3T3 cells transfected with PACAP-R SV-2 than PACAP-R basic, SV-1 or SV-3. PACAPhybrid antagonized the increase in c-fos mRNA caused by PACAP-27. These data suggest that PACAPhybrid is a useful PACAP receptor antagonist for PACAP-R SVs.

Original languageEnglish
Pages (from-to)631-639
Number of pages9
JournalLife Sciences
Volume61
Issue number6
DOIs
StatePublished - 3 Jul 1997

Keywords

  • PACAP
  • PACAP antagonist
  • Receptor
  • Splice variants

Fingerprint

Dive into the research topics of 'PACAP hybrid: A new PACAP receptor antagonist'. Together they form a unique fingerprint.

Cite this