Abstract
The properties of the pituitary adenylate cyclase activating polypeptide (PACAP) type I receptor were studied on a clone of Chinese hamster ovary cells (CHO) stably transfected with the recombinant receptor. PACAP(1-27), PACAP(1-38) and VIP inhibited [125I-acetyl-His1]PACAP (1-27) binding, stimulated cyclic AMP and inositol phosphates production and induced [Ca2+]i increase with the same order of potency: PACAP(1-27) = PACAP(1-38) > VIP. The concentrations required for half maximal receptor occupancy, IP3- and [Ca2+]i increase were not different for both PACAPs (1 nM) and 100-fold higher than those required for cyclic AMP increase (0.010 nM). These data suggest that the occupancy of a portion of the total receptors available was sufficient for maximal cyclic AMP production but not for maximal IP3 production. It is concluded that the possibility of the type I PACAP receptor being coupled to a transduction pathway is not located at the level of the ligand but rather at the level of the G-proteins.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Adenylyl Cyclases / drug effects*
-
Animals
-
CHO Cells / drug effects
-
CHO Cells / metabolism
-
Calcium / metabolism
-
Cricetinae
-
Cyclic AMP / metabolism
-
Enzyme Activation / drug effects
-
GTP-Binding Proteins / physiology
-
Ligands
-
Neuropeptides / pharmacology*
-
Pituitary Adenylate Cyclase-Activating Polypeptide
-
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
-
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I
-
Receptors, Pituitary Hormone / classification
-
Receptors, Pituitary Hormone / genetics
-
Receptors, Pituitary Hormone / metabolism*
-
Recombinant Fusion Proteins / metabolism
-
Signal Transduction / drug effects
-
Transfection
-
Vasoactive Intestinal Peptide / pharmacology*
Substances
-
Ligands
-
Neuropeptides
-
Pituitary Adenylate Cyclase-Activating Polypeptide
-
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
-
Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide, Type I
-
Receptors, Pituitary Hormone
-
Recombinant Fusion Proteins
-
Vasoactive Intestinal Peptide
-
Cyclic AMP
-
GTP-Binding Proteins
-
Adenylyl Cyclases
-
Calcium