Abstract
Arodyn (aromatic dynorphin) is a novel analogue of the opioid peptide dynorphin A with a nonbasic N-terminus that exhibits nanomolar affinity (K(i) = 10 nM) and remarkable selectivity for kappa opioid receptors (K(i) ratio (kappa/mu/delta) = 1/174/583). Arodyn completely reverses the agonism of dynorphin A (1-13)NH(2) in a concentration-dependent manner in the adenylyl cyclase assay. Thus arodyn is a novel kappa opioid receptor selective antagonist that will be useful to study these receptors.
Publication types
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Adenylyl Cyclases / metabolism
-
Amino Acid Sequence
-
Animals
-
CHO Cells
-
Cricetinae
-
Dynorphins / chemical synthesis*
-
Dynorphins / chemistry
-
Dynorphins / pharmacology
-
Peptide Fragments / chemical synthesis*
-
Peptide Fragments / chemistry
-
Peptide Fragments / pharmacology
-
Radioligand Assay
-
Receptors, Opioid, kappa / antagonists & inhibitors*
-
Structure-Activity Relationship
Substances
-
Peptide Fragments
-
Receptors, Opioid, kappa
-
arodyn
-
Dynorphins
-
dynorphin (1-11)
-
Adenylyl Cyclases