125I-DPDYN, monoiodo [D-Pro10]- dynorphin (1-11), is an effective and useful tool for the study of kappa opioid receptors.
Iodination of the kappa-selective peptide DPDYN, [D-Pro10]-dynorphin (1-11), has been performed. The non radioactive monoiodo derivative of DPDYN retains kappa-selectivity (kappa/mu = 48 and kappa/delta = 140), despite a general but moderate decrease in affinity. Radioiodination of DPDYN leads to the monoiodinated peptide (S.A 700-800 Ci/mmol) which interacts specifically and reversibly with the kappa-sites in guinea-pig cerebellum membranes with high affinity (KD = 0.12-0.18 nM). In guinea-pig brain (mu-delta-kappa) and rabbit cerebellum (kappa much less than mu), 125I-DPDYN discriminates between kappa- and other (mu, delta) binding sites. We have used this new labelled probe for the direct, precise and rapid (exposure time less than 100 hours) visualization of kappa-sites in guinea-pig and rabbit cerebellar slices using autoradiography.
D000818:Animals; D002462:Cell Membrane / Q000378:metabolism; D002531:Cerebellum / Q000378:metabolism*; D004399:Dynorphins / Q000031:analogs & derivatives* / Q000378:metabolism; D006168:Guinea Pigs; D007457:Iodine Radioisotopes; D007700:Kinetics; D010446:Peptide Fragments / Q000378:metabolism*; D011957:Receptors, Opioid / Q000378:metabolism*; D017473:Receptors, Opioid, kappa
D007457:Iodine Radioisotopes; D010446:Peptide Fragments; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D004399:Dynorphins; C044619:dynorphin (1-11), Pro(10)-