Gairin J E, Jomary C, Cros J, Meunier J C
Laboratoire de Pharmacologie et Toxicologie Fondamentales, CNRS, Toulouse, France.
NIDA Res Monogr. 1986;75:232-5.
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.
已对κ-选择性肽DPDYN，即[D-脯氨酸10]-强啡肽（1-11）进行了碘化。DPDYN的非放射性单碘衍生物保留了κ-选择性（κ/μ = 48，κ/δ = 140），尽管亲和力普遍但适度降低。DPDYN的放射性碘化产生了单碘化肽（比活700 - 800 Ci/mmol），其与豚鼠小脑膜中的κ-位点以高亲和力（KD = 0.12 - 0.18 nM）特异性且可逆地相互作用。在豚鼠脑（μ-δ-κ）和兔小脑（κ远小于μ）中，125I-DPDYN可区分κ-和其他（μ、δ）结合位点。我们已使用这种新的标记探针，通过放射自显影法对豚鼠和兔小脑切片中的κ-位点进行直接、精确且快速（曝光时间少于100小时）的可视化。
