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The anatomical localization of nociceptin receptors was examined by in vitro quantitative autoradiography techniques in rat spinal cord sections by using [(125)I-Tyr(14)]nociceptin. [(125)I-Tyr(14)]nociceptin appeared to interact with a single class of binding sites (K(D)=0.1 nM) present in the grey matter in all laminae of the spinal cord from cervical to(More)
A structure-activity study was carried out to determine the importance of the C-terminal amino acids of the octapeptide Neuropeptide FF (NPFF) in binding and agonistic activity. Affinities of NPFF analogues were tested toward NPFF receptors of the rat spinal cord and the human NPFF2 receptors transfected in CHO cells. The activities of these analogues were(More)
[123I]iodomorphine (IMPH) was administered intracerebroventriculary (i.c.v.) in eight patients treated by i.c.v. morphinotherapy (i.c.v.m.). Scans obtained by gamma-scintigraphy over 1 h post-injection showed only a slight diffusion of IMPH beyond the ventricular system, particular attention being paid to the spinal cord. These data agree well with induced(More)
The binding properties of neuropeptide FF (NPFF) receptors were investigated in different laminae of the rat spinal cord by using quantitative autoradiography and [125I][D.Tyr1, (NMe)Phe3]NPFF as radioligand. In the superficial layers, the specific binding of [125I][D.Tyr1, (NMe)Phe3]NPFF was time-dependent, reversible, and saturable (KD = 0.1 nM).(More)
During striatal development, dopamine afferents initially reach the striosomal compartment, and this early dopamine innervation is thought to influence, through the D1 receptors first expressed in the developing patches, the phenotype of target striatal cells. Dopaminergic control of gene expression during ontogeny could be mediated by transcription factors(More)
Three unsaturated Schiff base tetradentate (N2S2 or N2SO) ligands were synthesized and characterized. Oxo and nitrido 99m-technetium complexes were obtained with these ligands. The nitrido complexes were formed using a new easy method available as a kit. When injected into rats and mice, these lipophilic complexes were able to cross the blood-brain barrier(More)
Several high-affinity analogs of neuropeptide FF (Phe-Leu-Phe-Gln-Pro-Gln-Arg-Phe-NH2, NPFF) exhibiting both supraspinal anti-opioid and spinal analgesic activities were studied for their abilities to interact with specific mu, delta, and kappa opioid binding in the rat spinal cord. Measurements by quantitative receptor autoradiography in the superficial(More)
The distribution and quantification of opioid receptor types in post-mortem human pituitary cryostat sections was determined by quantitative in vitro receptor autoradiography. Highly specific radioligands were used for each opioid receptor type i.e. [125l]-FK-33-824 for mu-opioid sites, [125l][D.Ala2]-Deltorphin-l for delta-opioid sites and 3H-U69,593 for(More)
In France, radiopharmaceuticals have been considered as drugs since 1992. Few adverse reactions with radiopharmaceuticals were described in the literature. Some authors have reported a rate of 1 to 6 reactions per 100,000 injections. The purpose of the present study was to evaluate the prevalence of radiopharmaceutical-induced side effects. A prospective(More)
The distribution of delta-opioid binding sites was studied by quantitative autoradiography in rat brain and spinal cord using the highly selective ligand [125I][D.Ala2]deltorphin-I. The binding properties of [125I][D.Ala2]deltorphin-I were investigated by microdensitometry of autoradiographic films with the aid of a computer-assisted image-analysis system.(More)