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Receptor binding parameters and autoradiographic distribution of various opioid receptor sites have been investigated in normal human brain, post-mortem. [3H]DAGO, a highly selective mu ligand, binds to a single class of high affinity (Kd = 1.1 nM), low capacity (Bmax = 160 fmol/mg protein) sites in membrane preparations of frontal cortex. These sites show(More)
1. The autoradiographic distribution of kappa opioid receptor binding sites in human brain was examined using two radiolabeled probes, namely [3H]U69,593 and [3H]bremazocine. 2. [3H]U69,593 binding was performed in the absence of blockers for other sites, while [3H]bremazocine binding was investigated in the presence of saturating concentrations of mu and(More)
Our experiments focused on the examination of the distribution of mu opioid receptor binding sites in normal human brain using the highly selective ligand [3H]DAGO, in both membrane binding assay and in vitro receptor autoradiography. Mu opioid binding sites are very discretely distributed in human brain with high densities of sites found in the posterior(More)
In guinea-pig cerebellum, saturation studies reveal that the nonselective opioid [3H]ethylketazocine has a binding capacity (R) of 6.79 pmol/g tissue which is similar to the sum of the individual R values of the mu-, delta- and kappa 1-selective opioids. Conversely, the binding parameters of the nonselective opioid [3H]bremazocine are best-fitted to a(More)
[3H]U69,593 and [3H]ethylketazocine (mu + delta suppressed) binding was measured in homogenates of guinea-pig brain. Both ligands bind with high affinity to a single class of opioid sites. The relative equilibrium dissociation constant (KD) for [3H]U69,593 is 1.15 nM, while [3H]ethylketazocine has a KD value of 0.33 nM. Their respective maximum binding(More)
The presence of multiple opioid binding sites in human fetal brain at 20 weeks gestational age was determined using the following selective tritiated ligands: D-Ala2, N-MePhe4, Gly-ol5-enkephalin (DAGO) for the mu-type, D-Pen2, D-Pen5-enkephalin (DPDP) for the delta-type and U-69,593 for the kappa-type. [3H]DAGO and [3H]U-69,593 each bind to a single class(More)
The electrically-evoked contractions of the rat vas deferens were selectively inhibited by beta-endorphin, the preparation being much less sensitive to enkephalins and narcotic analgesic drugs. However, introduction of D-Ala in position 2 of [Leu]-enkephalin enhanced the activity of the opioid peptide to the order of that of beta-endorphin. It is concluded(More)
Somatostatin (SS) inhibits in a dose-dependent manner electrically evoked contractions in the rat vas deferens. This action was not modified by yohimbine, naloxone or a mixture of antagonists containing atropine, phentolamine, methysergide, burimamide, propranolol and indomethacin, but was markedly potentiated by reducing the Ca2+ concentration of the(More)
The existence of specific, high-affinity opioid binding sites was demonstrated in 21-week-old human fetuses with the use of tritiated etorphine, a non-selective opioid ligand. Binding capacities measured in the brain, the cerebellum and the spinal cord give values of 2.83, 3.71 and 5.42 pmol/g of tissue. Kd values do not vary from one region to the other(More)