PubMed · 15425278
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A TZANCK, E SIDI, S MORRILL-DOBKEVITCH. [Crossed sensitization].. https://pubmed.ncbi.nlm.nih.gov/15425278/
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Use of excess quantity of additives such as 1-hydroxybenzotriazole, 1-hydroxy-7-azabenzotriazole, or 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine could retard carbodiimide-mediated peptide coupling or aminolysis of the active esters in organic solvents generally employed in peptide chemistry. Solubility test and infrared spectroscopic data suggested that the amine components interacted with the additives to form some aggregates, which were less reactive toward acylation. The use of 0.1 equimolar additives against carboxyl components or carbodiimides was advantageous for rapid and efficient coupling reaction, especially when the carboxyl components were amino acids carrying urethane type N-protecting groups.
Two somatostatin analogues, [(99m)Tc]Demotide and [(99m)Tc]Demotate 4, were compared with [(99m)Tc]Demotate 1, a previously reported somatostatin receptor subtype 2 (sst(2)) targeting tracer. Conjugates were prepared by coupling an open-chain tetraamine chelator to D-Phe(1) of [Tyr(3)]-octreotide or [Tyr(3)]-octreotate, respectively, via a p-benzylaminodiglycolic acid spacer adopting solid-phase peptide synthesis techniques. Peptide conjugates were collected in a highly pure form after chromatographic purification. Eventually, [(99m)Tc]Demotide and [(99m)Tc]Demotate 4 were obtained in approximately 1 Ci/micromol specific activity and >96% purity after labeling under alkaline conditions. Demotide and Demotate 4 exhibited similar high binding affinities for the sst(2) expressed in AR4-2J cells with IC(50) values 0.16 and 0.10 nM, respectively. The (radio)metallated analogues [(99m)Tc]Demotide and [(99m)Tc]Demotate 4 showed equally high affinities to the sst(2) during saturation binding assays in AR4-2J cell membranes (K(d)s 0.08 and 0.07 nM, respectively). During incubation at 37 degrees C with AR4-2J cells, the radiopeptides internalized effectively via a receptor-mediated process, with [(99m)Tc]Demotate 4 exhibiting a faster internalization rate than [(99m)Tc]Demotide. After injection in athymic mice bearing sst(2)-expressing AR4-2J tumors, the radiotracers showed high and specific uptake in the tumor (>25%ID/g at 1 h) and in the sst(2)-positive organs. However, both [(99m)Tc]Demotide and [(99m)Tc]Demotate 4 showed unfavorably higher background activity, especially in the abdomen, in comparison to [(99m)Tc]Demotate 1 and are, therefore, less suited than [(99m)Tc]Demotate 1 for sst(2)-targeted tumor imaging in man.
We report on a female patient with brachioradial pruritus, in whom the cause could be verified by purposeful diagnostics (e. g., MRI). The clinical symptoms with localized itching result from circumscribed nerve root compression and hyperexcitation of the nerve fibers. Under treatment with gabapentin, an anticonvulsant with a very good analgesic and good antipruritic effect, the itch ceased and the skin changes healed. This case shows that this special form of neuropathic itch requires targeted therapy, which apart from symptomatic treatment should primarily focus on remedying the cause, if feasible.