Enkephalin. Synthesis of two pentapeptides isolated from porcine brain with receptor-mediated opiate agonist activity.
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Biomedical subjects
Publications and source records attributed to J D Bower.
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Syntheses of the decapeptide luteinizing hormone-releasing hormone, less thanGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2 are described. The basic properties of arginine can provide a simple repetitive isolation procedure for arginine-containing peptides. The biological activities of the decapeptide, of a range of fragments and modified fragments, and of two analogs with alteration in the series at position 4 were measured by in vitro incubation with sheep pituitary slices, measuring the liberated LH by bioassay. None of the compounds of shortened sequence were active, with the exception of less thanGlu-His-Trp which showed 1% of the decapeptide in one of four experiments. Neither [Ser(But)4]-LH-RH-nor [Leu4]-LH-RH showed significant activity indicating (despite the known activity of [Ala4]-LH-RH) the importance of this part of the structure for full biological activity.
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The serum half-life of tobramycin was found to be the same as that of gentamicin in patients with similar renal function. The values ranged from 2 hr in normal volunteers to 53.4 hr in anephric patients. Both drugs were readily removed from the serum by the Kiil artificial kidney, with a 70% reduction in serum concentrations during a 12-hr dialysis period.
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