ogues of 8-D-homoarginine vasopressin

ogues of 8-D-homoarginine vasopressin

Analogues of 8-D-homoarginine vasopressin were prepared with the general formula where X is L-O-methyltyrosine, L-p-ethylphenylalanine, D-p-ethylphenylalanine, L-p-methylphenylalanine or D-methylphenylalanine and R is cysteine or beta -mercaptopropionic acid. These vasopressin analogues exhibited an...

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Hauptverfasser: MALETINSKA, LENKA, VELEK, JIRI, LEBL, MICHAL, BARTH, TOMISLAV, SKOPKOVA, JANA, BLAHA, IVO, SLANINOVA, JIRINA, VILHARDT, HANS, PROCHAZKA, ZDENKO, ZERTOVA, MIROSLAVA
Format: Patent
Sprache:eng
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CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Zusammenfassung:Analogues of 8-D-homoarginine vasopressin were prepared with the general formula where X is L-O-methyltyrosine, L-p-ethylphenylalanine, D-p-ethylphenylalanine, L-p-methylphenylalanine or D-methylphenylalanine and R is cysteine or beta -mercaptopropionic acid. These vasopressin analogues exhibited an increased affinity to uterus receptors for oxytocin, where they acted as ocytocin antagonists. Moreover, the analogues of deamino vasopressin have a significantly reduced antidiuretic activity in comparison with [8-D-arginine]vasopressin. Analogues of 8-D-homoarginine vasopressin were prepared with the general formula where X is L-O-methyltyrosine, L-p-ethylphenylalanine, D-p-ethylphenylalanine, L-p-methylphenylalanine or D-methylphenylalanine and R is cysteine or beta -mercaptopropionic acid. These vasopressin analogues exhibited an increased affinity to uterus receptors for oxytocin, where they acted as ocytocin antagonists. Moreover, the analogues of deamino vasopressin have a significantly reduced antidiuretic activity in comparison with [8-D-arginine]vasopressin.