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专利信息
专利号:EP-0412508-B1
优先权日:1989-08-07
标 题:Analogues of vasopressin, their preparation and pharmaceutical use
发明人:PROCHAZKA ZDENKO; BLAHA IVO; ZERTOVA MIROSLAVA; SLANINOVA JIRINA; VELEK JIRI; SKOPKOVA JANA; LEBL MICHAL; BARTH TOMISLAV; MALETINSKA LENKA; VILHARDT HANS
权利人:CESKOSLOVENSKA AKADEMIE VED
摘要:The invention relates to analogues of 8-D-homoarginine-vasopressin of the general formula in which the meanings are: X L-O-methyltyrosine L-p-ethylphenylalanine D-p-ethylphenylalanine L-p-methylphenylalanine or D-p-methylphenylalanine and R cysteine or beta -mercaptopropionic acid to a process for the preparation thereof by solid-phase synthesis and to the pharmaceutical use thereof. The analogues of vasopressin have a selectively increased affinity for uterine oxytocin receptors, where they have an antagonistic action to oxytocin. The analogues of deaminovasopressin furthermore have a significantly reduced antidiuretic activity compared with [8-D-arginine]-deaminovasopressin.