The analogs of oxytocin and D-homoarginine vasopressin with bulky substituted phenylalanine in position 2 |
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Authors: | Zdenko Prochá zka, Miroslava ertová Jiina Slaninová |
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Affiliation: | (1) Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Flemingovo nám. 2, 166 10 Prague 6, The Czech Republic |
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Abstract: | Solid phase technique on p-methylbenzhydrylamine resin wasused for the synthesis of eight analogs of oxytocin and 8-D-homoarginine vasopressin with the non-coded amino acids L- or D-2,3,4,5,6-pentamethylphenylalanine and L- or D-4-phenylphenylalanine in position 2. The preparation of theabove mentioned non-coded amino acids is described as well.All eight analogs were found to be potent inhibitors ofoxytocin activity in the uterotonic in vitro test in theabsence of Mg2+ ions. In the uterotonic test invitro in the presence of Mg2+ and in the test invivo, their potency is strongly decreased or completelyabolished. The substances are also weak pressor inhibitors.The L or D configuration does not seem to influence theactivity significantly. |
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Keywords: | antagonists hormones peptides andpolypeptides solid phase synthesis |
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