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Oxytocin, conformation-activity

We have extensively Investigated the conformation-activity relationships of oxytocin (H-C s-Tyr-Ile-Gln-Asn-C s-Pro-Leu-Gly-NH2) antagonists based on the antagonist [Pen ]-oxytocln (. . 2) ... [Pg.19]

Our approach to testing this hypothesis and developing oxytocin antagonists with prolonged In vivo activity has been to further restrict the conformations of side chain groups at positions believed to be Important for binding In the antagonist... [Pg.19]

The C-terminal tripeptide tail of oxytocin H-L-Pro-Leu-Gly-NH2 (melanocyte-stimulating hormone release inhibiting factor, MIF or melanostatin) is implicated as having a direct effect on the central nervous system. The ALeu analogue of melanostatin, [ALeu2-MIF] was prepared in view of the earlier work on the active conformation of melanostatin in which a (3-turn was implicated.11771 ALeu was prepared by the N-chlorination/dehydrochlorination reaction and then coupled with Boc-Pro-OH. [Pg.659]

Table 3. Conformational restrictions and structural features apparently related to antagonist activity in oxytocin analogs... [Pg.279]


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Active conformation

Active conformers

Conformer, active

Oxytocin

Oxytocin conformation

Oxytocine

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