Synthesis and properties of carba-6-analogues of oxytocin containing a deaminopenicillamine residue in position 1
Autor: | Jiřina Slaninová, Michal Lebl, Linda Servítová, Tomislav Barth, Pavel Hrbas |
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Rok vydání: | 1984 |
Předmět: | |
Zdroj: | Collection of Czechoslovak Chemical Communications. 49:2012-2023 |
ISSN: | 1212-6950 0010-0765 |
Popis: | A study was made of the influence of the so-called carba substitution of the disulphide bridge on the properties of inhibitors obtained by the introduction of deaminopenicillamine into position 1 of the oxytocin molecule. Two analogues - [dPen1]carba-6-oxytocin (Ia) and [dPen1, Tyr(Me)2]carba-6-oxytocin (Ib) were prepared and their biological activities were assayed. Compound Ia is a strong agonist in the uterotonic assay in vivo (280 I.U./mg) and a weak antagonistin the pressor assay. Compound Ib inhibited the utertonic activity of oxytocin in vitro (pA2 = 8.43) and in vivo (pA2 = 7.13) as well as the pressor action of lysine vasopressin (pA2 = 7.43). |
Databáze: | OpenAIRE |
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