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
Rok vydání:	1984
Předmět:	Residue (chemistry) Oxytocin Chemistry Stereochemistry In vivo medicine Liquid phase Biological activity General Chemistry Peptide hormone In vitro medicine.drug
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
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::e8cac6aef1aeb5e5da318b6837b5d131 https://doi.org/10.1135/cccc19842012 Zobrazit plný text záznamu