Oxytocin Agonists

OT receptor [38]. It was used therapeutically for the prevention of postpartum haemorrhage in the third stage of labour [39], and was shown to be better than oxytocin in prevention of uterine atony after Caesarean section [40].

NH,

cis and trans

nh2

h2n nh2

cis and trans h2n

3.1.2. Carba analogs

Recently, the synthesis, activity and stability of a series of analogues of oxytocin have been investigated [41,42]. In each case, the disulphide bridge was replaced with methylene or methine (olefinic) units in an effort to enhance the biological half-life of the analogues without compromising inherent activity. The cis-alkene 18 is a potent agonist (EC50 — 38 nM) that is ~ 10-fold less active than oxytocin, whereas the corresponding trans-alkene 19 and hydrogenated ethylene analogue 20 are both ~ 100-fold less active [41]. The analogue 21 as a 2:1 mixture of cis I trans isomers was 200-fold less active than oxytocin and has a greater half-life (8-11 min longer) than 1 when incubated in placental tissue from rats [42].

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