Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2

GK Tóth, K Bakos, B Penke, I Pávó, C Varga… - Bioorganic & medicinal …, 1999 - Elsevier
Analogues of oxytocin containing D-Trp, 2-amino-1, 2, 3, 4-tetrahydronaphthalene-1-
carboxylic acid (Atc) or 1, 2, 3, 4-tetrahydro-β-carboline-1-carboxylic acid (Car) with R or S …

Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban

M Manning, LL Cheng, S Stoev, NC Wo… - Journal of Peptide …, 2005 - Wiley Online Library
The peptide oxytocin (OT) antagonist atosiban, approved for tocolytic use in Europe (under
the tradename Tractocile), represents an important new therapeutic advance for the …

Introduction of a cis-Prolyl Mimic in Position 7 of the Peptide Hormone Oxytocin Does Not Result in Antagonistic Activity

A Wittelsberger, L Patiny, J Slaninova… - Journal of medicinal …, 2005 - ACS Publications
New insights into the structure− activity relationship of the peptide hormone oxytocin are
presented. Incorporation of the novel cis-prolyl mimic 2, 2-dimethyl-1, 3-thiazolidine-4 …

In vitro pharmacological profile of a novel structural class of oxytocin antagonists.

DJ Pettibone, BV Clineschmidt, EV Lis, DR Reiss… - … of Pharmacology and …, 1991 - ASPET
A number of structurally novel cyclic hexapeptides have been characterized as potent and
selective oxytocin (OT) antagonists in vitro. As a representative of this class of compounds, L …

Conformationally restricted analogs of oxytocin; stabilization of inhibitory conformation

M LEBL, P HILL, W KAZMIERSKI… - … Journal of Peptide …, 1990 - Wiley Online Library
Analogs of oxytocin containing tetrahydroisoquinoline carboxylic acid (Tic) of L or D
configuration in position 2 were synthesized and their biological activities were tested. Both …

Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7

M Fragiadaki, V Magafa, L Borovicková… - European journal of …, 2007 - Elsevier
We report the solid-phase synthesis and some pharmacological properties of twenty
oxytocin (OT) analogues. Basic modifications at position 7 (introduction of α-aminoisobutyric …

Design of novel bicyclic analogues derived from a potent oxytocin antagonist

G Flouret, O Chaloin, L Borovickova… - Journal of Peptide …, 2006 - Wiley Online Library
Eleven new analogues were synthesized by modification of the potent oxytocin antagonist
(OTA)(S) Pmp1, d‐Trp2, Pen6, Arg8‐Oxytocin, or PA (parent antagonist), in which (S) Pmp …

Synthetic antagonists of in vivo responses by the rat uterus to oxytocin

J Lowbridge, M Manning, J Seto, J Haldar… - Journal of Medicinal …, 1979 - ACS Publications
As part of a program in which we are attempting tosynthesize in vivo antagonists of oxytocin,
the following four analogues were synthesized and tested for antagonistic activitiesin rat …

Non-peptide oxytocin agonists

G Pitt, A Batt, R Haigh, A Penson, P Robson… - Bioorganic & medicinal …, 2004 - Elsevier
A library of compounds targeted to the vasopressin/oxytocin family of receptors was
screened for activity at a cloned human oxytocin receptor using a reporter gene assay …

Subtlety of the Structure− Affinity and Structure− Efficacy Relationships around a Nonpeptide Oxytocin Receptor Agonist

MC Frantz, J Rodrigo, L Boudier… - Journal of medicinal …, 2010 - ACS Publications
Very few nonpeptide oxytocin agonists have currently been reported, and none of them
seem suitable for the in vivo investigation of the oxytocin mediated functions. In an attempt to …