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1. Full Text Oral oxytocin antagonists
by Borthwick, Alan D
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2010, Volume 53, Issue 18, pp. 6525 - 6538
SELECTIVE ANTAGONISTS | POTENT | CHEMISTRY, MEDICINAL | RECEPTOR ANTAGONISTS | 2,5-DIKETOPIPERAZINES | LIGANDS | BENZOFURAN DERIVATIVES | VASOPRESSIN | IDENTIFICATION | PRETERM LABOR | DISCOVERY | Receptors, Oxytocin - physiology | Oxytocin - antagonists & inhibitors | Piperidines - chemistry | Sulfonamides - chemistry | Administration, Oral | Triazoles - chemistry | Humans | Biological Availability | Piperazines - chemistry | Sulfonamides - pharmacology | Piperazines - pharmacology | Pyrrolidines - chemistry | Receptors, Oxytocin - chemistry | Pyrrolidines - pharmacology | Triazoles - pharmacology | Camphor - analogs & derivatives | Animals | Piperidines - pharmacology | Indoles - pharmacology | Protein Conformation | Camphor - pharmacology | Indoles - chemistry | Oxytocin - chemistry | Camphor - chemistry
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2. Full Text Oxytocin receptor antagonists for inhibiting preterm labour
by Flenady, Vicki and Flenady, Vicki and Reinebrant, Hanna E and Reinebrant, Hanna E and Liley, Helen G and Liley, Helen G and Tambimuttu, Eashan G and Tambimuttu, Eashan G and Papatsonis, Dimitri N. M and Papatsonis, Dimitri N.M
The Cochrane database of systematic reviews, ISSN 1469-493X, 2014, Volume 6, Issue 6, p. CD004452
Background Preterm birth, defined as birth between 20 and 36 completed weeks, is a major contributor to perinatal morbidity and mortality globally. Oxytocin... 
SYSTEMATIC ANALYSIS | Humans | ATOSIBAN | Premature [drug therapy] | RANDOMIZED-TRIAL | Ritodrine [therapeutic use] | Tocolytic Agents [therapeutic use] | TIME TRENDS | Randomized Controlled Trials as Topic | Receptors, Oxytocin [antagonists & inhibitors] | Pregnancy | Terbutaline [therapeutic use] | MEDICINE, GENERAL & INTERNAL | Vasotocin [adverse effects, analogs & derivatives; therapeutic use] | Albuterol [therapeutic use] | ACUTE TOCOLYSIS | Obstetric Labor | NIFEDIPINE | DOUBLE-BLIND | Female | HEART-RATE | BIRTH | EPIDEMIOLOGY | Infant, Extremely Low Birth Weight | Terbutaline - therapeutic use | Receptors, Oxytocin - antagonists & inhibitors | Vasotocin - therapeutic use | Vasotocin - analogs & derivatives | Oligopeptides - therapeutic use | Ritodrine - therapeutic use | Tocolytic Agents - therapeutic use | Obstetric Labor, Premature - drug therapy | Albuterol - therapeutic use | Infant, Newborn
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3. Full Text In silico profiling the interaction mechanism of 2,5-diketopiperazine derivatives as oxytocin antagonists
by Yang, Ming and Yang, Ling and Luo, Jianghe and Zeng, Zhumei and Xu, Limian and Li, Yan
Journal of Molecular Graphics and Modelling, ISSN 1093-3263, 06/2019, Volume 89, pp. 178 - 191
Oxytocin plays a vital role in the occurrence of preterm birth by interacting with oxytocin receptor (OTR), and thus OTR antagonists provide effective... 
3D-QSAR | Premature labour | Oxytocin receptor | 2,5-diketopiperazine derivatives | Molecular docking | CoMSIA | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | BIOCHEMICAL RESEARCH METHODS | RECEPTOR | PRETERM INFANTS | CRYSTALLOGRAPHY | ITERATIVE PARTIAL EQUALIZATION | POTENT | COMPUTER SCIENCE, INTERDISCIPLINARY APPLICATIONS | PHARMACOKINETICS | MATHEMATICAL & COMPUTATIONAL BIOLOGY | VASOPRESSIN | RHODOPSIN | SCORING FUNCTIONS | Molecular dynamics | Amino acids | Derivatives (Financial instruments) | Obstetrics | Analysis
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4. Full Text Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: Synthesis, pharmacokinetics, and in vivo potency
by Borthwick, Alan D and Liddle, John and Davies, Dave E and Exall, Anne M and Hamlett, Christopher and Hickey, Deirdre M and Mason, Andrew M and Smith, Ian E. D and Nerozzi, Fabrizio and Peace, Simon and Pollard, Derek and Sollis, Steve L and Allen, Michael J and Woollard, Patrick M and Pullen, Mark A and Westfall, Timothy D and Stanislaus, Dinesh J
Journal of Medicinal Chemistry, ISSN 0022-2623, 01/2012, Volume 55, Issue 2, pp. 783 - 796
A six-stage stereoselective synthesis of indanyl-7-(3'-pyridyl)-(3R,6R,7R)-2,5-diketopiperazines oxytocin antagonists from indene is described. SAR studies... 
DESIGN | CHEMISTRY, MEDICINAL | 2,5-DIKETOPIPERAZINES | 1,3-DIPOLAR CYCLOADDITION | OCTANOL/WATER | IDENTIFICATION | DERIVATIVES | LABOR | Cytochrome P-450 Enzyme Inhibitors | Diketopiperazines - administration & dosage | Stereoisomerism | Humans | Microsomes, Liver - metabolism | Macaca fascicularis | Biological Availability | Male | Structure-Activity Relationship | Oxytocin - metabolism | Female | Radioligand Assay | Morpholines - chemical synthesis | Administration, Oral | Receptors, Oxytocin - antagonists & inhibitors | Morpholines - administration & dosage | Solubility | Rats | Diketopiperazines - pharmacology | Rats, Sprague-Dawley | Animals | Diketopiperazines - pharmacokinetics | Dogs | Morpholines - pharmacokinetics | Diketopiperazines - chemical synthesis | In Vitro Techniques
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5. Full Text Maintenance therapy with oxytocin antagonists for inhibiting preterm birth after threatened preterm labour
by Papatsonis, Dimitri N.M and Papatsonis, Dimitri N M and Flenady, Vicki and Flenady, Vicki and Liley, Helen G and Liley, Helen G
The Cochrane database of systematic reviews, ISSN 1469-493X, 2013, Volume 10, Issue 10, p. CD005938
Background In some women, an episode of preterm labour settles and does not result in immediate preterm birth. Subsequent treatment with tocolytic agents such... 
Obstetric Labor, Premature [prevention & control] | Humans | Vasotocin [analogs & derivatives; therapeutic use] | Tocolytic Agents [therapeutic use] | Randomized Controlled Trials as Topic | Receptors, Oxytocin [antagonists & inhibitors] | Pregnancy | MEDICINE, GENERAL & INTERNAL | Female | Premature Birth [prevention & control] | OUTCOMES | WEIGHT | EPIDEMIOLOGY | Tocolytic Agents - therapeutic use | Receptors, Oxytocin - antagonists & inhibitors | Vasotocin - therapeutic use | Premature Birth - prevention & control | Obstetric Labor, Premature - prevention & control | Vasotocin - analogs & derivatives
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6. Full Text The discovery of GSK221149A: A potent and selective oxytocin antagonist
by Liddle, John and Allen, Michael J and Borthwick, Alan D and Brooks, David P and Davies, David E and Edwards, Richard M and Exall, Anne M and Hamlett, Chris and Irving, Wendy R and Mason, Andrew M and McCafferty, Gerald P and Nerozzi, Fabrizio and Peace, Simon and Philp, Joanne and Pollard, Derek and Pullen, Mark A and Shabbir, Shaila S and Sollis, Steve L and Westfall, Timothy D and Woollard, Pat M and Wu, Charlene and Hickey, Deirdre M.B
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2008, Volume 18, Issue 1, pp. 90 - 94
Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has... 
Diketopiperazine | Labour | Oxytocin | Tocolytic | oxytocin | CHEMISTRY, MEDICINAL | 2,5-DIKETOPIPERAZINES | diketopiperazine | tocolytic | OCTANOL/WATER | CHEMISTRY, ORGANIC | RECEPTORS | LABOR | labour | Oxytocin - antagonists & inhibitors | Humans | Rats | Piperazines - chemistry | Structure-Activity Relationship | Oxytocin - metabolism | Piperazines - pharmacology | Rats, Sprague-Dawley | Uterine Contraction - drug effects | Receptors, Oxytocin - metabolism | Animals | Female | Kinetics | Piperazines - pharmacokinetics
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7. Full Text Treatment with oxytocin antagonists before embryo transfer may increase implantation rates after IVF
by Moraloglu, Ozlem and Tonguc, Esra and Var, Turgut and Zeyrek, Tugba and Batıoglu, Sertac
Reproductive BioMedicine Online, ISSN 1472-6483, 2010, Volume 21, Issue 3, pp. 338 - 343
Abstract This report aimed to examine the effects of atosiban on pregnancy outcome after IVF–embryo transfer. A prospective, randomized, placebo-controlled... 
Obstetrics and Gynecology | atosiban | uterine contractility | miscarriage rate | clinical pregnancy rate | implantation rate | IVF–embryo transfer | IVF-embryo transfer | MENSTRUAL-CYCLE | UTERINE CONTRACTIONS | DYSMENORRHEA | PRETERM LABOR | RECEPTOR ANTAGONIST | OBSTETRICS & GYNECOLOGY | WOMEN | REPRODUCTIVE BIOLOGY | PREGNANCY RATES | VASOPRESSIN | IN-VITRO FERTILIZATION | Oxytocin - antagonists & inhibitors | Embryo Implantation - drug effects | Prospective Studies | Humans | Male | Vasotocin - therapeutic use | Case-Control Studies | Hormone Antagonists - administration & dosage | Vasotocin - analogs & derivatives | Pregnancy | Young Adult | Sperm Injections, Intracytoplasmic | Fertilization in Vitro | Embryo Transfer | Adult | Female | Vasotocin - administration & dosage | Hormone Antagonists - therapeutic use | Infant, Newborn | Pregnancy Outcome
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8. Full Text The design of orally bioavailable 2, 5‐diketopiperazine oxytocin antagonists: from concept to clinical candidate for premature labor
by Borthwick, Alan D and Liddle, John
Medicinal Research Reviews, ISSN 0198-6325, 07/2011, Volume 31, Issue 4, pp. 576 - 604
A short, efficient and highly stereoselective synthesis has been developed for a series of 6‐indanyl‐3‐alkyl‐7‐aryl/heterocyclic‐(3R, 6R, 7R)‐2,... 
oxytocin antagonist | preterm labor | retosiban | diketopiperazines | GSK221149A | Preterm labor | Oxytocin antagonist | Diketopiperazines | Retosiban | CHEMISTRY, MEDICINAL | RECEPTOR | IDENTIFICATION | DISCOVERY | POTENT | 2,5-DIKETOPIPERAZINES | PHARMACOKINETICS | HUMAN INTESTINAL-ABSORPTION | VASOPRESSIN | PHARMACOLOGY & PHARMACY | EPIDEMIOLOGY | Oxytocin - antagonists & inhibitors | Diketopiperazines - administration & dosage | Administration, Oral | Diketopiperazines - chemistry | Diketopiperazines - therapeutic use | Humans | Biological Availability | Oxytocin - metabolism | Pregnancy | Obstetric Labor, Premature - drug therapy | Diketopiperazines - pharmacokinetics | Drug Design | Female
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9. Full Text Oxytocin antagonist disrupts male mouse medial amygdala response to chemical-communication signals
by Samuelsen, C.L and Meredith, M
Neuroscience, ISSN 0306-4522, 2011, Volume 180, pp. 96 - 104
Abstract The male mouse medial amygdala is an important site for integration of main and accessory olfactory information. Exposure to biologically relevant... 
Neurology | Pheromone | Behavior | Predator | Oxytocin | Olfaction | Immediate early gene | PREDATOR ODORS | oxytocin | DEFENSIVE BEHAVIORS | predator | INDIVIDUAL ODORS | FEMALE MICE | olfaction | VOMERONASAL ORGAN REMOVAL | KNOCKOUT MICE | NEUROSCIENCES | SOCIAL RECOGNITION | MATERNAL AGGRESSIVE-BEHAVIOR | OLFACTORY-BULB | ESTROGEN-RECEPTOR-ALPHA | immediate early gene | pheromone | behavior | Oxytocin - antagonists & inhibitors | Genes, Immediate-Early - physiology | Mice, Inbred C57BL | Amygdala - metabolism | Behavior, Animal - physiology | Male | Gene Expression Profiling | Animals | Social Behavior | Gene Expression - physiology | Female | Mice | Animal Communication | Immediate Early Gene (IEG)
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10. Full Text Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent
by Brown, T. Bruce and Brown, Alan and Calabrese, Andrew and Ellis, Dave and Puhalo, Nicholas and Ralph, Michael and Watson, Lesa
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2010, Volume 20, Issue 2, pp. 516 - 520
Several potent aryl ether/triazole Oxytocin antagonists are described. One of these compounds, , has excellent potency and selectivity, as well as promising in... 
Oxytocin | Medicinal chemistry | Antagonist | CHEMISTRY, ORGANIC | CHEMISTRY, MEDICINAL | Administration, Oral | Triazoles - chemistry | Humans | Microsomes, Liver - metabolism | Receptors, Vasopressin - metabolism | Rats | Azetidines - pharmacokinetics | Oxytocin - pharmacokinetics | Structure-Activity Relationship | Oxytocin - analogs & derivatives | Azetidines - chemistry | Animals | Dogs | Triazoles - chemical synthesis | Triazoles - pharmacokinetics | Azetidines - chemical synthesis | Antidiuretic Hormone Receptor Antagonists | Oxytocin - chemistry | Triazoles | Pituitary hormones
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11. The Oxytocin Antagonist Cligosiban Fails to Prolong Intravaginal Ejaculatory Latency in Men with Lifelong Premature Ejaculation: Results of a Randomized, Double-Blind, Placebo-Controlled Phase IIb trial (PEDRIX)
by Althof, S and Osterloh, IH and Muirhead, GJ and George, K and Girard, N and Jennings, W and Adams, M and Shockey, G and Kaminetsky, J and Miner, M and Belkoff, L and Gittelman, M and Goldstein, I and Reynolds, M and Severance, R and Kopp, J and Schumacher, D and White, C and Morgentaler, A and Rhee, M and Ellison, W and Francyk, D and Molin, C and Ervin, J and Efros, M and Altamirano, D and Noss, M and Croft, H and Miller, J and Church, P and Banov, M and Polepalle, S and Herman, C and Crocket, E and Rauzi, F and PEDRIX Multi-Ctr Study Grp and PEDRIX Multi-Centre Study Group
JOURNAL OF SEXUAL MEDICINE, ISSN 1743-6095, 08/2019, Volume 16, Issue 8, pp. 1188 - 1198
Introduction: Cligosiban is an orally administered, centrally penetrant oxytocin receptor antagonist being developed to treat premature ejaculation (PE). Aim:... 
Premature ejaculation | IX-01 | Cligosiban | UROLOGY & NEPHROLOGY | Efficacy | Oxytocin receptor antagonist | VALIDITY
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12. Oxytocin antagonists for the management of preterm birth: A review
by Usta, Ihab M and Khalil, Ali and Nassar, Anwar H
American Journal of Perinatology, ISSN 0735-1631, 2011, Volume 28, Issue 6, pp. 449 - 459
Preterm birth, the leading cause of neonatal morbidity and mortality, is estimated at incidence of 12.7% of all births, which has not decreased over the last... 
adverse effects | preterm labor | Oxytocin antagonists | dose | tocolysis | PROSPECTIVE RANDOMIZED-TRIAL | TERM PREGNANT-WOMEN | UTERINE CONTRACTIONS | ATOSIBAN | RECEPTOR ANTAGONIST | OBSTETRICS & GYNECOLOGY | ACUTE TOCOLYSIS | HUMAN-UTERUS | DOUBLE-BLIND | PEDIATRICS | CLINICAL-PRACTICE | LABOR | Sympathomimetics - therapeutic use | Oxytocin - antagonists & inhibitors | Humans | Vasotocin - therapeutic use | Vasotocin - pharmacokinetics | Hormone Antagonists - administration & dosage | Vasotocin - analogs & derivatives | Oligopeptides - therapeutic use | Pyrrolidines - therapeutic use | Tocolytic Agents - therapeutic use | Hormone Antagonists - pharmacokinetics | Tocolytic Agents - administration & dosage | Nifedipine - therapeutic use | Female | Indoles - therapeutic use | Vasotocin - administration & dosage | Hormone Antagonists - therapeutic use | Tocolytic Agents - pharmacokinetics | Premature Birth - prevention & control
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13. Full Text Oxytocin receptor antagonists for inhibiting preterm labour
by Papatsonis, D and Flenady, V and Cole, S and Liley, H
Cochrane database of systematic reviews (Online), ISSN 1469-493X, 2005, Issue 3, p. CD004452
Background Preterm birth, defined as birth before 37 completed weeks, is the single most important cause of perinatal mortality and morbidity in high-income... 
MORTALITY | CONTROLLED-TRIAL | MEDICINE, GENERAL & INTERNAL | METAANALYSIS | TOCOLYSIS | LOW-BIRTH-WEIGHT | ATOSIBAN | INFANTS | DOUBLE-BLIND | OUTCOMES | EPIDEMIOLOGY | Vasotocin - adverse effects | Terbutaline - therapeutic use | Receptors, Oxytocin - antagonists & inhibitors | Humans | Vasotocin - therapeutic use | Vasotocin - analogs & derivatives | Randomized Controlled Trials as Topic | Pregnancy | Ritodrine - therapeutic use | Tocolytic Agents - therapeutic use | Obstetric Labor, Premature - drug therapy | Albuterol - therapeutic use | Female
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14. Full Text Oxytocin antagonists
by Thornton, Steven and Vatish, Manu
Expert Opinion on Therapeutic Patents, ISSN 1354-3776, 09/2002, Volume 12, Issue 9, pp. 1403 - 1406
Preterm delivery is the single largest cause of perinatal mortality and morbidity. At present, there is no effective long-term treatment for uncomplicated... 
oxytocin (OT) | preterm labour | tocolysis | oxytocin antagonists | oxytocin receptor (OTR) | RITODRINE | MEDICINE, LEGAL | ATOSIBAN | MYOMETRIUM | GLYCERYL TRINITRATE | PRETERM LABOR | PHARMACOLOGY & PHARMACY | PARTURITION | RECEPTORS | Oxytocin receptor (OTR) | Oxytocin (OT) | Oxytocin antagonists | Preterm labour | Tocolysis
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15. Full Text 2,5-Diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency
by Borthwick, Alan D and Davies, Dave E and Exall, Anne M and Hatley, Richard J. D and Hughes, Jennifer A and Irving, Wendy R and Livermore, David G and Sollis, Steve L and Nerozzi, Fabrizio and Valko, Klara L and Allen, Michael J and Perren, Marion and Shabbir, Shalia S and Woollard, Patrick M and Price, Mark A
Journal of Medicinal Chemistry, ISSN 0022-2623, 07/2006, Volume 49, Issue 14, pp. 4159 - 4170
A short, efficient, and highly stereoselective synthesis of a series of (3R, 6R, 7R)-2,5-diketopiperazine oxytocin antagonists and their pharmacokinetics in... 
INTESTINAL-ABSORPTION | IDENTIFICATION | CHEMISTRY, MEDICINAL | Binding, Competitive | Indenes - pharmacology | Cricetinae | Oxytocin - pharmacology | Cricetulus | Indenes - chemical synthesis | Administration, Oral | Receptors, Oxytocin - antagonists & inhibitors | Stereoisomerism | Humans | Rats | Biological Availability | Structure-Activity Relationship | Piperazines - pharmacology | Uterine Contraction - drug effects | Indenes - pharmacokinetics | Animals | Calcium Signaling - drug effects | Dogs | Piperazines - chemical synthesis | Piperazines - pharmacokinetics | Radioligand Assay | Antidiuretic Hormone Receptor Antagonists | CHO Cells
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16. Full Text Maintenance therapy with oxytocin antagonists for inhibiting preterm birth after threatened preterm labour
by Papatsonis, Dimitri and Flenady, Vicki and Liley, Helen
Cochrane database of systematic reviews (Online), ISSN 1469-493X, 2009, Issue 1, p. CD005938
Background In some women, an episode of preterm labour settles and does not result in immediate preterm birth. Subsequent treatment with tocolytic agents such... 
Pregnancy | Premature birth [prevention & control] | Randomized controlled trials as topic | Humans | Receptors, oxytocin [antagonists & inhibitors] | Female | Tocolytic agents [therapeutic use] | Vasotocin [analogs & derivatives | Obstetric labor, premature [prevention & control] | Therapeutic use | MEDICINE, GENERAL & INTERNAL | OUTCOMES | WEIGHT | ECONOMIC CONSEQUENCES | EPIDEMIOLOGY | INFANTS | Tocolytic Agents - therapeutic use | Receptors, Oxytocin - antagonists & inhibitors | Vasotocin - therapeutic use | Premature Birth - prevention & control | Obstetric Labor, Premature - prevention & control | Vasotocin - analogs & derivatives | Randomized Controlled Trials as Topic
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17. Full Text Peripherally administered non-peptide oxytocin antagonist, L368,899 ®, accumulates in limbic brain areas: A new pharmacological tool for the study of social motivation in non-human primates
by Boccia, Maria L and Goursaud, Anne-Pierre S and Bachevalier, Jocelyne and Anderson, Kenneth D and Pedersen, Cort A
Hormones and Behavior, ISSN 0018-506X, 2007, Volume 52, Issue 3, pp. 344 - 351
Central administration of oxytocin (OT) antagonists inhibits maternal and sexual behavior in non-primates, providing the strongest experimental evidence that... 
Maternal behavior | Rhesus monkey | Oxytocin | Macaques | Sexual behavior | LOCALIZATION | oxytocin | ANXIETY | RATS | SEXUAL-BEHAVIOR | RECEPTOR | NEUROPEPTIDES | rhesus monkey | RESPONSES | sexual behavior | maternal behavior | ENDOCRINOLOGY & METABOLISM | BEHAVIORAL SCIENCES | macaques | BINDING-SITES | MONKEYS | EXPRESSION | Bornanes - blood | Oxytocin - antagonists & inhibitors | Frontal Lobe - metabolism | Amygdala - metabolism | Bornanes - pharmacology | Male | Septum of Brain - metabolism | Limbic System - metabolism | Macaca mulatta | Maternal Behavior - drug effects | Piperazines - pharmacology | Blood-Brain Barrier - metabolism | Hormone Antagonists - pharmacology | Hippocampus - metabolism | Animals | Hypothalamus - metabolism | Hormone Antagonists - pharmacokinetics | Bornanes - pharmacokinetics | Female | Piperazines - pharmacokinetics | Hormone Antagonists - blood | Piperazines - blood | Sexual Behavior, Animal - drug effects | Brain | Pharmacology | Antagonist drugs | Animal behavior | Social interaction | Monkeys & apes
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