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Design and synthesis of highly selective in vitro and in vivo uterine receptor antagonists of oxytocin: comparisons with Atosiban.
- M. Manning, K. Miteva, S. Pancheva, S. Stoev, N. Wo, W. Y. Chan
- Biology, ChemistryInternational journal of peptide and protein…
- 12 January 2009
The solid phase synthesis and some pharmacological properties of seven position two analogues of one of the authors' lead oxytocin antagonists, des-9-glycinamide, appear to be as or more potent and much more selective than the closely related OT antagonist 1-deamino.
A study on the mechanism of vasopressin escape: effects of chronic vasopressin and overhydration on renal tissue osmolality and electrolytes in dogs.
- W. Y. Chan
- Medicine, BiologyThe Journal of pharmacology and experimental…
It is concluded that vasopressin escape results not from a prolonged exposure of the kidney tissue to the hormone but is related to a dissipation of corticomedullary osmotic gradient consequent to overhydration.
Characterization of a novel, linear radioiodinated vasopressin antagonist: an excellent radioligand for vasopressin V1a receptors.
HO-LVA appeared to be the first radioligand to successfully identify and localize the presence of V1a receptors in rat liver and blood vessel walls, and several new brain regions expressing V 1a receptors could be identified, in addition to those brain regions that were previously identified with other radiolabelled AVP analogues.
Agonist and antagonist specificities of decidual prostaglandin-releasing oxytocin receptors and myometrial uterotonic oxytocin receptors in pregnant rats.
- D. L. Chen, W. Y. Chan, M. Manning
- Biology, MedicineJournal of reproduction and fertility
- 1 November 1994
It was found that the decidual and myometrial oxytocin receptors exhibit different ligand specificities and arginine-vasopressin was found to have 16% of its PGF2 alpha-releasing activity.
The role of oxytocin receptors and vasopressin V1a receptors in uterine contractions in rats: implications for tocolytic therapy with oxytocin antagonists.
Advances in the design of selective antagonists, potential tocolytics, and radioiodinated ligands for oxytocin receptors.
The current status of the field is reviewed, studies in laboratories which have led to the design of highly potent non-selective and selective OT antagonists are reported on and a number are more selective than Atosiban, currently in clinical trial as a tocolytic agent.
Isosteric substitution of Asn5 in antagonists of oxytocin and vasopressin leads to highly selective and potent oxytocin and V1a receptor antagonists: new approaches for the design of potential…
- W. Y. Chan, N. Wo, L. Cheng, M. Manning
- Biology, ChemistryThe Journal of pharmacology and experimental…
- 1 May 1996
The Dap5 and Dab5 and OT andVP antagonist analogues were surprisingly shown to be much more selective than their respective parent compounds, and appear to be the first single-receptor-type-selective OT and VP antagonists discovered to date.
Effects of oxytocin and uterine and luteal prostaglandins on the functional regression of the corpus luteum in pseudopregnant rats.
The oxytocin-induced shortening of pseudopregnancy was associated with a premature functional regression of the corpus luteum and both luteal and uterine PGF2 alpha concentrations were found to increase with luteolysis and reached peak values before the return of oestrus.
Relationship between the uterotonic action of oxytocin and prostaglandins: oxytocin action and release of PG-activity in isolated nonpregnant and pregnant rat uteri.
- W. Y. Chan
- BiologyBiology of reproduction
- 1 November 1977
RENAL EXCRETION AND TISSUE DISTRIBUTION OF RADIOACTIVITY AFTER ADMINISTRATION OF TRITIUM-LABELED OXYTOCIN TO RATS.
- J. P. Aroskar, W. Y. Chan, J. E. Stouffer, C. Schneider, V. V. Murti, V. Duvigneaud
- Biology, MedicineEndocrinology
- 1 February 1964
Renal excretion and tissue distribution of radioactivity after injection of oxytocin synthesized from tritium-labeled leucine were studied in anesthetized male rats, indicating the deep and generalized radioactivity detected in skeletal muscle and cerebral cortex.