Effects of the Oral Oxytocin Receptor Antagonist Tocolytic OBE001 on Reproduction in Rats

Abstract

OBE001 at up to 125 mg/kg/d had no effects on EED and no adverse effects on FD and postnatal development of rats. These results constitute an important step toward the development of OBE001 in preterm labor and ART indications.

Oxytocin in the Male Reproductive Tract; The Therapeutic Potential of Oxytocin-Agonists and-Antagonists

“…• Retosiban (GSK221149A) is a highly selective, orally active, non-peptide OTR-antagonist that inhibits OT-induced uterine contractions (241) and showed efficacy in human clinical trials (242). • OBE001 is an orally active, non-peptide OT-antagonist that is tested for management of preterm labor and showed no adverse effects on early embryonic development in the rat model (243). AVP1A-receptor selective antagonist that also showed tocolytic properties in treatment of preterm labor (246) and was able to potently antagonize OT's effect in the rat and rabbit ejaculatory tissues (prostatic urethra, bladder neck and ejaculatory duct) (81).…”

A Potentially New Tocolytic Agent

“…Therefore, intense research on the topic has been performed resulting on several important publications. [4][5][6][7][8][9] Accordingly, in the current issue of Reproductive Sciences, Danielsson and colleagues report their findings on the anoctamin family and its impact on the uterine smooth muscle contractions. 10 Anoctamins (ANO) are a family of calcium-activated chloride channels, from which a subset has been previously shown to be involved in procontractile depolarizing membrane currents leading to contraction of murine uterine smooth muscle cells.…”