Table 1.
The most extensively studied OT antagonists and their experimental or clinical applications.
| Oxytocin antagonists | Organism | Experimental or therapeutic application |
|---|---|---|
| (I) Peptide | ||
|
| ||
| 1-Deamino-2-D-Tyr-(O-ethyl)-4-Thr-8-ornoxytocin (Atosiban) | Human | Clinically used tocolytic agent |
| d(CH2)5[Tyr(Me)2]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| desGly–NH2,d(CH2)5[Tyr(Me)2,Thr4]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| desGly–NH2,d(CH2)5[D-Tyr2,Thr4]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| d(CH2)5,[D-Thi2,Thr4,Tyr–NH2 9]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| desGly–NH2,d(CH2)5[D-Trp2,Thr4,Dap5]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| desGly–NH2,d(CH2)5[D-2-Nal2,Thr4]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| desGly–NH2,d(CH2)5[2-Nal2,Thr4]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| d(CH2)5[D-2-Nal2,Thr4,Tyr–NH2 9]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| d(CH2)5[2-Nal2,Thr4,Tyr–NH2 9]OVT | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| FE 200 400 (Barusiban) | Monkeys/human myometrial tissue | Pharmacological tool in experimental studies of OT functions |
|
| ||
| (II) Nonpeptide | ||
|
| ||
| GSK221149A (Retosiban) | Rats | Tocolytic action. A phase ll clinical trial for its use as a tocolytic in humans has not yet been completed |
| L-368,899 | Animals/human cells and tissues, or both | Pharmacological tools in experimental studies of OT function. CNS effects. Inhibits spontaneous nocturnal uterine contractions in pregnant rhesus monkeys. Clinical studies discontinued |
| L-371,257 | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| WAY-162720 | Animals/human cells and tissues, or both | Pharmacological tool in experimental studies of OT functions |
| SSR-126768A | Rats/human myometrial tissue | Tocolytic action in rats. Inhibits the response to OT in term human pregnant uterine sections |