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Restrict the search for
vasopressin
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Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
OPC-21268, a non-peptide vasopressin V1 receptor antagonist, inhibited oxytocin- and vasopressin-induced contractions of myometrial strips from rats and from full-term pregnant women. OPC-21268, because of its non-peptide structure, is orally active and has been shown to lower blood pressure in a patient with congestive heart failure and in spontaneously hypertensive rats. It also attenuates vasopressin induced bradycardia in rabbits and pressor responses in rats. It has been demonstrated that OPC-21268 exerts its inhibitory action through binding to the vasopressin V1 receptors in rat liver and kidney. Finally, OPC-21268 was reported to be safe and non-toxic in healthy humans. Merck scientists showed that OPC-21268 had significant affinity for the rOTR and the hOTR. OPC-21268 has been in phase II clinical trials by Otsuka for the treatment of heart failure and hypertension. However, this research has been discontinued.
