opc-21268

**OPC-21268** is an orally active, nonpeptide antagonist of the vasopressin V1 receptor developed chiefly for research and potential therapeutic applications. It selectively and competitively blocks the V1 subtype of vasopressin receptors, showing markedly higher affinity for rat V1 receptors than for human V1 receptors. Pharmacologically, OPC-21268 antagonizes arginine vasopressin (AVP)-induced vasoconstriction and pressor responses, and its selectivity makes it a useful tool in studying the physiological role of AVP. Therapeutic potential has been discussed in conditions such as hypertension and congestive heart failure, as well as in pathological states involving vasoconstriction mediated by AVP. OPC-21268 exhibits oral bioavailability and has a favorable safety and pharmacokinetic profile in human studies[1][2][3][4][5][6][7].

Other names

opc-21268opc21268opc 21268