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Vasopressin Receptor

Vasopressin receptor antagonists and agonists target the receptors for the hormone arginine vasopressin. The V1a receptor mediates vascular contraction, the V1b receptor controls pituitary corticotropin release, and the V2 receptor regulates water reabsorption in the kidney. Cloning of the rat V1a receptor and of the V2 receptor was reported in 1992, and V2 receptor defects were linked to nephrogenic diabetes insipidus. Tolvaptan and mozavaptan are nonpeptide V2 receptor antagonists, while conivaptan hydrochloride blocks both V1a and V2 receptors. OPC21268 is a V1 antagonist, and Vasopressin antagonist 1867 targets the V1b receptor. Peptide agonists such as desmopressin and terlipressin serve as tools for receptor activation studies.

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  • TASP0434299
    Cat. No.
    A64053
    CAS No.
    1520893-08-6

    TASP0434299

    TASP0434299 is a radiolabeled ligand targeting the vasopressin V1b receptor. It demonstrates high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and exhibits potent antagonistic activity at the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 acts as a substrate for human and rhesus monkey P-glycoprotein, leading to low brain uptake. Additionally, it binds specifically and saturably to V1B receptors in rat and monkey pituitary tissues, making it suitable for in vivo and in vitro studies. When radiolabeled, it serves as an effective V1B receptor radiotracer for visualization in positron emission tomography.

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