Fedovapagon (VA106483)是一种选择性的加压素 V2 受体 (V2R) 激动剂，EC50 为 24 nM，可用于夜尿症研究。

Balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.

RO5028442 is a potent and selective brain-penetrant vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).

Lixivaptan is an orally active and selective vasopressin receptor V2 antagonist with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.

Conivaptan HCl is an inhibitor of antidiuretic hormone or antagonist of vasopressin receptor. It can inhibit rat liver V1A receptor and kidney V2 receptor with Ki of 0.48 nM and 3.04 nM, respectively.

Atosiban is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

Atosiban is competitive antagonist of vasopressin and oxytocin receptors. It is a nonapeptide and the analogue of desamino-oxytocin.

SR49059 is a potent and selective non-peptide vasopressin V1A receptor antagonist which is devoid of agonist activity. SR49059 displays high affinity and efficacy at both rat (Ki = 1.6 nM) and human (Ki = 1.1 - 6.3 nM) V1A receptors and potently antagonizes arginine vasopressin-induced effects in vitro (IC50 = 3.7 nM for inhibition of human platelet aggregation) and is orally active in vivo.