Conivaptan (hydrochloride)

Conivaptan is an antagonist of the arginine vasopressin (AVP) receptors V_1A and V₂ (K_is = 0.48 and 3.04 nM for rat liver V_1A and kidney V₂, respectively).¹ It also competitively inhibits oxytocin binding to rat uterine oxytocin receptors (K_i = 44 nM) but has no effect on AVP binding to anterior pituitary V_1B receptors at concentrations up to 100 μM in a radioligand binding assay. Conivaptan suppresses AVP-induced increases in intracellular calcium in vascular smooth muscle cells (VSMCs) in vitro and the pressor response in pithed rats. Conivaptan (0.01-0.3 mg/kg, i.v.) increases urine output and decreases urine osmolality in dehydrated conscious rats in a dose-dependent manner. It also reduces brain edema and blood-brain barrier disruption in a mouse experimental stroke model.²

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1. Tahara, A., Tomura, Y., Wada, K.-I., et al. Pharmacological profile of YM087, a novel potent nonpeptide vasopressin V1A and V2 receptor antagonist, in vitro and in vivo. J. Pharmacol. Exp. Ther. 282(1), 301-308 (1997).

2. Zeynalov, E., Jones, S.M., Seo, J.W., et al. Arginine-vasopressin receptor blocker conivaptan reduces brain edema and blood-brain barrier disruption after experimental stroke in mice. PLoS One 10(8), e0136121 (2015).