Conivaptan HCl is an orally active vasopressin receptor (V1a/V2; Ki=0.48nM/3.04nM) antagonist. Conivaptan HCl modulates vascular resistance and enhances diuresis to increase serum sodium concentration. Conivaptan HCl can be used in research related to hyponatremia and heart failure[1-4].
In vitro, in the presence of anti-CD3 (2μg/ml), anti-CD28 (2μg/ml), interleukin-2 (10ng/ml), and transforming growth factor-β (10ng/ml), Conivaptan HCl (1μM) was used to treat mouse CD4⁺ T cells for 4 days. Conivaptan HCl significantly inhibited the differentiation of CD4⁺ T cells into helper T cells[5]. Conivaptan HCl (0.78-100μM) was used to pretreat HCT-8 cells for 30 minutes, followed by infection with HCoV-OC43 (MOI=0.05) for 72 hours. Conivaptan HCl inhibited the replication of HCoV-OC43 and reduced virus-induced cytopathic effects[6].
In vivo, Conivaptan HCl (0.5mg/kg/day) was intraperitoneally injected into TNBS-induced colitis Balb/c mice for 6 days. Conivaptan HCl significantly attenuated TNBS-induced colitis[7]. Conivaptan HCl (0.1 or 0.3mg/kg; single injection) was intravenously injected into Sprague-Dawley rats with myocardial infarction-induced congestive heart failure. Conivaptan HCl significantly improved cardiac hemodynamics and alleviated pulmonary congestion[8].
References:
[1] Fernández-Varo G, Ros J, Cejudo-Martín P, et al. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61.
[2] Yatsu T, Tomura Y, Tahara A, et al. Cardiovascular and renal effects of conivaptan hydrochloride (YM087), a vasopressin V1A and V2 receptor antagonist, in dogs with pacing-induced congestive heart failure. Eur J Pharmacol. 1999 Jul 9;376(3):239-46.
[3] Li R, Sun H, Zheng H, et al. Intradermal Injection of Oxytocin Aggravates Chloroquine-Induced Itch Responses via Activating the Vasopressin-1a Receptor/Nitric Oxide Pathway in Mice. Front Pharmacol. 2019 Nov 15;10:1380.
[4] He Y, Bae JSH, Nowak E, et al. Rational discovery of therapeutic PAK1 allosteric activators. Cell. 2026 Mar 31:S0092-8674(26)00275-8.
[5] Dou D, Ji Y, Zheng J, et al. A New Role for Conivaptan in Ulcerative Colitis in Mice: Inhibiting Differentiation of CD4+T Cells into Th1 Cells. Dig Dis Sci. 2022 Aug;67(8):3683-3692.
[6] Yang CW, Peng TT, Hsu HY, et al. Repurposing old drugs as antiviral agents for coronaviruses. Biomed J. 2020 Aug;43(4):368-374.
[7] Dou D, Chen L, Di H, et al. Vasopressin augments TNBS-induced colitis through enteric neuronal V1a receptor-mediated COX-2-dependent prostaglandin release from mast cells in mice. Neurogastroenterol Motil. 2019 Feb;31(2):e13493.
[8] Wada K, Fujimori A, Matsukawa U, et al. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51.