AVPR1A,2 bind AVPR antagonists

Stable Identifier
Reaction [binding]
Homo sapiens
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Conivaptan (YM087, brand name Vaprisol) (Tahara et al. 1998, 1998b) and tolvaptan (trade names Samsca, Jinarc) (Schrier et al. 2006) are non-peptide inhibitors of the vasopressin receptors AVPR1A and AVPR2. They are used to treat hyponatremia (low blood sodium levels) (Greenberg & Verbalis 2006). They function by antagonizing AVPR2 receptors in the renal collecting ducts thus causing aquaresis (water secretion) but without electrolyte loss. AVPV2 receptor antagonists may also be useful in the treatment of polycystic kidney disease (PKD) (Belibi et al. 2004, Poch et al. 2018). Satavaptan was under investigation in clinical trials for the prevention of ascites (Soupart et al. 2006) and hyponatremia (Gines et al. 2008) but development has been discontinued. Lixivaptan is a potent, non-peptide, selective AVPR2 antagonist (Albright et al. 1998) that shows promise in treating heart failure in patients with hyponatremia (Abraham et al. 2008, Liamis et al. 2014).

Literature References
PubMed ID Title Journal Year
16672911 Vasopressin receptor antagonists

Greenberg, A, Verbalis, JG

Kidney Int. 2006
30303493 An update on tolvaptan for autosomal dominant polycystic kidney disease

Blasco, M, Rodas, L, Quintana, L, Poch, E, Molina, A

Drugs Today 2018
24766294 Treatment of hyponatremia: the role of lixivaptan

Liamis, G, Elisaf, MS, Filippatos, TD

17699341 Successful long-term treatment of hyponatremia in syndrome of inappropriate antidiuretic hormone secretion with satavaptan (SR121463B), an orally active nonpeptide vasopressin V2-receptor antagonist

Legros, JJ, Alföldi, S, Soupart, A, Heshmati, HM, Annane, D, Gross, P, Decaux, G

9884074 Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells

Wada, K, Ishii, N, Sugimoto, T, Tsukada, J, Saito, M, Tahara, A, Tomura, Y, Yatsu, T, Tanaka, A, Uchida, W, Kusayama, T

Br. J. Pharmacol. 1998
9651149 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors

Reich, MF, Sum, FW, Mazandarani, H, Bailey, T, Albright, JD, Venkatesan, AM, Dusza, JP, Chan, PS, Coupet, J, Delos Santos, EG, Ru, X

9459574 Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist

Wada, K, Ishii, N, Sugimoto, T, Tsukada, J, Saito, M, Tahara, A, Tomura, Y, Yatsu, T, Tanaka, A, Uchida, W, Kusayama, T

Naunyn Schmiedebergs Arch. Pharmacol. 1998
17105757 Tolvaptan, a selective oral vasopressin V2-receptor antagonist, for hyponatremia

Berl, T, Verbalis, JG, Schrier, RW, Czerwiec, FS, SALT Investigators, -, Orlandi, C, Gross, P, Gheorghiade, M

N. Engl. J. Med. 2006
20973922 Rationale and design of the treatment of hyponatremia based on lixivaptan in NYHA class III/IV cardiac patient evaluation (THE BALANCE) study

Abraham, WT, Hasenfuss, G, Aranda, JM, Elkayam, U, Orlandi, C, Kukin, M, Gilbert, EM, Gottlieb, SS, Tavazzi, L, Feldman, AM, Lowes, BD, O'Connell, JB, Ticho, B, Boehmer, JP

18508290 Effects of satavaptan, a selective vasopressin V(2) receptor antagonist, on ascites and serum sodium in cirrhosis with hyponatremia: a randomized trial

Wong, F, Ginès, P, Milutinovic, S, Watson, H, HypoCAT Study Investigators, -, Olteanu, D, del Arbol, LR

15327388 Cyclic AMP promotes growth and secretion in human polycystic kidney epithelial cells

Helmkamp, GM, Grantham, JJ, Reif, G, Wallace, DP, Li, H, Yamaguchi, T, Belibi, FA, Olsen, L

Kidney Int. 2004
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