Balovaptan (RG7314; RG-7314; RO-5285119) is a novel potent and brain-penetrant vasopressin 1a (hV1a) receptor antagonist with the potential to be used for autism.

Lixivaptan (formerly known as VPA-985, WAY-VPA 985) is a novel, potent, selective and orally bioactive non-peptide antagonist of vasopressin receptor V2 with IC50 values of 1.2 and 2.3 nM for human afnd at V2, respectively.

Mozavaptan (formerly known as OPC-31260; OPC-31260l; OPC31260; OPC31260l) is an orally bioactive, selective and competitive vasopressin receptor antagonist for both V1 and V2 receptors with anti-hypernatremic activity.

Tolvaptan (formerly OPC41061; OPC-41061; trade names Samsca; Jinarc; Resodim) is a selective, competitive, orally bioavailable and nonpeptide antagonist of arginine vasopressin V2 receptor with anti-hypernatremic activity.

Terlipressin is a potent vasoconstrictor that acts via V1 receptors on arteriolar smooth muscle cells.

Conivaptan HCl (formerly known as YM-087; YM087; YM 087, trade name Vaprisol), the hydrochloride salt of Conivaptan, is an orally bioavailable and non-peptide antagonist of vasopressin V1A and V2 receptors with anti-hypernatremic activity.

OPC-21268 is a vasopressin 1 receptor antagonist potentially for the treatment of heart failure and hypertension.

Terlipressin acetate is a novel and potent analogue of vasopressin.