Vasopressin Receptor

Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM.

Desmopressin is a synthetic vasopressin analog that acts as an agonist at V1B and V2 receptors (EC50 values are 11.4 and 23.9 nM and Ki values are 5.84 and 65.9 nM respectively).

Big Endothelin-1 (1–38), human, is the biologically inactive precursor of endothelin-1 (ET-1), a potent endogenous vasoconstrictive peptide. Upon enzymatic cleavage by endothelin-converting enzymes (ECEs), Big Endothelin-1 is processed into the active ET-1 form, which plays a critical role in the regulation of vascular tone and blood pressure. This peptide is widely used as a research tool for investigating endothelin signaling pathways, cardiovascular physiology, and related pathophysiological processes.

OPC21268 is a non-peptide AVP Receptor V (Vasopressin Receptor) antagonist that shows 1000-fold selectivity for V1 receptors over V2 receptors.

Vasopressin antagonist, Orally available and selective V1b receptor antagonist (IC50 value 3 nM for hV1b inhibition, exhibiting >1000-fold selectivity over hV1a, hV2, and hOT).

Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM.

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

Balovaptan (RG7314) 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.

WAY-151932 is a vasopressin V2-receptor agonist with IC50 of 80.3 nM and 778 nM in human-V2 binding and V1a binding assay.

Lixivaptan (VPA-985, WAY-VPA 985) 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.

Fedovapagon is a selective vasopressin V2 receptor (V2R) agonist with an EC50 of 24 nM, which is being developed for the treatment of nocturia.

RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).

Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.

Felypressin acetate (PLV-2 acetate) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin acetate is widely used in dental procedures.

SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP.

Felypressin (PLV-2) is a non-catecholamine vasoconstrictor and a vasopressin 1 agonist. Felypressin is widely used in dental procedures.

Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.

Ornipressin (POR-8) is a vasopressin analog and selective V1 receptor agonist. It is used as a local vasoconstrictor and can effectively reverse hypotension associated with combined general/epidural anesthesia. Ornipressin exhibits antidiuretic activity and, in renal failure models, decreases renal vascular resistance while increasing renal blood flow.

Argipressin acetate is a potent vasopressin receptor agonist, primarily targeting the V1, V2, and V3 receptors. It exhibits high affinity for the V1 receptor, with a dissociation constant (Kd) of 1.31 nM in A7r5 rat aortic smooth muscle cells. This compound is valuable for research applications exploring vascular physiology, fluid balance, and the modulation of blood pressure.