Vasopressin Receptor Antagonist

Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V₂R) antagonist with an IC₅₀ of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia.

Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with K_i values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

Atosiban (RW22164; RWJ22164) 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.

SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a K_i vaule of 1.4 nM.

Atosiban-d₅ TFA (RW22164-d₅ TFA) is the deuterium labeled Atosiban TFA. Atosiban (RW22164; RWJ22164) 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.

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.

Nelivaptan (SSR-149415) is a selective and orally active vasopressin V_1b receptor antagonist (K_i: 3.7 and 1.3 nM for native and recombinant rat V_1b receptors, respectively). Nelivaptan inhibits arginine vasopressin (AVP)-induced Ca²⁺ increase and corticotropin secretion. Nelivaptan can be used for research of stress, anxiety and depression.

Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V₂ receptor antagonist with an IC₅₀ of 14 nM. Mozavaptan shows ~85-fold selectivity for V₂ receptor over V₁ receptor (IC₅₀ of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.

L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (K_i=19 nM) and vasopressin V1a receptor (K_i=3.7 nM).

Balovaptan (RG7314) is an orally available, selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with K_is of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.

Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V₂ receptor antagonist with an IC₅₀ of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V₂ receptor over V₁ receptor (IC₅₀ of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.

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.

SRX246 is a potent, BBB-penetrant, highly selective vasopressin 1a (V1a) receptor antagonist (K_i=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.

Fuscoside (OPC-21268) is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC₅₀ of 0.4 μM.

TASP0390325 is a high affinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities.

TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC₅₀=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an K_i value of 330 nM. TC OT 39 exhibits sedative effects in mouse models.

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.

Vasopressin V2 receptor antagonist 2 (Compound 33) is an antagonist of the arginine vasopressin V₂ receptor (V₂R) with a K_i value of 6.2 nM. Vasopressin V2 receptor antagonist 2 can effectively reduce cAMP levels, thereby inhibiting the growth of renal cysts[1].

RG7713 (RO5028442) is a highly potent, selective and brain-penetrant Vasopressin 1a (V1a) receptor antagonist with K_is of 1 nM (hV1a) and 39 nM (mV1a).

Brezivaptan (Brezivaptanum; TH1773; TS-121) is a vasopressin receptor antagonist.