V1a Receptor  Antagonist

Conivaptan hydrochloride (YM 087) is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure.

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

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.

Conivaptan-d₄ (YM 087-d₄) is the deuterated-labeled Conivaptan (HY-18347). Conivaptan (YM 087 free base) is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure.

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.

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.

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).

(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats.

V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (K_i: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC₅₀: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice.

(D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V_1aR), with a K_i of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R.

VA-111913 (VT-913) is a vasopressin receptor V1A antagonist (K_i = 1.74 nM). VA-111913 reduces uterine contractions and improves uterine blood flow by inhibiting vasopressin, thereby alleviating dysmenorrhea. VA-111913 can be used for research on menstrual pain.

ML389 is a highly selective vasopressin 1a (V1a) receptor antagonist (IC₅₀=40 nM). ML389 is promising for research of central nervous system disorders such as anxiety, depression, and post-traumatic stress disorder (PTSD).

Conivaptan (YM 087 free base) is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure.

YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a K_i value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with K_i values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease.

Conivaptan hydrochloride (Standard) (YM 087 (Standard)) is the analytical standard of Conivaptan hydrochloride (HY-18347A). This product is intended for research and analytical applications. Conivaptan hydrochloride is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure.