Vasopressin Receptor

Tolvaptan (OPC-41061) is an orally bioavailable, selective, arginine vasopressin receptor 2 (V2, AVPR2) antagonist that can be used to treat hyponatremia.

Desmopressin acetate (16679-58-6 free base) (DDAVP) is the synthetic analog of the antidiuretic hormone arginine vasopressin. Vasopressin Receptor The antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin acetate (16679-58-6 free base) works by limiting the amount of water that is eliminated in the urine. Desmopressin acetate (16679-58-6 free base) binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates the release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

Desmopressin (DDAVP)(DDAVP) is the synthetic analogue of the antidiuretic hormone arginine vasopressin.Vasopressin Receptor The antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin works by limiting the amount of water that is eliminated in the urine. Desmopressin binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

E-4177 is an angiotensin II type 1 receptor (AT1R) antagonist and can be used to study cardiovascular diseases.

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

OPC-51803 is an orally available nonapeptidylpressor (AVP) V(2) receptor selective agonist for the treatment of urinary incontinence and nocturia.

Atosiban acetate (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban acetate (RW22164) inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban acetate (RW22164) suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.

Fedovapagon (VA106483) is a selective and potent agonist of the vasopressin V2 receptor (V2R) that inhibits the growth of intersegmental vessels in zebrafish. It can be used to study overactive bladder, nocturia, and painful bladder syndromes.

Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner.

Terlipressin Acetate, a highly selective vasopressin V1 receptor agonist, on oxygen and glucose deprivation re-oxygenation (OGD R)-induced damage in intestinal epithelial cells (IEC-6).Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

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. It is used for the research of autism.

Mozavaptan (OPC-31260) is a competitive antagonist of vasopressin receptors, targeting both V1 and V2 receptors, with IC50 values of 1.2 μM and 14 nM, respectively.

Felypressin acetate (PLV-2) is an agonist of vasopressin 1 and acts on all arginine vasopressin receptors 1AS. Felypressin acetate can be used in dental procedures.

Argipressin (Arg8-vasopressin) inhibits central corticotropin-releasing hormone. Argipressin acts as a repressor in the regulation of central CRH levels. 5A2-SC8 is an APC-dependent protein.

TASP0390325 is an orally active and high affinity arginine pressin receptor 1B (V1B receptor) antagonist that shows antidepressant and anxiolytic activity in animal studies and blocks V1B receptors in the anterior pituitary gland in vivo.

Felypressin (Octapressin) is a synthetic analog of LYPRESSIN with a PHENYLALANINE substitution at residue 2. Felypressin is a vasoconstrictor with reduced antidiuretic activity.

Fuscoside (OPC-21268) is a non-peptide arginine vasopressin (AVP) receptor VI antagonist with an IC50 value of 0.4 μM[2].

Lixivaptan (VPA-985) is an orally active and selective vasopressin receptor V2 antagonist(Ki = 2.3 nM)

d[Cha4]-AVP acetate is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). Stimulates ACTH and corticosterone secretion and exhibits negligible vasopr

Conopressin S acetate(111317-90-9 free base) (Con-S acetate) is a natural product isolated from Conus striatus, shows high affinity with vasopressin V1b receptor (AVPR1B), with a Ki of 8.3 nM.

d[Leu4,Lys8]-VP acetate is a selective vasopressin V1b receptor agonist. The Kis for rat, human and mouse V1b receptors are 0.16 nM, 0.52 nM and 0.1.38 nM, respectively. d[Leu4,Lys8]-VP acetate exhibits weak antidiuretic, vasopressor and oxytocic activiti

RG7713 (RO 5028442) has been used in trials studying Autistic Disorder.

Atosiban (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence.

Vasopressin Dimer (anti-parallel) TFA, an anti-parallel dimer form of vasopressin, has the capability to activate four G protein-coupled receptors: V1aR, V1bR, V2R, and OTR [1].

'(D-Arg8)-Inotocin is a potent, selective, and competitive antagonist of the vasopressin receptor (V 1a R), exhibiting a binding affinity (K i) of 1.3 nM. It demonstrates over 3000-fold selectivity for the human V1aR compared to the OTR, V1bR, and V2R subtypes [1].'

Vasopressin Dimer (parallel) TFA, a parallel dimer of Vasopressin, has the capability to activate four G protein-coupled receptors—namely, V1aR, V1bR, V2R, and OTR [1].

Val9-Oxytocin, an Oxytocin analog where Gly9 is substituted with Val9 [1], functions as a complete antagonist of the vasopressin (V1a) receptor.

Invopressin (Compound 42), a vasopressin V1A receptor partial agonist (EC50: 1.0 nM), is utilized in research related to cirrhosis conditions such as bacterial peritonitis, HRS2, and refractory ascites [1].

[Deamino-Pen1,Val4,D-Arg8]-vasopressin (AVP-A) is an antagonist of arginine-vasopressin (AVP) that effectively reduces plasma aldosterone concentration in rats and is used to study the growth and steroidogenic capacity of the rat adrenal zona glomerulosa [1].

Dp[Tyr(Me)2,Arg8]-Vasopressin is a non-selective antagonist of the peptide arginine vasopressin V1b receptor [1].

(d(CH2)5[Tyr(Me)2, Dab5]AVP), a vasopressin V1a receptor-specific antagonist, demonstrates a pA2 value of 6.71 [1].