vasopressin receptor

Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM, used in the treatment of autosomal dominant polycystic kidney disease (ADPKD).

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

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.

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

PF-184563 is an effective and selective non-peptide antagonist of the V1a receptor with oral activity, suitable for studying Raynaud's disease and dysmenorrhoea.

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

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.

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.

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.

SRX246 has no interaction at V1b and V2 receptors. SRX246 shows negligible binding at 64 other receptors classes, including 35 G-proteincoupled receptors. SRX246 is a potent and CNS-penetrant vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V

VNA-932 is an agonist of the vasopressin V2-receptor (IC50: 80.3 nM and 778 nM in human-V2 binding and V1a binding assay).

Elsovaptan is an antagonist of the vasopressin receptor and is applicable for research in Alzheimer's disease.

Mozavaptan is a vasopressin receptor antagonist.

vasopressin V1A receptor antagonist

TC OT 39 is an oxytocin analog and selective agonist of OXTR (oxytocin receptor) (EC50=180 nM), also acting as a V1aR (vasopressin 1a receptor) antagonist. It mimics oxytocin-induced scratching in mouse models.

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

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.

Selepressin, an analog of vasopressin, is a potent, selective vasopressin V1a receptor agonist.

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.

Enuvaptan is a vasopressin receptor antagonist and has the potential for research into renal and cardiovascular diseases.

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

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.

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.