• A vasopressin receptor antagonist (VRA) is an agent that interferes with action at the vasopressin receptors. (wikipedia.org)
  • The "vaptan" drugs act by directly blocking the action of vasopressin at its receptors (V1A, V1B and V2). (wikipedia.org)
  • Demeclocycline is not a direct antagonist of the vasopressin receptors however, but rather inhibits activation of the intracellular second messenger cascade of this receptor in the kidney by an unknown mechanism. (wikipedia.org)
  • Vasopressin receptors in rat brain and kidney: studies using a radio-iodinated V1 receptor antagonist. (austin.org.au)
  • Arginine8-vasopressin (AVP) acts via V1 receptors (blood vessels, liver and brain) and V2 receptors (renal collecting duct). (austin.org.au)
  • To study brain and kidney V1 receptors selectively, a specific V1 receptor antagonist [d(CH2)5,Sar7]AVP was radio-iodinated and purified by high performance liquid chromatography. (austin.org.au)
  • Vasopressin acts on the V2 receptors found in the walls of the vasculature and luminal membranes of renal collecting ducts. (ncats.io)
  • The selective V-1B antagonist SSR149415 strongly reduced the ability of vasopressin to increase intracellular Ca2+ concentration but also cAMP, suggesting a cooperation between V1BR and V2R in IMCD cells expressing both receptors. (mtmt.hu)
  • This research explores the role of the sex-different brain peptide, vasopressin as well as its receptors, in the regulation of social behavior and communication using modern intersectional genetic approaches. (gsu.edu)
  • Demeclocycline, a tetracycline antibiotic, is sometimes used to block the action of vasopressin in the kidney in hyponatremia due to inappropriately high secretion of vasopressin (SIADH), when fluid restriction has failed. (wikipedia.org)
  • Release of Vasopressin within the Rat Paraventricular Nucleus in Response to Emotional Stress: A Novel Mechanism of Regulating Adrenocorticotropic Hormone Secretion? (jneurosci.org)
  • Antidiuretic hormone (ADH, arginine vasopressin) secretion results in a concentrated urine and therefore a reduced urine volume. (medilib.ir)
  • Central DI is characterized by decreased secretion of antidiuretic hormone (ADH)-also known as arginine vasopressin (AVP)-which gives rise to polyuria and polydipsia by diminishing the person's ability to concentrate urine. (medscape.com)
  • Selective vasopressin V2-receptor antagonist. (medscape.com)
  • Selective V2R antagonists such as tolvaptan, lixivaptan etc. will likely be useful in patients for whom oral therapy is suitable and for more chronic forms of hyponatremia. (wikipedia.org)
  • Clinical studies in patients with X-linked NDI showed that the selective V1R antagonist relcovaptan (SR49059, Sanofi-Aventis) significantly increased urine osmolality and decreased 24-hour urine flow. (wikipedia.org)
  • Tolvaptan is a selective and competitive arginine vasopressin receptor 2 antagonist. (ncats.io)
  • The inhibition by Ado was reproduced with the selective A 1 agonist, N-6-phenylisopropyladenine (2 nM), and was reversed by 8-cyclopentyl-1,3-dipropylxanthine, an A 1 -receptor antagonist. (utmb.edu)
  • Finally, a mixture of a V1 AVP and the α-helical corticotropin-releasing hormone (CRH) receptor antagonists administered via inverse microdialysis into the PVN caused a significant increase in the plasma adrenocorticotropic hormone (ACTH) concentration compared with vehicle-treated controls both under basal conditions and during social defeat, indicating inhibitory effects of intra-PVN-released AVP and/or CRH on HPA system activity. (jneurosci.org)
  • Angiotensin-converting enzyme inhibitors, b-adrenergic receptor blockers and mineralocorticoid receptor antagonists target the inhibition of renin--angiotensin--aldosterone system and adrenergic nervous system and have become a standard component of therapy for heart failure (HF). (docksci.com)
  • ACCF/AHA 2013 Guideline states V 2 -receptor antagonists may be considered in the short term to improve serum sodium concentration in hospitalized HF patients with persistent severe hypervolemic hyponatremia who are at risk for or are having active cognitive symptoms despite water restriction and guideline-directed medical therapy. (samsca.com)
  • There are 2 main types of medication used to treat Alzheimer's disease cholinesterase inhibitors and NMDA receptor antagonists. (acupuncture.org.uk)
  • Measurements of urine osmolality are recommended to monitor the adequacy of vasopressin inhibition. (medicines.org.uk)
  • Here we demonstrate that a likely mechanism underlying the orexigenic action of RLN3 is RXFP3-mediated inhibition of oxytocin- and arginine-vasopressin-synthesizing paraventricular nucleus (PVN) magnocellular neurosecretory cells. (jneurosci.org)
  • Inhibition of the binding of endogenous oxytocin by the receptor antagonist delayed the GER by 37 % compared to saline (p = 0.037). (biomedcentral.com)
  • It is well-established that the neuropeptide arginine vasopressin (Avp) is important to the neural modulation of mammalian behavior. (frontiersin.org)
  • The neuropeptide arginine vasopressin (AVP) has long been implicated in the regulation of social behavior and communication, but precisely which AVP cell groups are involved is largely unknown. (eneuro.org)
  • The neuropeptide arginine-vasopressin (AVP) has long been implicated in the regulation of social behavior and communication in diverse taxa, but the source of AVP release relevant for behavior has not been precisely determined. (gsu.edu)
  • The neuropeptide arginine-vasopressin (AVP) has long been implicated in the regulation of social behavior and communication in diverse taxa, often through its actions on the V1a receptor (V1aR) and in a sex-different and steroid-dependent way. (gsu.edu)
  • The analgesic effects of both agonist and antagonist are markedly potentiated by spinalization. (tau.ac.il)
  • It also highlights the status of the agonist and antagonist of brain RAS in the treatment of various neurological disorders. (hindawi.com)
  • Tolvaptan is especially useful for heart failure patients as they have higher serum levels of vasopressin. (ncats.io)
  • Polycystin defects increase intracellular cAMP, secondary messenger for vasopressin acting at V2R, leading to cyst development. (wikipedia.org)
  • For hyponatremia in hospitalized patients, who are unable to take medication orally or for those in whom a more rapid correction of hyponatremia is desired, conivaptan (V1/V2R antagonist) will likely be the preferred agent. (wikipedia.org)
  • The arginine vasopressin 1b receptor (Avpr1b) is involved in the modulation of a variety of behaviors and is an important part of the mammalian hormonal stress axis. (frontiersin.org)
  • The aim of dose titration is to block activity of vasopressin at the renal V2 receptor as completely and constantly as possible, while maintaining acceptable fluid balance (see section 4.4). (medicines.org.uk)
  • Although vasopressin V-1B receptor (V1BR) mRNA has been detected in the kidney, the precise renal localization as well as pharmacological and physiological properties of this receptor remain unknown. (mtmt.hu)
  • Patients with heart failure are at risk for hypervolemic hyponatremia as a result of excess sodium and water retention , promoted by increased vasopressin levels and compromised glomerular filtration. (samsca.com)
  • It was observed that the greatest sensitivity for vasopressin was in the papilla (concentration of 8-arginine vasopressin required for 50% activation of adenylate cyclase [Kact] was 2.0 X 10(-9)M, 1.1 X 10(-9)M and 5.1 X 10(-10) M in the cortex, medulla and papilla, respectively). (aspetjournals.org)
  • Arginine vasopressin antagonist (V1A, V2) indicated for euvolemic (dilutional) and hypervolemic hyponatremia. (medscape.com)
  • V2R antagonists have become a mainstay of treatment for euvolemic (i.e. (wikipedia.org)
  • Also acting as antagonists of the antidiuretic action of arginine vasopressin are compounds of the formula ##STR2## wherein X and Z are as above and n is 4 or 5. (utoledo.edu)
  • Sex differences in vasopressin 1a receptor regulation of social communication within the lateral habenula and dorsal raphe of mice. (gsu.edu)
  • Despite over thirty years of indirect evidence implicating sexually-dimorphic arginine vasopressin (AVP) cells within the bed nucleus of the stria terminalis (BNST) in the control of social and anxiety-related behavior in mammals, the function of these cells has never been directly tested. (eneuro.org)
  • This cooperation arises from a cross talk between second messenger cascade involving PKC rather than receptor heterodimerization, as supported by potentiation of arginine vasopressin-stimulated cAMP production in human embryonic kidney-293 cells coexpressing the two receptor isoforms and negative results obtained by bioluminescence resonance energy transfer experiments. (mtmt.hu)
  • We reported earlier that vasopressin (AVP) peptide expression is significantly decreased in the postmortem hypothalamus of glucocorticoid (GC) treated patients, while such a decrease was not observed in AVP prohormone (proAVP) expression. (nel.edu)
  • Lithium, as lithium carbonate, possesses similar properties to those of demeclocycline on the action of vasopressin in the kidney, and was used clinically before demeclocycline, which largely superseded it for this indication. (wikipedia.org)
  • Studies in several animal models of polycystic kidney disease have shown a reduction in kidney size and cyst volume after treatment with specific V2 receptor antagonist. (wikipedia.org)
  • and [1-(beta-mercapto-beta, beta-cyclopenta-methylenepropionic acid), 2-D-(O-ethyl)tyrosine,4-valine,8-arginine]vasopressin (SK&F 100398, 101071 and 101498, respectively) using plasma membranes prepared from cortex, medulla and papilla of dog kidney. (aspetjournals.org)
  • Thus V1R and/or V2R antagonists may serve as molecular chaperones to mitigate misfolding defects in selected patients with type 2 NDI. (wikipedia.org)
  • To examine morphological, radiological and biochemical effects of arginine vasopressin (AV) and V1 receptor antagonist on cerebral vasospasm (CVS) after subarachnoid hemorrhage (SAH) in rabbits. (turkishneurosurgery.org.tr)
  • The aim of this study was therefore to examine whether oxytocin, or the receptor antagonist atosiban, influence the gastric emptying. (biomedcentral.com)
  • The aim of this study was to further examine the effect of oxytocin on gastric emptying in healthy individuals, by examining the gastric emptying rate (GER) during continuous infusion of either oxytocin or the oxytocin receptor antagonist atosiban. (biomedcentral.com)
  • this model of an ADP-receptor antagonist, DDAVP results in partial reversal of clopidogrel-induced platelet dysfunction. (eotp.org)
  • In general, vasopressin is a nonapeptide consisting of a six-amino-acid ring with a cysteine 1 to cysteine 6 disulfide bridge or an octapeptide containing a CYSTINE. (lookformedical.com)
  • Other antagonists of the antidiuretic action of arginine vasopressin are of the formula ##STR3## wherein X and n are as above and Z' is (D- or L-)Orn or (D- or L-)Lys. (utoledo.edu)
  • Arginine vasopressin (AVP) and terlipressin were proposed as alternatives to catecholamines in shock states characterized by decreased plasma AVP concentrations. (silverchair.com)