Vasopressin 2 receptor. Medical search. Frequent questions

These interact with the receptor to restore cognate receptor function devoid of antagonist or agonist activity. (wikipedia.org)
Ramelteon is a melatonin receptor agonist with high selectivity for human melatonin MT1 and MT2 receptors. (medscape.com)
Vasopressin V2 Receptor (V2R) Agonist - Pipeline Insight, 2022" report by the publisher offers comprehensive insights of the pipeline (under development) therapeutics scenario and growth prospects across Vasopressin V2 Receptor (V2R) Agonist development. (researchandmarkets.com)
The report assesses the active Vasopressin V2 Receptor (V2R) Agonist pipeline products by developmental stage, product type, molecule type, and administration route. (researchandmarkets.com)
In vivo, only acute administration of high doses of V-1B agonist triggered significant diuretic effects, in contrast with injection of selective V-2 agonist. (mtmt.hu)
Lysine vasopressin, the selective V2 agonist dDAVP, and the V1-selective agonist SK&F 105349 were at least 10- to 100-fold less potent than oxytocin and exhibited only partial agonist activity. (aspetjournals.org)
GA20084 (Deamino-Cys¹,β-cyclohexyl-Ala⁴,Arg⁸)-Vasopressin Studies revealed that this specific vasopressin agonist exhibited a nanomolar affinity for V-1b receptors from various mammalian species (bovine, human, rat). (glpbio.cn)
In this case, positive inotropes (dobutamine 1-5 mcg/kg/min IV - an agonist of beta-adrenergic receptors) and diuretics are administered depending on the cardiomyopathy. (vin.com)
Binding of these receptors to an agonist such as norepinephrine reduces cAMP, which leads to smooth muscle contraction. (cvphysiology.com)

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)
Calcium transients were induced by oxytocin and the oxytocin selective analog AM-2-40 and blocked by the oxytocin-selective antagonist KB-5-21. (aspetjournals.org)
However, the poor correlation between antagonism at the LLC-PK1 receptors and the rat uterus oxytocin receptors suggests marked differences in antagonist recognition. (aspetjournals.org)
Tolvaptan is a selective V 2 vasopressin receptor antagonist, which had been hypothesized to slow the progression of ADPKD by reducing the development and growth of kidney cysts, which are characteristic of the disease and often associated with pain, hypertension and kidney failure. (empr.com)

Evidence suggests that the 2p12 region of chromosome 2 and a variation in a gene called the arginine vasopressin receptor 1A ( AVPR1A ) might contribute to ASPD. (psychcentral.com)
Variation in mothers' arginine vasopressin receptor 1a and dopamine receptor D4 predicts mat. (uncg.edu)

Vasopressin receptor antagonists that are selective for the V2 receptor include: Tolvaptan (FDA-approved) Lixivaptan Mozavaptan Satavaptan Their main uses are in hyponatremia, such as that caused by syndrome of inappropriate antidiuretic hormone (SIADH) and heart failure, however these agents should be avoided in patients with cirrhosis. (wikipedia.org)
Demeclocycline and lithium carbonate act as indirect antagonists of renal vasopressin V2 receptors by inhibiting activation of the second messenger cascade of the receptors. (wikipedia.org)
At the extreme, functionally selective ligands may be both agonists and antagonists at different functions mediated by the same receptor. (aspetjournals.org)
Treatment strategies for syndrome of inappropriate antidiuretic hormone include fluid restriction to 1 to 1.5 L of free water per day, sodium chloride tablets, isotonic saline along with furosemide or hypertonic saline (2% or 3%) alone, and vasopressin-2 (V2) receptor antagonists (conivaptan and tolvaptan). (mhmedical.com)

During her MSc studies, Dr Plouffe also contributed to the characterisation of new selective AT 2 R agonists in collaboration with research teams from Uppsala University (Sweden). (qub.ac.uk)
Genetic drift and selective forces have shaped the individual structure of a given receptor gene but also of the species-specific receptor repertoire - a process that is still ongoing. (springer.com)

Oxytocin induces a transient increase in cytosolic free [Ca2+] in renal tubular epithelial cells: evidence for oxytocin receptors on LLC-PK1 cells. (aspetjournals.org)
These data indicate that oxytocin-induced calcium transients in LLC-PK1 cells were not mediated by V1 or V2 vasopressin receptors, but by oxytocin receptors. (aspetjournals.org)
The effects on [Ca2+]i probably are not mediated by V1 and V2 vasopressin receptors, but by putative oxytocin receptors. (aspetjournals.org)

North WG, Fay MJ, Longo KA, Du J: Expression of all known vasopressin receptor subtypes by small cell tumors implies a multifaceted role for this neuropeptide. (hmdb.ca)
Mapping neuropeptide receptors in these nontraditional species questions existing assumptions and informs proposed evolutionary explanations about the biological bases of monogamy. (brainresearchlab.com)
Intrinsic brain RAS is an enzyme-neuropeptide system having functional components (angiotensinogen, peptidases, angiotensin, and specific receptor proteins) with important biological and neurobiological activities in the brain. (hindawi.com)

Patients were randomized 2:1 to receive either a morning/afternoon split dose regimen of tolvaptan (45/15mg, 60/30mg or 90/30mg daily as tolerated) or placebo. (empr.com)
The blockade of vasopressin receptors with tolvaptan continues to make appearances as a potential therapy in multiple arenas. (medscape.com)

Then, she quickly developed a marked interest for G protein-coupled receptor (GPCR) signalling. (qub.ac.uk)
This promotes G protein uncoupling from receptor, GPCR internalisation and signalling arrest. (qub.ac.uk)
The valuable source of large-scale genomic information initiated attempts to identify the origin(s) of G protein-coupled receptors (GPCR), count and categorize those genes, and follow their evolutionary history. (springer.com)
The chapter summarizes evolutionary processes working on GPCR genes and sheds light on their consequences at the levels of receptor structure and function. (springer.com)
Characterisation of G protein-coupled receptors (GPCR) relies on the availability of a toolbox of ligands that selectively modulate different functional states of the receptors. (liverpool.ac.uk)

Seibold A, Brabet P, Rosenthal W, Birnbaumer M: Structure and chromosomal localization of the human antidiuretic hormone receptor gene. (hmdb.ca)

Vasopressin receptor 2 (V2R), or arginine vasopressin receptor 2 (officially called AVPR2), is a protein that acts as receptor for vasopressin. (wikipedia.org)
AVPR2 belongs to the subfamily of G-protein-coupled receptors. (wikipedia.org)
Because von Willebrand factor helps stabilize circulating levels of factor VIII, the vasopressin analog desmopressin can be used to stimulate the AVPR2 receptor and increase levels of circulating factor VIII. (wikipedia.org)
The vasopressin receptor gene AVPR2 is located on the X chromosome. (britannica.com)

Arg-vasotocin (AVT) is the homolog of mammalian Arg-vasopressin (AVP). (frontiersin.org)
Contemporary theory that emphasizes the roles of oxytocin and vasopressin in mammalian sociality has been shaped by seminal vole research that revealed interspecific variation in neuroendocrine circuitry by mating system. (brainresearchlab.com)

Fay MJ, Du J, Yu X, North WG: Evidence for expression of vasopressin V2 receptor mRNA in human lung. (hmdb.ca)
Aged animals showed an attenuated entrainment response to noradrenergic stimulation as well as decreased adrenergic receptor mRNA expression in target peripheral organs. (nature.com)
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)
Protein and mRNA expression of V1BR were very low compared with the V-2 receptor (V2R). (mtmt.hu)
NEW & NOTEWORTHY Although 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)

Desmopressin is a synthetic antidiuretic hormone with actions mimicking vasopressin. (medscape.com)

It may be initiated by differences in ligand-induced intermediate conformational states, as shown for the β 2 -adrenergic receptor. (aspetjournals.org)

Vasopressin Receptor Type-2 Mediated Signaling in Renal Cell Carcinoma Stimulates Stromal Fibroblast Activation. (bvsalud.org)
Vasopressin type-2 receptor (V2R) is ectopically expressed and plays a pathogenic role in clear cell renal cell carcinoma (ccRCC) tumor cells . (bvsalud.org)
To understand the regulation of vasopressin receptors in an animal model of hypertension, localization and age-related changes in renal arginine vasopressin (AVP) receptors in spontaneously hypertensive rats (SHR) were investigated using in vitro (macro) autoradiography and a radiolabeled receptor assay. (elsevierpure.com)
Autoradiography localized renal AVP V2 receptors to the distal tubules and collecting ducts in the medulla. (elsevierpure.com)
The radiolabeled receptor assay of the medulla membrane fraction revealed that the binding affinity of renal V2 receptors did not differ significantly between SHR and control Wistar-Kyoto rats in any age group. (elsevierpure.com)
These findings suggest that SHR have different developmental changes in kidney AVP receptors and that renal V2 receptors play a role in maintaining fluid homeostasis in SHR with established hypertension. (elsevierpure.com)

Then, Dr Plouffe completed a PhD in Neuroscience at University of Ottawa (ON, Canada) (2006-2011), where she identified the molecular mechanisms involved in the opposite regulation of dopamine D1 and D5 receptors by protein kinase C. Her work shed light on the mechanisms underlying the positive action of prefrontal cortex on motor activity and of the thalamic parafascicular nucleus on awareness. (qub.ac.uk)

An approach to rescue receptor function utilizes pharmacoperones or molecular chaperones, which are typically small molecules that rescue misfolded proteins to the cell surface. (wikipedia.org)
Subsequent mechanisms that may play a role include diversity of G proteins, scaffolding and signaling partners, and receptor oligomers. (aspetjournals.org)
As GPCRs represent the largest family of cell surface proteins, and control a vast repertoire of physiological functions, these receptors are the actual target of 30-50% of all prescribed drugs. (qub.ac.uk)
Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. (uams.edu)
Sequence comparison does not support an evolutionary link between halobacterial retinal proteins including bacteriorhodopsin and eukaryotic G-protein-coupled receptors. (springer.com)
Gi-proteins in vascular smooth muscle are coupled to α 2 -adrenoceptors . (cvphysiology.com)
Gq-proteins in vascular smooth muscle are coupled to α 1 -adrenoceptors (bind to norepinephrine ), ET A receptors (bind to endothelin-1), AT 1 receptors (bind to angiotensin II ), V 1 receptors (bind to vasopressin ), and muscarinic (M 3 ) receptors (bind to acetylcholine ). (cvphysiology.com)

Arg-vasopressin (AVP) is a nonapeptide homologous to Arg-vasotocin (AVT) in teleosts that has comparable affinity for the OT receptor. (frontiersin.org)
Using peptide analogs, a poor correlation was found between antagonism of oxytocin-induced calcium transients of LLC-PK1 cells and pig kidney V2 and rat liver V1 receptor affinity. (aspetjournals.org)
Its binding to Gs-protein-coupled β 2 -adrenoceptors versus Gq-protein-coupled α 1 -adrenoceptors is concentration dependent because β 2 -adrenoceptors have a higher affinity for epinephrine than α 1 -adrenoceptors. (cvphysiology.com)

R. The Arg8/D-Arg8 ligand-pair was further investigated to gain novel insights into the oxytocin/vasopressin peptide-receptor interaction, which led to the identification of key residues of the receptors that are important for ligand functionality and selectivity. (liverpool.ac.uk)
Ahlstedt J., Tran T.A., Strand S-E, Gram M., Åkerström B. Human Anti-Oxidation Protein A1M-A Potential Kidney Protection Agent in Peptide Receptor Radionuclide Therapy. (lu.se)

The concept of intrinsic efficacy has been enshrined in pharmacology for half of a century, yet recent data have revealed that many ligands can differentially activate signaling pathways mediated via a single G protein-coupled receptor in a manner that challenges the traditional definition of intrinsic efficacy. (aspetjournals.org)
Kim JY, Haastert PV, Devreotes PN (1996) Social senses: G-protein-coupled receptor signaling pathways in Dictyostelium discoideum . (springer.com)
Characterization of a functional V-1B vasopressin receptor in the male rat kidne evidence for cross talk between V-1B and V-2 receptor signaling pathways. (mtmt.hu)
Using original pharmaceutical tools, this study brings new data on the localization and signaling pathways of V1BR, highlights a cross talk between V1BR and V-2 receptor (V2R) in the inner medullary collecting duct, and suggests that V1BR may counterbalance in some pathophysiological conditions the antidiuretic effect triggered by V2R activation. (mtmt.hu)

In this work, in silico selection of DNA-aptamers to the receptor-binding domain (RBD) of the SARS-CoV-2 spike protein was performed using molecular modeling methods. (jyu.fi)
Her fields of interest include: G protein-coupled receptor signalling, biased signalling and selectivity, compartmentalised G protein signalling, bioluminescence resonance energy transfer (BRET)-based technology. (qub.ac.uk)
Schioth HB, Fredriksson R (2005) The GRAFS classification system of G-protein coupled receptors in comparative perspective. (springer.com)
Nordstrom KJ, Sallman Almen M, Edstam M et al (2011) Independent HHsearch, Needleman-Wunsch-based, and motif analyses reveal the overall hierarchy for most of the G protein-coupled receptor families. (springer.com)
Vasopressin receptors are G-protein coupled receptors that mediate coagulation factor release, platelet aggregation, vasoconstriction, release of antidiuresis and ACTH release etc. (glpbio.cn)
Two important mechanisms will be described here: 1) G-protein-coupled pathway, and 2) the nitric oxide-cGMP pathway. (cvphysiology.com)
The Gs-protein is coupled to several important receptors that bind vasodilator substances, among which are β 2 -adrenoceptors (bind to β 2 -agonists such as epinephrine and isoproterenol), A 2 purinergic receptors (bind to adenosine), and IP receptors (bind prostacyclin , PGI 2 ). (cvphysiology.com)
To summarize, the following agonists act directly on vascular smooth muscle through binding to their receptors, causing contraction via Gq-protein: norepinephrine, epinephrine, angiotensin II, endothelin-1, arginine vasopressin, and acetylcholine. (cvphysiology.com)

Vasopressin: Disturbed Secretion and Its Effects. (wikipedia.org)
The syndrome of inappropriate antidiuretic hormone secretion (SIADH) involves the continued secretion or action of arginine vasopressin (AVP) despite normal or increased plasma volume. (medscape.com)
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)
Vasopressin (antidiuretic hormone [ADH]) secretion increases despite a decrease in osmolality to maintain blood volume. (msdmanuals.com)

She also worked on the ghrelin receptor, involved in energy homeostasis and food intake, in collaboration with Prof Birgitte Holst (University of Copenhagen). (qub.ac.uk)
This study lead to the identification of the ghrelin receptor-induced biased signalling mediated by a new compound responsible for unique physiological outcomes observed in murine model. (qub.ac.uk)

We isolated the insect oxytocin/vasopressin orthologue inotocin from the black garden ant (Lasius niger), identified and cloned its cognate receptor and determined its pharmacological properties on the insect and human oxytocin/vasopressin receptors. (liverpool.ac.uk)

Association between opioid and dopamine receptor gene polymorphisms OPRM1rs1799971, DAT VNTR9-10 repeat allele, DRD1 rs4532 and DRD2 rs1799732 and alcohol dependence: an ethnicity oriented meta-analysis. (cdc.gov)

She started her journey in this exciting research field by investigating the molecular mechanisms involved in the angiotensin type 2 receptor (AT 2 R)-mediated neurite outgrowth as a MSc student (2003-2005). (qub.ac.uk)
Angiotensin-converting enzyme (ACE) converts Ang I into angiotensin II (Ang II) which acts on an angiotensin type 1 (AT1) and angiotensin type 2 (AT2) receptor. (hindawi.com)

Within this branch of research, I am studying: 1) the physiological and genomic responses of vertebrates to crude oil and its chemical derivatives, and 2) the influence of biotic and abiotic factors on metal bioavailability and toxicity in fish. (lsu.edu)
These observations could play an important role for development of oxytocin/vasopressin receptor modulators that would enable clear distinction of the physiological and pathological responses of the individual receptor subtypes. (liverpool.ac.uk)

Besides the heuristically interesting nature of functional selectivity, there is a clear impact on drug discovery, because this mechanism raises the possibility of selecting or designing novel ligands that differentially activate only a subset of functions of a single receptor, thereby optimizing therapeutic action. (aspetjournals.org)
It exhibited high V-1b/V-1a and V-1b/oxytocin selectivity for rat, human, and bovine receptors. (glpbio.cn)

diabetes insipidus: Types and causes: …in a gene known as AQP2 (aquaporin 2), which encodes a specific form of aquaporin. (britannica.com)

Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. (uams.edu)
Although ACh binds to M 3 receptors on both endothelial and vascular smooth muscle cells, if the endothelium is normal, then the formation of endothelial-derived NO and vasodilation overrides smooth muscle M 3 -mediated contraction. (cvphysiology.com)

Predictors of treatment retention and survival among methadone-maintained patients: A possible role for a functional delta opioid receptor gene variant. (cdc.gov)

The increase in cortisol may be interpreted as an overactivity of the stress hormone system, i.e. the hypothalamic-pituitary-adrenocortical (HPA) axis, on the basis of a dysfunctional glucocorticoid receptor (GR) feedback. (karger.com)

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)

Acetylcholine (ACh), whether administered intravascularly or released by cholinergic autonomic (parasympathetic) nerves, binds to muscarinic receptors (M 3 ) on the vascular endothelium, which stimulates the formation and release of NO as described above to produce vasodilation. (cvphysiology.com)

Voinsky I, Bennuri SC, Svigals J, Frye RE, Rose S, Gurwitz D. Peripheral Blood Mononuclear Cell Oxytocin and Vasopressin Receptor Expression Positively Correlates with Social and Behavioral Function in Children with Autism. (uams.edu)

Sibirskoe Medicinskoe Obozrenie , 2021 (2), 66-67. (jyu.fi)

A study in Wistar rats demonstrated that peripheral administration of both OT and AVP induced profound effects manifested as a reduction in body temperature and heart rate, and these changes were predominantly mediated by the AVP V1a receptor (V1aR) ( 23 ). (frontiersin.org)

In the kidney, AVPR2's primary property is to respond to arginine vasopressin by stimulating mechanisms that concentrate the urine and maintain water homeostasis in the organism. (wikipedia.org)

Furthermore, it showed a high V-1b/V-2 specificity for both bovine and human vasopressin receptors. (glpbio.cn)

We are working to determine the relative contributions of circadian function in vasopressin, VIP, kisspeptin and GnRH neurons in order to reveal the loci at which the clock controls ovulation. (umass.edu)

To uncover such molecules, we explored a unique strategy for ligand discovery that takes advantage of the evolutionary conservation of the 600-million-year-old oxytocin/vasopressin signalling system. (liverpool.ac.uk)

In collaboration with Prof Ralf Jockers from Institut Cochin (France), she investigated the signalling parameters of the melatonin type 2 receptor preventing development of type 2 diabetes. (qub.ac.uk)

The precise mechanism of action is unknown but is believed to involve interaction with gamma-aminobutyric acid (GABA) receptors at binding domains close to, or allosterically coupled to, benzodiazepine receptors. (medscape.com)
We also found small numbers of AVP-binding sites within glomeruli, possibly representing V1 receptors in the mesangium. (elsevierpure.com)
The main mechanism of action proposed for local anesthetics (LAs) is related to the binding of these substances to sodium channels receptors (Na+), leading to the reduction or elimination of the permeability of these ions and interruption of the nervous conduction 3-4 . (bvsalud.org)

Although the lack of estrogen receptor β (ERβ) is a risk factor for the development of inflammatory bowel disease (IBD) and psychiatric disorders, the underlying cellular and molecular mechanisms are not fully understood. (biomedcentral.com)

Both monogamous and non-monogamous species exist within Eulemur, a genus of strepsirrhine primate, offering a rare opportunity to broaden a comparative perspective on oxytocin and vasopressin neurocircuitry with increased evolutionary relevance to humans. (brainresearchlab.com)

A 51-year-old male Type 2 diabetic patient was referred to our department for infected foot ulcer. (endocrine-abstracts.org)

The brain has shown the presence of various components of brain RAS such as angiotensinogen (AGT), converting enzymes, angiotensin (Ang), and specific receptors (ATR). (hindawi.com)

Anatomy17

Organisms6

Diseases9

Chemicals and Drugs43

Analytical, Diagnostic and Therapeutic Techniques and Equipment3

Psychiatry and Psychology3

Phenomena and Processes15

Agonist9

Antagonist4

Arginine va2

Antagonists4

Selective2

Oxytocin receptors3

Neuropeptide3

Tolvaptan2

GPCR5

Antidiuretic hormone receptor1

AVPR24

Mammalian2

MRNA5

Desmopressin1

Adrenergic receptor1

Renal6

Regulation1

Proteins7

Affinity3

Peptide receptor2

Pathways4

Protein8

Secretion4

Ghrelin receptor2

Cognate receptor1

Dopamine receptor1

Angiotensin type2

Physiological2

Selectivity2

Diabetes insipidus1

Vascular smooth2

Opioid1

Pituitary1

Second messeng1

Binds1

Correlates1

20211

Rats1

Homeostasis1

Human1

Kisspeptin1

Ligand1

Melatonin1

Binding3

Mechanisms1

Humans1

Type1

Angiotensinogen1