Page last updated: 2024-08-07 16:25:09
Vasopressin V2 receptor
A vasopressin V2 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30518]
Synonyms
V2R;
AVPR V2;
Antidiuretic hormone receptor;
Renal-type arginine vasopressin receptor
Research
Bioassay Publications (44)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (2.27) | 18.7374 |
| 1990's | 4 (9.09) | 18.2507 |
| 2000's | 17 (38.64) | 29.6817 |
| 2010's | 18 (40.91) | 24.3611 |
| 2020's | 4 (9.09) | 2.80 |
Compounds (26)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| arginine vasopressin | Homo sapiens (human) | Kact | 0.0003 | 1 | 1 |
| way-151932 | Homo sapiens (human) | Kact | 0.0095 | 2 | 2 |
Oral oxytocin antagonists.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Selective fluorescent nonpeptidic antagonists for vasopressin V₂ GPCR: application to ligand screening and oligomerization assays.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.Bioorganic & medicinal chemistry, , Volume: 7, Issue:8, 1999
New analgesic drugs derived from phencyclidine.Journal of medicinal chemistry, , Volume: 24, Issue:5, 1981
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 17, Issue:21, 2007
Next-generation spirobenzazepines: identification of RWJ-676070 as a balanced vasopressin V1a/V2 receptor antagonist for human clinical studies.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 15, Issue:22, 2005
Potent nonpeptide vasopressin receptor antagonists based on oxazino- and thiazinobenzodiazepine templates.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 14, Issue:11, 2004
Synthesis and biological evaluation of novel indoloazepine derivatives as non-peptide vasopressin V2 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-24, Volume: 13, Issue:4, 2003
Bridged bicyclic vasopressin receptor antagonists with V(2)-selective or dual V(1a)/V(2) activity.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
The synthesis and vasopressin (AVP) antagonist activity of a novel series of N-aroyl-2,4,5,6-tetrahydropyrazolo[3,4-d]thieno[3,2-b]azepines.Bioorganic & medicinal chemistry letters, , Apr-17, Volume: 10, Issue:8, 2000
The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery.Bioorganic & medicinal chemistry letters, , Apr-17, Volume: 10, Issue:8, 2000
4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 9, Issue:13, 1999
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
Long Residence Time at the Vasopressin VJournal of medicinal chemistry, , 06-09, Volume: 65, Issue:11, 2022
Benzodiazepine Derivatives as Potent Vasopressin VJournal of medicinal chemistry, , 07-14, Volume: 65, Issue:13, 2022
Synthesis and Characterization of New VJournal of medicinal chemistry, , 07-22, Volume: 64, Issue:14, 2021
Yohimbine as a Starting Point to Access Diverse Natural Product-Like Agents with Re-programmed Activities against Cancer-Relevant GPCR Targets.Bioorganic & medicinal chemistry, , 07-15, Volume: 28, Issue:14, 2020
Novel design of nonpeptide AVP V(2) receptor agonists: structural requirements for an agonist having 1-(4-aminobenzoyl)-2,3,4, 5-tetrahydro-1H-1-benzazepine as a template.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist.Bioorganic & medicinal chemistry, , Volume: 7, Issue:8, 1999
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.Bioorganic & medicinal chemistry, , 07-15, Volume: 26, Issue:11, 2018
Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay.Journal of medicinal chemistry, , Mar-12, Volume: 58, Issue:5, 2015
New, potent, and selective peptidic oxytocin receptor agonists.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Synthesis and characterization of fluorescent antagonists and agonists for human oxytocin and vasopressin V(1)(a) receptors.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.Bioorganic & medicinal chemistry, , 07-15, Volume: 26, Issue:11, 2018
New, potent, and selective peptidic oxytocin receptor agonists.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
A comparative protease stability study of synthetic macrocyclic peptides that mimic two endocrine hormones.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 23, Issue:4, 2013
Selective fluorescent nonpeptidic antagonists for vasopressin V₂ GPCR: application to ligand screening and oligomerization assays.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
New, potent, selective, and short-acting peptidic V1a receptor agonists.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Design, synthesis, and pharmacological characterization of fluorescent peptides for imaging human V1b vasopressin or oxytocin receptors.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropyJournal of medicinal chemistry, , Aug-15, Volume: 45, Issue:17, 2002
[no title available]Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
New, potent, and selective peptidic oxytocin receptor agonists.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4.Journal of medicinal chemistry, , Apr-22, Volume: 47, Issue:9, 2004
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
New benzylureas as a novel series of potent, nonpeptidic vasopressin V2 receptor agonists.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Identification and synthesis of major metabolites of Vasopressin V2-receptor agonist WAY-151932, and antagonist, Lixivaptan.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 17, Issue:21, 2007
Pyridobenzodiazepines: a novel class of orally active, vasopressin V2 receptor selective agonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Oral oxytocin antagonists.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Carbon-11 N-methyl alkylation of L-368,899 and in vivo PET imaging investigations for neural oxytocin receptors.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 23, Issue:3, 2013
Oral oxytocin antagonists.Journal of medicinal chemistry, , Sep-23, Volume: 53, Issue:18, 2010
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Synthesis and SAR studies of novel 2-(4-oxo-2-aryl-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Pyridyl-2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists: synthesis, pharmacokinetics, and in vivo potency.Journal of medicinal chemistry, , Jan-26, Volume: 55, Issue:2, 2012
LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
New, potent, and selective peptidic oxytocin receptor agonists.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| vasopressin receptor activity | molecular function | Combining with vasopressin to initiate a change in cell activity. [GOC:ai] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| peptide binding | molecular function | Binding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl] |
Located In
This protein is located in 8 target(s):
| Target | Category | Definition |
|---|
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
| Golgi apparatus | cellular component | A membrane-bound cytoplasmic organelle of the endomembrane system that further processes the core oligosaccharides (e.g. N-glycans) added to proteins in the endoplasmic reticulum and packages them into membrane-bound vesicles. The Golgi apparatus operates at the intersection of the secretory, lysosomal, and endocytic pathways. [ISBN:0198506732] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| endocytic vesicle | cellular component | A membrane-bounded intracellular vesicle formed by invagination of the plasma membrane around an extracellular substance. Endocytic vesicles fuse with early endosomes to deliver the cargo for further sorting. [GOC:go_curators, PMID:19696797] |
| clathrin-coated endocytic vesicle membrane | cellular component | The lipid bilayer surrounding a clathrin-coated endocytic vesicle. [GOC:mah] |
| perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 15 target(s):
| Target | Category | Definition |
|---|
| positive regulation of systemic arterial blood pressure | biological process | The process that increases the force with which blood travels through the systemic arterial circulatory system. [GOC:mtg_cardio] |
| renal water retention | biological process | The process in which renal water excretion is decreased. [GOC:mtg_cardio] |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
| activation of adenylate cyclase activity | biological process | Any process that initiates the activity of the inactive enzyme adenylate cyclase. [GOC:ai] |
| hemostasis | biological process | The stopping of bleeding (loss of body fluid) or the arrest of the circulation to an organ or part. [ISBN:0198506732] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| telencephalon development | biological process | The process whose specific outcome is the progression of the telencephalon over time, from its formation to the mature structure. The telencephalon is the paired anteriolateral division of the prosencephalon plus the lamina terminalis from which the olfactory lobes, cerebral cortex, and subcortical nuclei are derived. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, PMID:12626695] |
| response to cytokine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cytokine stimulus. [GOC:sl] |
| positive regulation of intracellular signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of intracellular signal transduction. [GOC:BHF, GOC:dph, GOC:signaling, GOC:tb, GOC:TermGenie] |
| cellular response to hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hormone stimulus. [GOC:mah] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| regulation of systemic arterial blood pressure by vasopressin | biological process | The regulation of blood pressure mediated by the signaling molecule vasopressin. Vasopressin is produced in the hypothalamus, and affects vasoconstriction, and renal water transport. [GOC:mtg_cardio, ISBN:0721643949] |