Page last updated: 2024-08-07 18:36:16
Vasopressin V1b receptor
A vasopressin V1b receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P47901]
Synonyms
V1bR;
AVPR V1b;
AVPR V3;
Antidiuretic hormone receptor 1b;
Vasopressin V3 receptor
Research
Bioassay Publications (18)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (5.56) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (16.67) | 29.6817 |
| 2010's | 14 (77.78) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (14)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Synthesis of oxytocin derivatives lipidated via a carbonate or carbamate linkage as a long-acting therapeutic agent for social impairment-like behaviors.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like Behaviors.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
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
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
Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like Behaviors.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
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
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
[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
The characterization of a novel V1b antagonist lead series.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 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
Potent and selective oxindole-based vasopressin 1b receptor antagonists with improved pharmacokinetic properties.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 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
Development of a Highly Potent Analogue and a Long-Acting Analogue of Oxytocin for the Treatment of Social Impairment-Like Behaviors.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
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 kinase C binding | molecular function | Binding to protein kinase C. [GOC:jl] |
| 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 3 target(s):
| Target | Category | Definition |
|---|
| endosome | cellular component | A vacuole to which materials ingested by endocytosis are delivered. [ISBN:0198506732, PMID:19696797] |
| 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] |
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 13 target(s):
| Target | Category | Definition |
|---|
| 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] |
| activation of phospholipase C activity | biological process | The initiation of the activity of the inactive enzyme phospolipase C as the result of The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand. [GOC:dph, GOC:mah, GOC:tb, PMID:8280098] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| positive regulation of phospholipase A2 activity | biological process | Any process that activates or increases the activity of the enzyme phospholipase A2. [GOC:mah] |
| regulation of cell population proliferation | biological process | Any process that modulates the frequency, rate or extent of cell proliferation. [GOC:jl] |
| positive regulation of MAPK cascade | biological process | Any process that activates or increases the frequency, rate or extent of signal transduction mediated by the MAPK cascade. [GOC:go_curators] |
| symbiont entry into host cell | biological process | The process by which a symbiont breaches the plasma membrane or cell envelope and enters the host cell. The process ends when the symbiont or its genome is released into the host cell. [GOC:jl] |
| positive regulation of inositol phosphate biosynthetic process | biological process | Any process that increases the rate, frequency or extent of inositol phosphate biosynthesis. Inositol phosphate biosynthetic processes are the chemical reactions and pathways resulting in the formation of an inositol phosphate, 1,2,3,4,5,6-cyclohexanehexol, with one or more phosphate groups attached. [GOC:dph, GOC:tb] |
| positive regulation of arachidonic acid secretion | biological process | Any process that increases the rate, frequency, or extent of arachidonic acid secretion, the controlled release of arachidonic acid from a cell or a tissue. [GOC:BHF, GOC:dph, GOC:tb] |
| transport across blood-brain barrier | biological process | The directed movement of substances (e.g. macromolecules, small molecules, ions) through the blood-brain barrier. [GOC:aruk, GOC:bc, PMID:29377008] |
| 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] |
| 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] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |