Page last updated: 2024-08-07 16:26:08
Oxytocin receptor
An oxytocin receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30559]
Synonyms
OT-R
Research
Bioassay Publications (44)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 5 (11.36) | 18.2507 |
2000's | 11 (25.00) | 29.6817 |
2010's | 27 (61.36) | 24.3611 |
2020's | 1 (2.27) | 2.80 |
Compounds (19)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
way-151932 | Homo sapiens (human) | Kinact | 0.4880 | 2 | 2 |
l 371257 | Homo sapiens (human) | Kinact | 0.0009 | 1 | 1 |
[no title available]Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
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
Building bridges for highly selective, potent and stable oxytocin and vasopressin analogs.Bioorganic & medicinal chemistry, , 07-15, Volume: 26, Issue:11, 2018
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
Hybrid peptide-small molecule oxytocin analogs are potent and selective agonists of the oxytocin receptor.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Potent and selective oxytocin receptor agonists without disulfide bridges.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Design and Characterization of Superpotent Bivalent Ligands Targeting Oxytocin Receptor Dimers via a Channel-Like Structure.Journal of medicinal chemistry, , 08-11, Volume: 59, Issue:15, 2016
Systematic N-methylation of oxytocin: Impact on pharmacology and intramolecular hydrogen bonding network.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
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
Modulating oxytocin activity and plasma stability by disulfide bond engineering.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Synthesis and biological activity of oxytocin analogues containing conformationally-restricted residues in position 7.European journal of medicinal chemistry, , Volume: 42, Issue:6, 2007
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
Synthesis of oxytocin antagonists containing conformationally constrained amino acids in position 2.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 9, Issue:5, 1999
Hybrid peptide-small molecule oxytocin analogs are potent and selective agonists of the oxytocin receptor.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Potent and selective oxytocin receptor agonists without disulfide bridges.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Systematic N-methylation of oxytocin: Impact on pharmacology and intramolecular hydrogen bonding network.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
New, potent, and selective peptidic oxytocin receptor agonists.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
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
Modulating oxytocin activity and plasma stability by disulfide bond engineering.Journal of medicinal chemistry, , Dec-23, Volume: 53, Issue:24, 2010
Investigation of pyrazolo-sulfonamides as putative small molecule oxytocin receptor agonists.European journal of medicinal chemistry, , Aug-18, Volume: 136, 2017
Discovery and optimization of highly ligand-efficient oxytocin receptor antagonists using structure-based drug design.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
The discovery of GSK221149A: a potent and selective oxytocin antagonist.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 18, Issue:1, 2008
2,5-diketopiperazines as potent, selective, and orally bioavailable oxytocin antagonists. 3. Synthesis, pharmacokinetics, and in vivo potency.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists.Journal of medicinal chemistry, , Dec-01, Volume: 48, Issue:24, 2005
[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
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
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
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
Design and optimization of potent, selective antagonists of Oxytocin.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 18, Issue:15, 2008
Identification of potent and selective oxytocin antagonists. Part 1: indole and benzofuran derivatives.Bioorganic & medicinal chemistry letters, , May-20, Volume: 12, Issue:10, 2002
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.Bioorganic & medicinal chemistry letters, , May-20, Volume: 12, Issue:10, 2002
Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.Journal of medicinal chemistry, , Nov-10, Volume: 38, Issue:23, 1995
The characterization of a novel V1b antagonist lead series.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 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
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
Discovery of SHR1653, a Highly Potent and Selective OTR Antagonist with Improved Blood-Brain Barrier Penetration.ACS medicinal chemistry letters, , Jun-13, Volume: 10, Issue:6, 2019
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
[no title available]Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
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
Conformationally rigid derivatives of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin-1a receptors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
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
Targets for Drug Therapy for Autism Spectrum Disorder: Challenges and Future Directions.Journal of medicinal chemistry, , 11-22, Volume: 60, Issue:22, 2017
Potent and selective oxytocin receptor agonists without disulfide bridges.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Flexible analogues of WAY-267,464: Synthesis and pharmacology at the human oxytocin and vasopressin 1a receptors.European journal of medicinal chemistry, , Jan-27, Volume: 108, 2016
Enables
This protein enables 4 target(s):
Target | Category | Definition |
peptide hormone binding | molecular function | Binding to a peptide with hormonal activity in animals. [GOC:jl, ISBN:0198506732] |
peptide binding | molecular function | Binding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl] |
vasopressin receptor activity | molecular function | Combining with vasopressin to initiate a change in cell activity. [GOC:ai] |
oxytocin receptor activity | molecular function | Combining with oxytocin to initiate a change in cell activity. [GOC:ai] |
Located In
This protein is located in 4 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] |
microvillus | cellular component | Thin cylindrical membrane-covered projections on the surface of an animal cell containing a core bundle of actin filaments. Present in especially large numbers on the absorptive surface of intestinal cells. [ISBN:0815316194] |
adherens junction | cellular component | A cell-cell junction composed of the epithelial cadherin-catenin complex. The epithelial cadherins, or E-cadherins, of each interacting cell extend through the plasma membrane into the extracellular space and bind to each other. The E-cadherins bind to catenins on the cytoplasmic side of the membrane, where the E-cadherin-catenin complex binds to cytoskeletal components and regulatory and signaling molecules. [GOC:aruk, GOC:bc, GOC:mah, ISBN:0198506732, PMID:17854762, PMID:20571587, PMID:21422226, PMID:28096264] |
apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
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 37 target(s):
Target | Category | Definition |
suckling behavior | biological process | Specific behavior of a newborn or infant mammal that results in the derivation of nourishment from the breast. [GOC:dph, GOC:pr] |
response to amphetamine | 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 an amphetamine stimulus. Amphetamines consist of a group of compounds related to alpha-methylphenethylamine. [GOC:dph, GOC:ef] |
muscle contraction | biological process | A process in which force is generated within muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. [GOC:ef, GOC:mtg_muscle, ISBN:0198506732] |
cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
heart development | biological process | The process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948] |
lactation | biological process | The regulated release of milk from the mammary glands and the period of time that a mother lactates to feed her young. [ISBN:0198506732] |
memory | biological process | The activities involved in the mental information processing system that receives (registers), modifies, stores, and retrieves informational stimuli. The main stages involved in the formation and retrieval of memory are encoding (processing of received information by acquisition), storage (building a permanent record of received information as a result of consolidation) and retrieval (calling back the stored information and use it in a suitable way to execute a given task). [GOC:curators, ISBN:0582227089] |
response to xenobiotic stimulus | 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 stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
positive regulation of norepinephrine secretion | biological process | Any process that increases the frequency, rate or extent of the regulated release of norepinephrine. [GOC:dph, GOC:tb] |
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] |
positive regulation of synaptic transmission, GABAergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of GABAergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter gamma-aminobutyric acid (GABA). [GOC:mah] |
response to estradiol | 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 stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123] |
response to progesterone | 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 progesterone stimulus. [GOC:sl] |
response to anoxia | 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 stimulus indicating a decline in oxygen levels to trace amounts, <0.1%. [GOC:kmv] |
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] |
social behavior | biological process | Behavior directed towards society, or taking place between members of the same species. Occurs predominantly, or only, in individuals that are part of a group. [GOC:jh2, PMID:12848939, Wikipedia:Social_behavior] |
response to cocaine | 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 cocaine stimulus. Cocaine is a crystalline alkaloid obtained from the leaves of the coca plant. [GOC:ef, GOC:jl] |
maternal behavior | biological process | Female behaviors associated with the care and rearing of offspring. [GOC:curators] |
sperm ejaculation | biological process | The expulsion of seminal fluid, thick white fluid containing spermatozoa, from the male genital tract. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
eating behavior | biological process | The specific behavior of an organism relating to the intake of food, any substance (usually solid) that can be metabolized by an organism to give energy and build tissue. [GOC:jl, GOC:pr, PMID:19361967] |
response to peptide hormone | 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 peptide hormone stimulus. A peptide hormone is any of a class of peptides that are secreted into the blood stream and have endocrine functions in living animals. [PMID:11027914, PMID:15134857, Wikipedia:Peptide_hormone] |
estrous cycle | biological process | A type of ovulation cycle, which occurs in most mammalian therian females, where the endometrium is resorbed if pregnancy does not occur. [GOC:jl, Wikipedia:Estrous_cycle] |
positive regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is increased. [GOC:go_curators, GOC:mtg_cardio] |
digestive tract development | biological process | The process whose specific outcome is the progression of the digestive tract over time, from its formation to the mature structure. The digestive tract is the anatomical structure through which food passes and is processed. [GOC:go_curators] |
positive regulation of synapse assembly | biological process | Any process that activates, maintains or increases the frequency, rate or extent of synapse assembly, the aggregation, arrangement and bonding together of a set of components to form a synapse. [GOC:ai, GOC:pr] |
positive regulation of synaptic transmission, glutamatergic | biological process | Any process that activates, maintains or increases the frequency, rate or extent of glutamatergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter glutamate. [GOC:ai] |
positive regulation of penile erection | biological process | Any process that increases the rate, frequency or extent of penile erection. Penile erection is the hardening, enlarging and rising of the penis which often occurs in the sexually aroused male and enables sexual intercourse. Achieved by increased inflow of blood into the vessels of erectile tissue, and decreased outflow. [GOC:dph, GOC:tb] |
ERK1 and ERK2 cascade | biological process | A MAPK cascade containing at least the ERK1 or ERK2 MAP kinases. It starts with the activation of a MAP3K, and the consecutive activation of a MPK2K and of ERK1 or ERK2. The cascade can also contain an additional tier: the upstream MAP4K. The kinases in each tier phosphorylate and activate the kinase in the downstream tier. The ERK1/ERK2 cascade is activated by mitogens, growth factors, G protein-coupled receptors, and results in cellular responses such as cell proliferation, cell differentiation and development. [PMID:20811974, PMID:23125017, PMID:28903453] |
positive regulation of uterine smooth muscle contraction | biological process | Any process that increases the frequency, rate or extent of uterine smooth muscle contraction. [GOC:go_curators] |
positive regulation of cold-induced thermogenesis | biological process | Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809] |
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] |
female pregnancy | biological process | The set of physiological processes that allow an embryo or foetus to develop within the body of a female animal. It covers the time from fertilization of a female ovum by a male spermatozoon until birth. [ISBN:0192800825] |
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] |
maternal process involved in parturition | biological process | A reproductive process occurring in the mother that results in birth. [GOC:dph] |
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] |