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OX2R Agonist
OX-201 is a potent OX2R agonist that effectively crosses the blood-brain barrier, exhibiting an EC50 of 8.0 nM. This compound stimulates OX2R, leading to increased wakefulness and neuronal activation. Additionally, OX-201 facilitates the release of activity-dependent tau protein from neurons into the interstitial fluid of hippocampal tissues. It is a valuable tool for research into Alzheimer's disease and tauopathies. -
OX2R Antagonist
OX2-2303 is a potent and selective antagonist of the orexin-2 receptor (OX2R), demonstrating exceptional binding affinity with a Ki value of 0.1 nM and over 890-fold selectivity for OX2R compared to OX1R. This compound is valuable for applications in central nervous system (CNS) research, particularly as a positron emission tomography (PET) radioligand, enabling the study of OX2R's role in various neurological processes. -
OX2R Agonist
Cleminorexton is an orally active agonist of the orexin-2 receptor (OX2R), exhibiting a pEC50 value between 9 and 10.4. This compound is primarily utilized in research related to narcolepsy and other disorders characterized by orexin deficiency and excessive daytime sleepiness. Its modulation of OX2R activity makes it a valuable tool for studying sleep-wake regulation and potential therapeutic interventions. -
Orexin Receptor Modulator
Orexin receptor modulator-1 is a selective modulator of orexin receptors, playing a vital role in the regulation of arousal, wakefulness, and appetite. It demonstrates significant biological activity in the context of substance addiction, anxiety, depression, and various stress-related disorders. This compound serves as a valuable tool for investigating the pathophysiology of disorders such as post-traumatic stress disorder, panic disorder, and seasonal affective disorder, as well as the modulation of pain and hypertension. -
OX2R Agonist
Ledasorexton is a potent oral agonist of the OX2 receptor (OX2R), exhibiting an EC50 of 0.99 nM. This compound has been demonstrated to induce wakefulness and promote alertness, making it a valuable tool for research into sleep regulation and associated disorders. Its specificity for the OX2R highlights its potential applications in studying neurobiology and pharmacology related to sleep and wakefulness. -
Orexin Receptor Agonist
Orexin receptor activator-1 is an agonist for the orexin receptor. This compound exhibits biological activity by modulating orexin signaling pathways, making it valuable for studying orexin-related disorders such as narcolepsy and obesity. Its application extends to research on sleep regulation and energy homeostasis, contributing to the understanding of various neurophysiological processes. -
OX2R Agonist
OX2R-IN-3 is a potent agonist of the type 2 orexin receptor (OX2R) with an EC50 value of less than 100 nM. This compound demonstrates significant biological activity in modulating orexin signaling pathways, making it a valuable tool for research in sleep disorders, energy homeostasis, and neurodegenerative diseases. OX2R-IN-3 can facilitate the exploration of OX2R-related functions in various physiological and pathological contexts. -
OXR Agonist
YNT-3708 is an orexin receptor (OXR) agonist that demonstrates selective activation of OX1R and OX2R. It has EC50 values of 14.6 nM for OX1R and 277 nM for OX2R, making it a valuable tool for studying orexin signaling pathways. This compound is primarily utilized in research applications related to sleep regulation, appetite control, and neurodegenerative diseases. -
OX2R Antagonist
Fumiporexant is a selective antagonist of the Orexin receptor 2 (OX2R), demonstrating oral bioavailability and effective penetration into the brain. This compound modulates the sleep-wake cycle and influences emotion-related pathways within the central nervous system. Fumiporexant is of significant interest in the study of neurological disorders, particularly insomnia and major depressive disorder. -
Orexin Receptor Activator
Xenopus orexin A acts as a potent agonist of the orexin receptor OX1R, functioning as a neuropeptide that binds to G-protein-coupled receptors. This endogenous ligand plays a critical role in modulating various physiological processes, including appetite regulation and arousal. Research applications of Xenopus orexin A include studying energy homeostasis, sleep-wake cycles, and potential implications in metabolic disorders. -
OX2R Antagonist
Orexin receptor antagonist 4 is a potent and selective antagonist of the orexin 2 receptor (OX2R), exhibiting an IC50 of 4.27 nM. This compound demonstrates a notable 61-fold selectivity for OX2R over the orexin 1 receptor (OX1R), which has an IC50 of 295 nM. Orexin receptor antagonist 4 is valuable for research applications exploring the role of orexin signaling in sleep regulation, energy metabolism, and various neurobiological processes. -
Orexin Receptor Agonist
Xenopus orexin B is a neuropeptide that acts as an agonist for the orexin receptor, specifically OX2R. This compound plays a crucial role in regulating various physiological processes, including arousal, appetite, and energy homeostasis. Its ability to activate orexin receptors makes it a valuable tool for research investigating sleep-wake cycles, metabolic disorders, and neurodegenerative diseases. -
Orexin Receptor (OX Receptor) Agonist
Orexin B (human) is an endogenous agonist that selectively targets the Orexin receptors, OX1 and OX2, with inhibition constants (Kis) of 420 nM and 36 nM, respectively. This compound plays a critical role in regulating arousal, appetite, and energy homeostasis. Orexin B is widely used in research applications focused on sleep disorders, metabolic syndromes, and neurodegenerative diseases, making it an essential tool for understanding Orexin signaling pathways. -
OX2R Antagonist
OX2R-IN-1 is a selective antagonist of the OX2 receptor (OX2R), exhibiting a low cytotoxicity profile. With an IC50 value of 484 μM, it serves as a potential binder for OX2R studies. Notably, OX2R-IN-1 demonstrates the ability to penetrate the blood-brain barrier (BBB) and possesses a short half-life, making it suitable for research applications targeting central nervous system functions and disorders. -
RNAi
DMTr-2'-O-C16-rC(Ac)-3'-CE-phosphoramidite is an RNAi agent that specifically targets and inhibits Ataxin-2 (ATXN2). This compound plays a critical role in research focused on ATXN2-associated neurological disorders, facilitating the study of gene silencing mechanisms and potential therapeutic interventions. Its application may enhance understanding of disease pathways related to ATXN2. -
OX1R Antagonist
Orexin receptor antagonist 7 selectively targets the orexin receptor 1 (OX1R) with a Ki value of 4.05 nM, demonstrating potent antagonistic activity. This compound shows negligible affinity for the orexin receptor 2 (OX2R) and minimal binding to opioid receptors (μ, δ, κ) with Ki values exceeding 1,000 nM. Orexin receptor antagonist 7 is suitable for research applications focused on opioid addiction and the elucidation of orexin-related pathways in various physiological and pathological contexts. -
OX1 Receptor Antagonist
Rocavorexant is a selective antagonist of the orexin-1 receptor (OX1) with a pIC50 of 9.1 for human OX1 and a pIC50 of 6.0 for human OX2. This compound effectively inhibits the signaling pathways associated with orexin receptors, making it a valuable tool for investigating sleep disorders, appetite regulation, and related neurological conditions. Rocavorexant is utilized in research studies aimed at understanding the physiological roles of orexin signaling and for the development of therapeutic strategies targeting these pathways. -
OX2R Agonist
OX2R Agonist 1 is a selective agonist of the orexin receptor 2 (OX2R), exhibiting an effective concentration (EC50) of less than 100 nM. This compound is instrumental in studying the neurobiology of sleep regulation and is particularly relevant for research focused on excessive daytime sleepiness and narcolepsy. Its potent biological activity positions it as a valuable tool in the exploration of treatments for sleep disorders. -
OX1 Antagonist
Orexin receptor antagonist 6 selectively targets the orexin 1 receptor (OX1) with a potent Ki of 8.5 nM and demonstrates more than 1180-fold selectivity for the OX2 receptor. This compound does not elicit conditioned place preference (CPP) or aversive effects and effectively inhibits CPP induced by psychoactive substances. Orexin receptor antagonist 6 is a valuable tool for investigating the role of orexin signaling in neurological diseases and related research applications. -
Orexin 1/2 Receptor Antagonist
DORA 42 is a dual antagonist of the orexin 1 and orexin 2 receptors. It demonstrates significant efficacy in promoting sleep in rat models, highlighting its potential utility in insomnia research. This compound serves as an important tool for studying the role of orexin receptors in sleep regulation and related disorders. -
OX Receptor Antagonist
MK-8133 is a selective orexin-2 receptor antagonist that inhibits orexin signaling pathways. It has demonstrated efficacy in the modulation of sleep-wake cycles, making it a valuable tool for researching insomnia and other sleep disorders. This compound can be utilized in various experimental models to investigate the role of orexin in sleep regulation and potential therapeutic interventions. -
Antioxidant
Ethoxyquin dimer is a dimeric form of the compound Ethoxyquin, functioning primarily as an antioxidant. This compound demonstrates enhanced accumulation in liver and adipose tissues relative to its monomer counterpart. Research indicates that concentrations exceeding 10 mg/kg can lead to hepatotoxicity in mice, making it a significant consideration in studies of oxidative stress and tissue-specific accumulation. -
Oxytocin Receptor Agonist
LIT-001 is a selective nonpeptide agonist of the oxytocin receptor, exhibiting an EC50 of 55 nM and a Ki of 226 nM. This compound has demonstrated the ability to enhance social interaction in preclinical mouse models of autism, making it a valuable tool for research into social behavior modulation and potential therapeutic applications in neurodevelopmental disorders. LIT-001 provides a unique avenue for exploring the role of oxytocin signaling in various neurobiological contexts. -
Oxytocin Receptor Antagonist
Erlosiban is a potent oxytocin receptor antagonist that exhibits oral bioactivity. By inhibiting the increase in intracellular calcium concentration, Erlosiban effectively reduces uterine smooth muscle contraction. This compound is primarily utilized in research related to premature birth and enhancing embryo implantation and pregnancy rates in assisted reproductive technologies. -
Oxytocin Receptor Agonist
Merotocin is a selective agonist of the oxytocin receptor, known for its short-acting properties. This peptidic compound primarily enhances lactation by promoting milk ejection through stimulation of the mammary glands. Merotocin is utilized in research aimed at understanding lactation dynamics and the physiological roles of oxytocin in reproductive biology. -
Oxytocin Receptor Antagonist
L-367773 is a selective antagonist of the oxytocin receptor, demonstrating Ki values of 26 nM for the rat uterine oxytocin receptor and 61 nM for the human uterine oxytocin receptor. This compound effectively inhibits oxytocin-stimulated uterine contractions, making it a valuable tool for research related to reproductive biology and uterine physiology. Its oral bioactivity further enhances its utility in pharmacological studies. -
Oxytocin Receptor Agonist
Carbetocin acetate is an oxytocin receptor agonist known for its high affinity with a Ki of 7.1 nM. This compound binds effectively to the chimeric N-terminus of the oxytocin receptor with a Ki of 1.17 μM. Carbetocin acetate holds potential for applications in postpartum hemorrhage research and is capable of crossing the blood-brain barrier, demonstrating antidepressant-like effects through the activation of central nervous system oxytocin receptors. -
Tocolytic Agent
5β-Dihydroprogesterone (5βDHP) is a metabolite of Progesterone that functions as a tocolytic agent. It exerts its biological activity by binding to the oxytocin receptor, subsequently diminishing oxytocin-induced calcium signaling. This property positions 5βDHP as a valuable reagent for research in obstetrics and reproductive biology, particularly in studies focused on the modulation of uterine contractions. -
Oxytocin Derivative
[Glu4]-Oxytocin is a synthetic derivative of oxytocin designed to facilitate the study of the conformational properties of "oxytocin-like" peptides in aqueous environments. This compound retains the biological activity of oxytocin, making it suitable for research applications in neurobiology and endocrinology. Its unique structure allows for enhanced investigation into the interactions and mechanisms of oxytocin-related signaling pathways. -
Oxytocin Receptor (OTR) Agonist
WAY-267464 is a non-peptide agonist targeting the oxytocin receptor (OTR). It has been shown to impair social recognition memory in rat models, likely through its antagonistic action on the vasopressin 1A receptor. This compound is relevant for research into psychiatric disorders, including autism spectrum disorder, schizophrenia, and social anxiety disorder. -
Oxytocin Antagonist
L-372662 is a potent, orally active non-peptide antagonist of the oxytocin receptor (OTR). It has a Ki value of 4.8 nM and demonstrates high affinity with Kd values of 5.8 nM for wild-type OTR and 73 nM for the [A318G] variant. This compound exhibits selectivity for OTR over the vasopressin 1a receptor (V1aR), making it a valuable tool in research applications related to neuroendocrine regulation and social behavior. -
OXTR Agonist
TC OT 39 is a synthetic analog of oxytocin and a selective agonist of the oxytocin receptor (OXTR), demonstrating an EC50 value of 180 nM. This compound also acts as an Avprla vasopressin receptor antagonist with a Ki value of 330 nM. TC OT 39 is noted for its sedative effects in mouse models, making it a valuable tool for research into neuropsychological and behavioral studies involving the oxytocin system. -
Vasoconstrictor Agent
[Arg8]-Vasotocin is a neurohypophyseal peptide that functions as a potent vasoconstrictor agent. This compound mimics the structure of vasopressin, enhancing its biological activity in regulating vascular tone and blood pressure. It is widely used in research to study cardiovascular physiology, neuroendocrine signaling, and the role of vasopressin-related peptides in various biological processes. -
Oxytocin Analogue
[Leu3]-Oxytocin is an oxytocin analogue characterized by a substitution of leucine at the third position of the peptide sequence. This modification enhances its binding affinity to oxytocin receptors. [Leu3]-Oxytocin is utilized in research to investigate various physiological processes, including social bonding, stress response, and reproductive behaviors, making it a valuable tool for studying neuropeptide signaling pathways. -
OXT ligand
Pro8-Oxytocin is a modified oxytocin (OXT) ligand that exhibits enhanced potency and efficacy at primate oxytocin receptors (OXTR) compared to Leu8-Oxytocin. This compound demonstrates significantly stronger behavioral effects, making it a valuable tool in neuropharmacology research. Additionally, Pro8-Oxytocin shows a lower efficacy than vasopressin at human AVPR1a receptors while producing a higher efficacy at marmoset AVPR1a receptors, positioning it as an important reagent for studying receptor specificity and ligand-receptor interactions. -
Oxytocin Receptor Agonist
WAY-267464 hydrochloride is a non-peptide agonist of the oxytocin receptor. This compound has demonstrated the ability to impair social recognition memory in rats, likely through its action as a vasopressin 1A receptor antagonist. WAY-267464 hydrochloride is valuable for researching psychiatric disorders, including autism spectrum disorder, schizophrenia, and social anxiety disorder. -
Isomer
(S)-Retosiban is an isomer of Retosiban, serving as a valuable experimental control in research. As a selective oxytocin antagonist, it exhibits potent binding affinity with a Ki value of 0.65 nM. This compound is applicable in studies investigating the role of oxytocin in various physiological and pathological processes, contributing to advancements in understanding its biological activities. -
Oxytocin Analog
Demoxytocin is a cyclic peptide analog of oxytocin, primarily targeting oxytocin receptors. It enhances cell membrane permeability and elevates intracellular calcium levels in smooth muscle cells, resulting in increased contraction. This compound is particularly valuable for investigating the role of labor stimulation in conditions such as preterm premature rupture of membranes, as it mimics the biological activity of oxytocin in promoting uterine smooth muscle contraction. -
Antidiabetic Agent
[Asu1,6]-Oxytocin is an analog of oxytocin, functioning as an antidiabetic agent. It has been shown to reverse insulin resistance and improve glucose intolerance, independent of weight loss. This compound is valuable for research into obesity and diabetes, particularly in understanding mechanisms that contribute to metabolic regulation. -
Oxytocin Receptor Antagonist
L 366509 is a spiroindenylpiperidine camphorsulfonamide that acts as an antagonist of the oxytocin receptor. It demonstrates high affinity and selectivity for oxytocin receptors, making it a valuable tool in studies investigating oxytocin's physiological roles. This compound is particularly relevant for research into uterine contractions and has shown efficacy in inhibiting oxytocin-stimulated contractions, showcasing its potential applications in reproductive health. Additionally, molecular modeling indicates that its structure effectively mimics critical elements found in potent oxytocin antagonists. -
Oxytocin Analogue
Cargutocin, an oxytocin analogue, selectively targets the oxytocin receptor, facilitating uterine contractions. This compound enhances understanding of reproductive biology and assists in exploring therapeutic avenues for obstetric conditions. Its applications in research include studying labor induction and modulation of social behaviors linked to oxytocin signaling. -
OT-R Antagonist
Barusiban is a potent oxytocin receptor (OT-R) antagonist with a Ki of 0.8 nM, effectively inhibiting oxytocin-induced contractions. This compound is valuable for research applications in preterm labor, in vitro fertilization, and infertility studies. Its ability to modulate OT-R activity provides insights into reproductive health and physiological processes related to labor. -
Oxytocin Antagonist
L-366682 is a cyclic hexapeptide that acts as an oxytocin antagonist. It is primarily involved in research applications focused on the modulation of oxytocin-related physiological processes, including social behavior, stress response, and reproductive functions. This compound is valuable for studies investigating the effects of oxytocin signaling and its implications in various neuroendocrine conditions. -
0xytocin Antagonist Analog
OT Antagonist 3 Analog is an analog of the oxytocin receptor antagonist. This compound exhibits inhibitory activity on oxytocin signaling, making it a valuable tool for research into the modulation of social behaviors, reproductive functions, and stress responses. Its application spans therapeutic exploration in conditions associated with oxytocin dysregulation, providing insights into neuroendocrine pathways and potential pharmacological interventions. -
OT Receptor Antagonist
L-368,899 is a selective antagonist of the oxytocin (OT) receptor, exhibiting IC50 values of 8.9 nM and 26 nM in rat and human uterine tissues, respectively. This orally active compound effectively crosses the blood-brain barrier and is proven to inhibit oxytocin-stimulated uterine contractions in rat models. L-368,899 is valuable for research into preterm labor and the physiological roles of oxytocin in reproductive biology. -
Oxytocin Receptor Agonist
LIT-001 free base is a selective oxytocin receptor agonist, exhibiting an EC50 of 55 nM and a Ki of 226 nM. This compound has demonstrated significant enhancement of social interaction behaviors in mouse models of autism, making it a valuable tool for research in neuropsychiatric disorders and social behavior. Its nonpeptide structure distinguishes it as a lead candidate for further investigation into therapeutic applications related to oxytocin signaling. -
Gq-Dependent Pathway Agonist
(Val3,Pro8)-Oxytocin is a Gq-dependent pathway agonist that selectively activates the oxytocin receptor (OXTR). This compound demonstrates potential biological activity by engaging β-arrestin and promoting endocytosis, albeit at a weaker efficacy compared to its primary action. It is valuable for research applications targeting neurobiology, reproductive health, and cardiovascular studies, facilitating insights into therapeutic mechanisms involving the oxytocin signaling pathway. -
Oxytocin Analog
Oxytocin free acid, also known as 9-Deamidooxytocin, is an analog of oxytocin characterized by the substitution of the glycinamide residue at position 9 with a glycine residue. This peptide hormone exhibits diverse biological activities, influencing various physiological processes such as reproductive functions, social behaviors, and stress responses. Oxytocin free acid serves as an important tool in research exploring the mechanisms of action of oxytocin and its potential therapeutic applications in neurobiology and endocrinology. -
Oxytocin Receptor Antagonist
L 156373 is a potent antagonist of the oxytocin receptor, exhibiting an inhibitory constant (Ki) of 150 nM. This compound is valuable for studies investigating the physiological and pathophysiological roles of oxytocin, making it applicable in research areas such as neurobiology, endocrinology, and reproductive health. Its ability to selectively inhibit oxytocin receptor activity facilitates exploration of its implications in social behaviors, stress response, and various clinical conditions. -
Oxytocin Receptor Antagonist
SSR126768A free base is a potent oxytocin receptor antagonist with a Ki of 0.44 nM. This compound acts as a tocolytic agent by inhibiting oxytocin-induced intracellular calcium signaling and prostaglandin release in human uterine smooth muscle cells. As a result, SSR126768A effectively inhibits oxytocin-induced uterine contractions and has been shown to delay parturition in pregnant rats experiencing labor. This reagent is valuable for research applications focused on reproductive biology and the modulation of uterine contractility.

