Catalog No.
Product Name
Application
Product Information
Citations
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D3 Receptor Antagonist
(Rac)-GR218231 is a selective antagonist of the dopamine D3 receptor, exhibiting a pKi value of 8.9. This compound is valuable for studying the role of D3 receptors in various neurological and psychiatric disorders. Its pharmacological properties make it an important tool for research into dopamine-related pathways and potential therapeutic interventions. -
Antipsychotic Compound
A 23887 is a semirigid antipsychotic compound that primarily targets the dopamine D2 receptor. It exhibits significant affinity for this receptor, which is crucial for modulating dopaminergic signaling pathways. This compound is primarily utilized in research related to psychiatric disorders, particularly in the study of schizophrenia and other neuropsychiatric conditions. -
Stable Isotope
Ropinirole-d3 hydrochloride is a deuterium-labeled derivative of Ropinirole hydrochloride, functioning as a potent agonist for D2 and D3 dopamine receptors, with a Ki value of 29 nM for the D2 receptor. It exhibits pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively, while showing no affinity for D1 receptors. This compound is primarily utilized in research related to dopamine receptor signaling and has potential implications for therapies targeting Parkinson's disease. -
Dopamine D2 Receptor Antagonist
ADR 851 free base is a potent antagonist of the dopamine D2 receptor, making it valuable for research applications focused on antiemetic effects. This compound demonstrates significant potential in modulating dopamine-related pathways, contributing to the understanding of various neurological and psychiatric disorders. Its utilization in experimental studies may provide insights into therapeutic strategies targeting nausea and vomiting. -
D1 Receptor Agonist
SKF-80723 acts as a selective agonist for the dopamine D1 receptor, playing a crucial role in neurotransmitter signaling. This compound is primarily utilized in neuroscience research, particularly in studies related to Parkinson's disease and dopaminergic dysfunction. Its activation of D1 receptors offers insights into potential therapeutic strategies for neurodegenerative conditions associated with dopaminergic signaling deficits. -
Dopamine Receptor Agonist
Aplindore fumarate is a partial agonist of the dopamine D2 receptor, primarily utilized in neurological research. This compound has shown potential in studies related to Parkinson's disease and schizophrenia, offering insights into dopaminergic signaling pathways. Its activity makes it a valuable tool for investigating therapeutic strategies and understanding the underlying mechanisms of these disorders. -
D3R agonist
7-Hydroxy-PIPAT is a selective agonist of the D3 dopamine receptor, exhibiting a high binding affinity with a Ki value of 0.99 nM. This compound is utilized in research to explore mechanisms related to dopaminergic signaling and may offer insights into the pathology of neuropsychiatric disorders. Its potent activity makes it a valuable tool for studying D3 receptor-mediated pathways in various biological contexts. -
Atypical Dopamine Agonist
S3608 is an atypical dopamine agonist that selectively activates dopamine receptors, contributing to enhanced locomotor activity. This compound has been shown to dose-dependently increase locomotor activity in rodent models, making it a valuable tool for studying dopaminergic signaling and its implications in neuropharmacology. S3608 can be utilized in research applications focused on movement disorders, addiction, and behavioral studies related to dopamine modulation. -
D4 Receptor Antagonist
Sonepiprazole mesylate is a selective D4 dopamine receptor antagonist that exhibits inhibition constants (Kis) of 3.6 nM for rD4-Dopamine and 10.1 nM for hD4.2-Dopamine, indicating potent activity at these targets. Additionally, it shows significantly lower affinity for rD2-Dopamine (5147 nM) and Histamine-H1 receptors (7430 nM). This compound is valuable for research applications focused on neurobiology, particularly in studies related to dopamine receptor signaling and its implications in psychiatric disorders. -
Dopamine D-2 Receptors Antagonist
A31472 is a potent antagonist of dopamine D-2 receptors, making it a valuable tool for studying the pharmacology of antipsychotic agents. Its mechanism of action is critical for exploring the underlying pathways associated with dopamine dysregulation. Researchers can utilize A31472 to investigate its effects on behavioral and neurochemical processes relevant to psychiatric disorders. -
Dopamine Antagonist
Clothixamide is a dopamine antagonist that primarily targets dopamine receptors in the central nervous system. It exhibits biological activity relevant to the modulation of dopaminergic signaling and is useful for investigating various psychiatric disorders, including schizophrenia and depression. Research applications include studying the effects of dopamine inhibition on behavior and neurotransmitter pathways. -
Dopamine Receptor Antagonist
Org-10490 is a potent antagonist of dopamine D1 and D2 receptors, primarily utilized in neurological and psychiatric research. It plays a critical role in studies related to disorders such as schizophrenia and bipolar disorder by modulating dopaminergic signaling pathways. Its efficacy in receptor inhibition makes Org-10490 valuable for investigating therapeutic strategies targeting dopamine-related conditions. -
Dopamine D2 Receptor Antagonist
Lensiprazine is a potent dopamine D2 receptor antagonist that also functions as a serotonin reuptake inhibitor. This compound is primarily utilized in research focusing on psychiatric disorders, including bipolar disorder and schizophrenia, facilitating the exploration of neurochemical pathways involved in these conditions. Its dual action provides valuable insights into the modulation of neurotransmitter systems. -
D2 Dopamine Receptor Blocker
Savoxepin mesylate is a selective antagonist of the D2 dopamine receptor, exhibiting antipsychotic properties. It specifically targets dopamine D2 receptors in the hippocampus while sparing those in the striatum, thereby minimizing the likelihood of extrapyramidal side effects. This selective action makes Savoxepin mesylate a valuable tool for research addressing dopaminergic signaling and its implications in neuropsychiatric disorders. -
D2 Receptor Antagonist
(S)-Remoxipride hydrochloride hydrate is a selective antagonist of the dopamine D2 receptor, exhibiting an IC50 value of 1.57 μM. This compound is primarily utilized in the study of psychotic disorders, providing a valuable tool for understanding the mechanisms underlying dopamine-related pathologies and developing therapeutic strategies. Its specificity for the D2 receptor makes it an important reagent in neuropharmacology research. -
Dopamine Antagonist
Milenperone is a potent dopamine antagonist that primarily targets dopamine receptors. Its biological activity allows for the modulation of dopaminergic signaling, making it valuable in research focusing on neurological disorders. Milenperone is particularly useful in studies investigating the mechanisms underlying conditions related to dopamine dysregulation. -
Drug Derivative
4-EEC hydrochloride is a synthetic stimulant that acts as a releasing agent for norepinephrine and dopamine. It exhibits neurochemical properties that can influence mood and cognitive function. This compound is primarily used in research applications related to neuropharmacology and the study of stimulant drugs. -
D2 Receptor Antagonist
Desethoxy Quetiapine dihydrochloride is a selective antagonist of the dopamine D2 receptor, exhibiting an IC50 value of 1330 nM. This compound effectively inhibits Apomorphine-induced climbing and swimming behavior in murine models, making it valuable for investigating neuropharmacological activity and the modulation of dopaminergic signaling. Its utility in behavioral studies supports research into the therapeutic effects of D2 receptor antagonism in psychiatric disorders. -
Dopamine D1 Antagonist
SKF 83509 is a selective dopamine D1 antagonist with a Ki value of 70.2 nM, demonstrating no activity at dopamine D2 receptors. This compound is primarily utilized in neuropharmacological research to investigate the role of dopamine D1 receptors in various neurological conditions. SKF 83509 aids in the exploration of dopaminergic signaling pathways and contributes to studies focused on drug addiction, schizophrenia, and other dopamine-related disorders. -
D4 Receptor Antagonist
Sonepiprazole hydrochloride is a selective antagonist of the D4 dopamine receptor, exhibiting Ki values of 3.6 nM for the rat D4 dopamine receptor and 10.1 nM for the human D4.2 dopamine receptor. This compound demonstrates significant selectivity, with much higher Ki values of 5147 nM and 7430 nM for the rat D2 dopamine and Histamine H1 receptors, respectively. Sonepiprazole hydrochloride is useful for investigating the role of D4 receptors in neurological disorders and may have applications in psychopharmacology research. -
Dopamine D2 Receptor Agonist
FR 64822 is a potent dopamine D2 receptor agonist that demonstrates significant antinociceptive activity in preclinical models, such as rats and mice, via indirect stimulation of these receptors. In addition to its analgesic properties, FR 64822 has been shown to facilitate penile erection in juvenile rats and mitigate scopolamine-induced amnesia during passive avoidance tasks. Its diverse biological activities make it a valuable tool for research in neuropharmacology and behavioral studies. -
D3 Receptor Agonist
(+)-UH 232 is a partially selective agonist of the D3 dopamine receptor, exhibiting an intrinsic activity of 0.2-0.4. This compound effectively antagonizes quinpirole-induced mitogenesis, with a reported Ki value of 9.4 nM. It is utilized in research to explore D3 receptor signaling and its implications in various neurobiological processes. -
Antipsychotic Agent
Butaclamol is an antipsychotic agent that functions primarily as a D2 dopamine receptor antagonist. This compound exhibits significant neuroleptic activity, making it a valuable tool in the study of psychotic disorders. It is utilized in research to explore the mechanisms underlying dopaminergic signaling and its implications in various neuropsychiatric conditions. -
Haloperidol Analogue
Deschlorohaloperidol is a potent analogue of Haloperidol, primarily acting as a dopamine D2 receptor (D2R) antagonist. This compound exhibits significant antipsychotic activity, making it valuable in research focused on schizophrenia and related disorders. Its structural modifications enhance its efficacy for investigating dopamine signaling pathways and therapeutic interventions in psychiatric conditions. -
D4 Receptor Ligand
U-101958 maleate is a highly selective antagonist for the dopamine D4 receptor, exhibiting an IC50 of 2.7 nM. In HEK-293 cells expressing the human recombinant D4.4 receptor, U-101958 behaves as an agonist, demonstrating its versatile interaction with this target. This compound is primarily utilized in research related to antipsychotic effects and the modulation of dopaminergic signaling pathways. -
Dopamine Receptor Modulator
Ordopidine hydrochloride is a modulator of dopamine receptors that demonstrates an ED50 of 68 μmol/kg for increasing DOPAC levels in the rat striatum. This compound is valuable in research applications focused on neurological disorders and dopamine-related signaling pathways. Its ability to influence dopamine metabolism makes it a useful tool for exploring the role of dopamine in various physiological and pathological conditions. -
Dopamine Receptor Agonist
PF-592379 is a selective agonist of the dopamine D3 receptor, exhibiting an EC50 of 21 nM. This compound demonstrates significant potential in modulating dopaminergic signaling pathways, making it valuable for research applications related to neuroinflammatory disorders and addiction. Its ability to influence dopamine receptor activity makes PF-592379 a useful tool for studying the role of dopamine in various physiological and pathological processes. -
Dopamine Receptor Antagonist
Benzamide Derivative 1 is a dopamine receptor antagonist with potential applications in the treatment of gastrointestinal disorders. This compound, derived from patent EP0213775A1, compound 18, exhibits key biological activity by modulating dopamine signaling pathways. Its role in gastrointestinal function makes it a valuable tool for researchers investigating the interplay between dopamine receptors and gut health. -
Dopamine Receptor Agonist
U91356 is a selective dopamine receptor agonist that targets D1-like receptors. This compound has been shown to enhance dopaminergic signaling, making it useful in studies investigating neurological disorders such as schizophrenia and Parkinson's disease. U91356 facilitates the exploration of dopamine-related pathways and receptor interactions in various biological systems. -
ETB Receptor Antagonist
BQ-788 is a selective endothelin B (ETB) receptor antagonist, exhibiting a potent IC50 of 1.2 nM against endothelin-1 (ET-1) binding in human Girardi heart cells. It demonstrates limited inhibitory activity on ETA receptors in the human neuroblastoma SK-N-MC cell line, with an IC50 of 1300 nM. This compound is primarily utilized in research on cardiovascular and neurobiological systems, aimed at elucidating the role of ETB receptors in various physiological and pathological conditions. -
Daul ETA/ETB Receptor Antagonist
J-104132 is a potent, orally active dual antagonist of the ETA and ETB receptors, exhibiting a Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. It effectively inhibits Endothelin-1 (ET-1)-induced signaling and vascular contractions in vitro. In vivo studies demonstrate that J-104132 mitigates hypertension, vascular remodeling, and diabetic endothelial dysfunction through dual blockade of ETA and ETB receptors, making it valuable for research into diabetic vascular complications. -
Endothelin-A Receptor Antagonist
SB 247083 is a selective and competitive antagonist of the endothelin-A receptor, exhibiting a Ki value of 0.41 nM. It displays a significantly lower affinity for the endothelin-B receptor with a Ki of 467 nM. SB 247083 effectively inhibits ET-1-induced contractions in rat aorta, with a Kb of 3.5 nM. This reagent is valuable for research focusing on cardiovascular diseases and their underlying mechanisms. -
ETA Receptor Antagonist
Clazosentan is a selective endothelin A (ETA) receptor antagonist. It effectively inhibits ET-1-mediated vasoconstriction, making it a valuable tool in research focused on cardiovascular function and cerebral health. Clazosentan is primarily utilized in studies investigating the prevention of cerebral vasospasm and associated complications, including cerebral infarction. -
Endothelin Receptor Agonist
Sarafotoxin S6a is an endothelin receptor agonist that selectively targets ETA and ETB receptors, exhibiting a profile comparable to Endothelin-3. This compound is known to effectively stimulate vasoconstriction in pig coronary arteries, with an EC50 value of 7.5 nM, making it a valuable tool for studying cardiovascular physiology and pathophysiology. Its targeted interactions facilitate research in vascular biology and related therapeutic areas. -
Endothelin Receptor Antagonist
BMS 182874 is a selective endothelin receptor type A (ETA) antagonist, demonstrating an IC50 value of 0.150 μM and a Ki of 0.055 μM. This compound effectively reduces arterial pressure in models of deoxycorticosterone acetate-induced hypertension in rats, making it a valuable tool for cardiovascular disease research. BMS 182874's targeted action on the endothelin receptor provides insights into vascular function and potential therapeutic approaches for hypertension. -
ETB Receptor Antagonist
Ro 46-8443 is a selective antagonist of the endothelin ETB receptor, exhibiting at least 100-fold selectivity for ETB over ETA receptors (IC50: 34-69 nM vs. 6800 nM). Its specificity allows for targeted investigations into ETB receptor-related biological mechanisms. This compound is valuable for research applications focused on cardiovascular effects, cell proliferation, and pathophysiological conditions related to endothelin signaling. -
Endothelin-B Receptor Agonist
Sarafotoxin S6c is a potent agonist of the endothelin-B receptor. This compound induces vasoconstriction in both endothelium-intact and endothelium-denuded vascular tissues, making it a valuable tool for studying endothelial function and vascular tone regulation. Its application in research aids in elucidating the role of endothelin pathways in cardiovascular physiology and pathology. -
ET(A) Receptor Antagonist
Nebentan is a selective, orally active non-peptide antagonist of the endothelin ETA receptor. It demonstrates significant inhibitory activity against [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptors, with Ki values of 0.697 nM and 569 nM, respectively. Research indicates that Nebentan may effectively mitigate the progression of cor pulmonale and myocardial infarction in vivo, making it a valuable tool for studies related to cardiovascular and pulmonary diseases. -
ET Receptor Antagonist
Enrasentan is an endothelin (ET) receptor antagonist with notable antihypertensive effects. It primarily functions by blocking the action of endothelin, a potent vasoconstrictor, thereby promoting vasodilation and lowering blood pressure. This compound is utilized in cardiovascular research to investigate mechanisms of hypertension and potential therapeutic interventions. -
ET(A) Receptor Antagonist
Nebentan potassium (YM598) is a selective, orally active non-peptide antagonist of the endothelin ETA receptor. It demonstrates significant inhibition of [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptors, with Kis of 0.697 nM and 569 nM, respectively. This compound has shown potential in ameliorating the progression of cor pulmonale and myocardial infarction in vivo, making it valuable for cardiovascular research applications. -
ETA Inhibitor
Diosuxentan is a selective inhibitor of the endothelin A (ETA) receptor. It demonstrates significant biological activity in suppressing vascular responses associated with endothelin-1, making it relevant for studies investigating cardiovascular, renal, and neuroinflammatory conditions. Diosuxentan provides valuable insights for research focused on the therapeutic modulation of ETA-mediated pathways. -
Endothelin-A Receptor Antagonist
PD-156707 is a selective endothelin-A receptor antagonist that exhibits potent oral activity. This compound binds to human ET-A and ET-B receptors with Ki values of 0.17 nM and 133.8 nM, respectively. PD-156707 has demonstrated efficacy in reversing established chronic hypoxic pulmonary hypertension in rat models. It is suitable for research on diseases related to aberrant endothelin-A receptor activation, with potential applications in pulmonary hypertension, stroke, and heart failure studies. -
ETA Receptor Antagonist
ABT-546 is a potent and highly selective endothelin ETA receptor antagonist, exhibiting a binding affinity (Ki) of 0.46 nM for [125I]endothelin-1 in cloned human ETA receptors. With over 25,000-fold selectivity for the ETA receptor compared to the ETB receptor, ABT-546 effectively inhibits endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis, displaying IC50 values of 0.59 nM and 3 nM, respectively. This compound serves valuable applications in cardiovascular and neurobiological research, particularly in studies investigating endothelin-mediated pathways. -
ETAR Antagonist
Ambrisentan sodium is a selective antagonist of the endothelin type A receptor (ETAR). This compound demonstrates potent inhibition of ETAR, making it valuable for investigating the role of endothelin signaling in various physiological processes and pathological conditions. It is primarily used in research related to cardiovascular diseases and pulmonary hypertension. -
Stable Isotope
(Rac)-Ambrisentan-d3 is a deuterated form of (Rac)-Ambrisentan, a selective endothelin receptor antagonist. This stable isotope is utilized in pharmacokinetic studies and metabolic research, allowing for precise tracking of drug metabolism and distribution in biological systems. Its application is essential for understanding the pharmacological properties and efficacy of endothelin receptor-targeted therapies. -
ETA Receptor Antagonist
Sulfatroxazole is a selective antagonist of the endothelin A (ETA) receptor, with an IC50 value of 0.26 μM. This compound is primarily utilized in research focused on cardiovascular disease and pulmonary hypertension by inhibiting the effects of endothelin-1, a potent vasoconstrictor. Its application in biological studies provides insights into the role of ETA signaling in various pathophysiological conditions. -
ETB Agonist
[Ala1,3,11,15]-Endothelin (53-63) is a selective agonist for the ETB receptor, exhibiting potent activity with IC50 values between 0.33 nM and 0.61 nM. This compound is valuable for research focused on vasoconstriction and related physiological processes. Its specificity for the ETB receptor makes it a useful tool for investigating the role of endothelins in vascular biology and potential therapeutic applications. -
ETA Antagonist
BMS-193884 is a selective, orally active antagonist of the endothelin A (ETA) receptor, exhibiting a significant 10,000-fold increased affinity for this target (Ki=1.4 nM) compared to the endothelin B (ETB) receptor. This compound is primarily utilized in research applications focused on vascular biology, cardiovascular conditions, and pathology related to endothelin signaling. Its potent inhibition of ETA receptor activity makes it a valuable tool for investigating endothelin-mediated processes and therapeutic intervention strategies. -
Endothelin Receptor Agonist
[Lys4] Sarafotoxin S6c is a potent partial agonist of the endothelin receptor. This sarafotoxin analogue induces contraction in pig coronary artery tissues, demonstrating an EC50 of 1.5 nM. It serves as a valuable tool for research in cardiovascular physiology and the study of endothelin receptor signaling pathways. -
ETB Receptor Antagonist
RES-701-1 is a cyclic peptide that serves as a specific antagonist for the endothelin receptor type B (ETB). This compound effectively inhibits the binding of 125I-labeled endothelin-1 (ET-1) to the ETB receptor, demonstrating an IC50 value of 10 nM. RES-701-1 is primarily utilized for research applications aimed at studying the role of ETB receptors in cardiovascular and other physiological processes.
