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Catalog No.
Product Name
Application
Product Information
Citations
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Dopamine Receptor Inhibitor
GBR 12783 is a selective dopamine uptake inhibitor that targets dopamine receptors with high potency. It effectively inhibits [3H]dopamine uptake in striatal synaptosomes from rats and mice, exhibiting IC50 values of 1.8 nM and 1.2 nM, respectively. This compound has been shown to enhance memory performance and increase hippocampal acetylcholine release in rodent models, making it valuable for research in neuropharmacology and cognitive function studies. -
Dopamine Receptor Inhibitor
Cyclo(glycyl-L-leucyl) is a neuropeptide that specifically inhibits dopamine receptors, playing a crucial role in modulating dopaminergic signaling. This compound has been shown to down-regulate dopamine receptor activity and reduce dopaminergic supersensitivity, particularly in the context of morphine-induced analgesia in animal models. Cyclo(glycyl-L-leucyl) holds promise for potential therapeutic applications in preventing tardive dyskinesias and L-DOPA-induced dyskinesias, making it valuable for research in neuropharmacology and movement disorders. -
Dopamine Receptor Inhibitor
Fosopamine hydrochloride is a dopamine receptor D agonist, primarily targeting the dopamine receptor pathways. It has demonstrated significant utility in research related to hypertension, aiding in the exploration of cardiovascular mechanisms and blood pressure regulation. This compound may provide insights into both the physiological and pathological roles of dopamine signaling in hypertension-related studies. -
Dopamine Receptor Inhibitor
PD 128907 is a selective dopamine D3 receptor inhibitor that effectively modulates dopaminergic signaling. The active (+) enantiomer exhibits high affinity for rat D3 receptors and demonstrates significant inhibitory effects on neuronal firing in the ventral tegmental area and substantia nigra pars compacta, with EC50 values of 33 nM and 38 nM, respectively. Additionally, it inhibits dopamine release in the caudate putamen with an EC50 of 66 nM. While PD 128907 primarily targets D3 receptors, evidence suggests its actions may also involve D2 autoreceptors, making it a valuable tool for exploring dopamine receptor pharmacology and neurobehavioral research. -
Dopamine Receptor Inhibitor
ADTN is a dopamine receptor inhibitor that modulates dopamine neurotransmission. It demonstrates the ability to reduce dopamine-related signaling, which may help target conditions associated with excessive dopamine activity. ADTN is applicable in research focused on mental health disorders and cognitive function modulation, providing insights into therapeutic strategies for related pathologies. -
Dopamine Receptor Inhibitor
Metoclopramide dihydrochloride is a dopamine D2 receptor antagonist primarily used for its antiemetic effects. It demonstrates notable activity in managing nausea and vomiting, particularly in patients undergoing chemotherapy or surgery. This compound is also employed in research settings to explore the modulation of dopaminergic pathways and gastrointestinal motility. -
Dopamine Receptor Inhibitor
Bulbocapnine hydrochloride is a potent dopamine receptor inhibitor that plays a significant role in modulating dopaminergic activity. This aporphine alkaloid is known to inhibit dopamine synthesis and exhibits neuroleptic-like properties, alongside anticonvulsant and antinociceptive effects. Its pharmacological profile makes it a valuable tool in research related to neurological disorders and the exploration of dopamine-related pathways. -
Dopamine Receptor Inhibitor
Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia. -
Dopamine D1/D2 Receptor Inhibitor
(Z)-Flupenthixol decanoate is a potent antagonist of dopamine D1 and D2 receptors, functioning primarily to inhibit dopaminergic signaling. This compound exhibits significant antipsychotic activity, making it valuable in the study of psychiatric disorders and neuropharmacology. Research applications include investigations into the modulation of dopaminergic pathways and the evaluation of therapeutic strategies for schizophrenia and related conditions. -
Dopamine Receptor Inhibitor
Seproxetine hydrochloride is a dopamine receptor inhibitor known for its selective serotonin reuptake inhibitory activity. By specifically blocking the serotonin uptake transporter, it increases serotonin levels in the brain, while also exhibiting significant interactions with dopamine receptors. This compound is actively researched for its potential therapeutic applications in mood disorders and associated neurological conditions, showcasing enhanced biological activity and efficacy through its ability to form stable charge transfer complexes. -
Dopamine Receptor Inhibitor
TISCH is a potent and selective iodinated ligand that targets CNS D1 dopamine receptors, demonstrating a high affinity with a Kd value of 0.205 nM in rat striatal tissue. Its ability to cross the blood-brain barrier allows for effective distribution in regions with substantial D1 receptor density, making it a valuable pharmacological tool for characterizing these receptors. Additionally, TISCH, when labeled with I-123, has potential applications as an in vivo imaging agent for studying D1 dopamine receptor function in the central nervous system. -
Dopamine Receptor Inhibitor
Opromazine hydrochloride is a dopamine receptor inhibitor known for its sedative and antiemetic effects. It primarily reduces dopaminergic activity by blocking dopamine receptors in the brain, making it useful in the treatment of psychiatric disorders such as schizophrenia and psychosis. Additionally, studies have investigated its metabolites through various microsomal enzymes, highlighting differences in formation rates and the variability of drug-metabolizing enzymes in human liver and placenta microsomes, which is essential for understanding its pharmacokinetic profile. -
Adrenergic Receptor Inhibitor
Cetamolol hydrochloride acts as a potent β1-adrenergic receptor inhibitor, exhibiting intrinsic sympathomimetic activity and cardioselectivity. It demonstrates a prolonged inhibitory effect on heart rate and myocardial contractility at low to moderate doses, making it a valuable reagent for cardiovascular research. Its unique profile allows for exploration in studies evaluating hypertension, arrhythmias, and other cardiac conditions. -
β-Adrenergic Receptor Inhibitor
Bufetolol is a selective β-adrenergic receptor inhibitor that modulates cardiac activity by decreasing the maximum rate of depolarization during action potentials. Its antiarrhythmic properties make it a valuable tool for research into the mechanisms of cardiac rhythm disorders. Bufetolol is utilized in studies aimed at exploring therapeutic strategies for arrhythmias and related cardiovascular conditions. -
Adrenergic Receptor Inhibitor
Teoprolol is a selective β-adrenergic receptor inhibitor that effectively modulates adrenergic signaling pathways. It exhibits key biological activities including the reduction of heart rate and myocardial contractility, making it valuable for cardiovascular research. Teoprolol is widely used in studies investigating hypertension, anxiety, and heart failure, contributing to our understanding of adrenergic receptor function and pharmacological interventions. -
α1/β1-Adrenergic Receptor Inhibitor
Amosulalol hydrochloride functions as a dual inhibitor of α1 and β1-adrenergic receptors, demonstrating pronounced antihypertensive effects. By inhibiting α1-adrenergic receptors, it effectively lowers blood pressure, while β1-adrenergic receptor inhibition reduces reflexive increases in heart rate and plasma renin activity. This compound is particularly useful in studies involving spontaneously hypertensive rats, providing valuable insights into cardiovascular mechanisms and potential therapeutic interventions in hypertension. -
AR Inhibitor
Amidephrine hydrochloride is an adrenergic receptor (AR) agonist that functions primarily by stimulating adrenergic signaling pathways. It demonstrates key biological activities relevant to neurological research, making it a valuable reagent for studying various neurological diseases and disorders. Its effects on AR modulation can facilitate investigations into therapeutic interventions and pharmaceutical development in the field of neuroscience. -
Adrenergic Receptor Inhibitor
Tropodifene is an α-adrenergic receptor inhibitor that modulates adrenergic signaling pathways. It is primarily utilized in research related to cardiovascular pharmacology and the study of sympathetic nervous system functions. Its unique mechanism of action makes it valuable for investigating the role of adrenergic receptors in various physiological and pathological conditions. -
Adrenergic Receptor Inhibitor
Benzquinamide is an adrenergic receptor inhibitor that selectively binds to the α2A, α2B, and α2C adrenergic receptors, exhibiting Ki values of 1,365, 691, and 545 nM, respectively. This compound demonstrates antiemetic properties and is utilized in research applications relating to nausea and vomiting. Its mechanism of action involves modulation of adrenergic signaling pathways, making it a valuable tool for studying the role of adrenergic receptors in various physiological and pathological conditions. -
Angiotensin Receptor Inhibitor
H-Val-Pro-Pro-OH TFA is an inhibitor of Angiotensin I converting enzyme (ACE), demonstrating an IC50 of 9 μM. This milk-derived proline peptide derivative is utilized in research applications focused on cardiovascular biology and hypertension. Its role in modulating the renin-angiotensin system makes it a valuable tool for studying the effects of ACE inhibition in various physiological and pathological contexts. -
CXCR Inhibitor
ALX 40-4C is a small peptide inhibitor targeting the chemokine receptor CXCR4. It effectively prevents the binding of SDF-1 to CXCR4 with a Ki of 1 μM, thereby inhibiting the replication of X4 strains of HIV-1. Additionally, ALX 40-4C Trifluoroacetate serves as an antagonist of the APJ receptor, exhibiting an IC50 value of 2.9 μM. This dual activity makes ALX 40-4C a valuable tool for research in HIV-1 studies and chemokine receptor signaling pathways. -
CXCR Receptor Inhibitor
SCH-900875 is a selective inhibitor of the CXCR3 receptor, known for its oral bioavailability and ability to penetrate the blood-brain barrier. By binding to CXCR3, it effectively prevents the interaction of ligands CXCL9, CXCL10, and CXCL11, thereby inhibiting downstream G protein and β-arrestin signaling pathways, which reduces inflammatory cell migration. This compound holds potential for investigating various autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis, as well as inflammatory conditions like psoriasis and inflammatory bowel disease. -
PDK Inhibitor, CB1/CB2 Agonist
Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor, demonstrating an IC50 value of 9.5 μM. It effectively lowers blood glucose levels in diabetic mouse models. Additionally, Leelamine acts as a weak agonist of cannabinoid receptors CB1 and CB2. Its biological activity includes a reduction in mitotic activity and prostate-specific antigen expression, as well as the induction of apoptosis in cancer cells, making it a valuable tool for cancer research and metabolic studies. -
Cannabinoid Receptor Inhibitor
2-Linoleoyl glycerol is a monoacylglycerol that serves as an antagonist and partial agonist at the cannabinoid receptor type 1 (CB1). It effectively modulates the activity of cannabinoids such as anandamide (AEA) and 2-arachidonoylglycerol (2-AG) by attenuating their effects without enhancing them. This compound has significant implications in cannabinoid research, particularly in studies focused on the endocannabinoid system and potential therapeutic targets for various conditions. Additionally, its potency can be influenced by the inhibition of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). -
CB1 Inhibitor
ANEB-001 is an orally active inhibitor of the cannabinoid receptor type 1 (CB1). This compound is primarily utilized in research focused on acute cannabinoid intoxication, providing insights into the physiological effects and potential therapeutic approaches related to CB1 modulation. Its selective inhibition of CB1 makes it a valuable tool for studies investigating cannabinoid-related pathways and their implications in various biological contexts. -
DAGLα Inhibitor
O-7460 is a selective inhibitor of diacylglycerol lipase alpha (DAGLα), exhibiting an IC50 value of 0.69 μM. This compound demonstrates selectivity against monoacylglycerol lipase (MAGL) and both human CB1 and CB2 cannabinoid receptors. O-7460 has been shown to effectively reduce elevated 2-arachidonoylglycerol (2-AG) levels associated with high-fat diet conditions, making it a valuable tool for studying endocannabinoid signaling and its implications in metabolic disorders. -
CB/FAAH Inhibitor
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is a potent inhibitor of the central cannabinoid receptor (CB1) and fatty acid amide hydrolase (FAAH), exhibiting similar inhibitory activities with IC50 values around 2 nM. It serves as a valuable tool for investigating cannabinoid signaling pathways and lipid metabolism in various biological contexts. Researchers utilize IDEFP to explore the therapeutic potential of modulating endocannabinoid systems in pain, inflammation, and neuroprotection studies. -
BChE Inhibitor/CB2R Agonist
hBChE-IN-2 is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 0.62 μM and functions as an agonist for cannabinoid receptor 2 (CB2R). This compound exhibits significant neuroprotective activities, making it a valuable tool in the study of neurodegenerative diseases and cannabinoid signaling pathways. Its dual action positions hBChE-IN-2 as an important reagent for research applications targeting cholinergic regulation and endocannabinoid modulation. -
CETP Inhibitor/CB1 Agonist
BI-5756 is a selective CETP inhibitor and cannabinoid receptor 1 (CB1) agonist. It promotes a significant increase in HDL-C levels while reducing LDL-C levels, thereby improving lipid profiles. Additionally, BI-5756 enhances the function of regulatory T cells and preserves T cell-mediated anti-tumor activity, exhibiting direct anti-proliferative effects on tumor cells. This compound also upregulates the expression of MHC I, MHC II, and CD80 on tumor cells and demonstrates protective effects in graft-versus-host disease. BI-5756 is applicable in research related to oncology, graft-versus-host disease, and metabolic disorders. -
CB1/2 Inhibitor
AM12814 is a potent and selective inhibitor of cannabinoid receptors CB1 and CB2, demonstrating Ki values of 0.7 nM and 3.4 nM, respectively. This compound effectively inhibits cAMP accumulation and promotes β-arrestin 2 recruitment, mimicking cannabimimetic effects. AM12814 is suitable for research applications related to neurological diseases, including studies on catalepsy. -
CB2R Agonist/FAAH Inhibitor
CB2R/FAAH modulator-1 is a potent full agonist of the cannabinoid type 2 receptor (CB2R), exhibiting a binding affinity with a Ki of 14.8 nM for CB2R and 241.3 nM for CB1R. This compound also serves as an inhibitor of fatty acid amide hydrolase (FAAH), demonstrating an IC50 of 4 μM. CB2R/FAAH modulator-1 is effective in modulating cytokine production by decreasing pro-inflammatory cytokines while enhancing anti-inflammatory cytokine levels, making it valuable for research in inflammation and pain modulation. -
Anandamide Transport Inhibitor
N-(3-Hydroxyphenyl)-arachidonoyl amide is an anandamide transport inhibitor, exhibiting an IC50 of 21.3 μM. This compound serves as a valuable tool in understanding endocannabinoid signaling and lipid metabolism. It can be utilized in research applications focusing on cannabinoid receptors and the modulation of neuronal activity. -
CB1 Inhibitor
CB1-IN-2 is a selective CB1 receptor inhibitor, characterized by an IC50 of 0.644 μM. This compound effectively penetrates the blood-brain barrier, making it suitable for studies exploring its potential central nervous system effects. CB1-IN-2 can be applied in research focused on cannabinoid receptor modulation and its implications in various neurological and psychological conditions. -
Adenosine Receptor Inhibitor
CVT-2759 is a potent inhibitor of the A1 adenosine receptor, exhibiting IC50 values of 0.18 μM and 9.5 μM to antagonize [3H]CPX binding in the absence and presence of 1 mM GTP, respectively. This compound is essential for assessing the modulation of AV nodal conduction, facilitating a reduction in ventricular rate without inducing AV block, bradycardia, atrial arrhythmias, or vasodilation. It serves as a valuable reagent for research on cardiovascular physiology and pharmacological modulation of adenosine receptor pathways. -
Adenosine Receptor Inhibitor
KF21213 is a selective adenosine A2A receptor inhibitor, demonstrating a high affinity with a Ki value of 3.0 nM. This compound is essential for research involving central nervous system (CNS) functions and disorders, providing valuable insights into adenosine receptor signaling pathways. Its precision in targeting A2A receptors makes it a suitable tool for studying their role in neuropharmacology and related therapeutic applications. -
Adenylate Cyclase Inhibitor
KUM 32 is a potent inhibitor of adenylate cyclase that functions by antagonizing epinephrine-induced platelet aggregation. By selectively binding to the alpha-2 adrenergic receptor on human platelets, KUM 32 modulates platelet activation and aggregation pathways. This compound is utilized in research focused on cardiovascular disease and hemostasis, providing insights into the mechanisms of platelet function. -
Gαi Inhibitor
0990CL is a selective inhibitor of the heterotrimeric Gαi subunit, functioning through direct interaction with Gαi. This compound effectively inhibits α2 adrenergic receptor-mediated regulation of cyclic AMP (cAMP), making it a valuable tool for studying Gαi signaling pathways. It is particularly useful in research related to neurotransmission and cardiovascular physiology, aiding in the exploration of GPCR-mediated processes. -
β3-adrenergic Receptor Inhibitor
Vemtoberant is a selective β3-adrenergic receptor inhibitor with a human Ki of 8.2 nM, demonstrating a significant selectivity of 400- to 600-fold over the human β1- and β2-adrenergic receptors. This compound effectively attenuates β3-AR-mediated cardiac inhibition, making it a valuable tool for studying mechanisms underlying systolic heart failure. Researchers can utilize Vemtoberant to investigate therapeutic strategies aimed at modulating β3-adrenergic signaling in cardiac contexts. -
Adrenergic Receptor Inhibitor
Todralazine hydrochloride is a selective β2 adrenergic receptor inhibitor primarily used in the treatment of hypertension. Its mechanism involves blocking β2 adrenergic receptors, contributing to its effectiveness as an antihypertensive agent. In addition to its receptor inhibition, Todralazine hydrochloride exhibits antioxidant properties, providing potential benefits in research focused on oxidative stress and cardiovascular health. -
α1/β1-Adrenergic Receptor Inhibitor
Amosulalol is a dual inhibitor of the α1 and β1-adrenergic receptors, demonstrating significant antihypertensive activity. By selectively inhibiting the α1-adrenergic receptor, Amosulalol effectively reduces blood pressure, while its β1-adrenergic receptor blockade leads to decreased reflex-induced heart rate and plasma renin activity in spontaneously hypertensive rats. This compound is valuable for research applications focused on cardiovascular physiology and the pharmacological modulation of blood pressure. -
β-AR inhibitor
β-AR antagonist 2 functions as a selective antagonist of β-adrenergic receptors, exhibiting an IC50 value of 0.17 μM. This compound has demonstrated significant inhibitory effects on the growth of mouse A549 xenograft tumors and exhibits cardioprotective properties in a model of doxorubicin-induced heart failure in C57 mice. Its applications in cancer research and cardiovascular studies make it a valuable tool for investigating β-AR signaling pathways. -
Adrenergic Receptor Inhibitor
Napitane is an adrenergic receptor inhibitor that primarily targets α-adrenergic receptors, leading to enhanced catecholamine availability. This compound has demonstrated significant potential in antidepressant research, highlighting its efficacy in modulating neurochemical pathways associated with mood regulation. Napitane serves as a valuable tool for investigating mechanisms underlying depression and exploring novel therapeutic approaches for mood disorders. -
α1 Adrenergic Receptor Inhibitor
Conopeptide rho-TIA is a peptide originating from the venom of the predatory sea snail Conus tulipa, serving as a highly selective noncompetitive inhibitor of the human α1B-adrenergic receptor. It also acts as a competitive inhibitor for both the α1A- and α1D-adrenergic receptors. By selectively binding to these receptor subtypes, conopeptide rho-TIA offers valuable insights for the development of novel, subtype-selective α1-adrenergic receptor therapies. Its unique mechanism of action makes it a potent tool for cardiovascular and pharmacological research. -
Adrenergic Receptor Inhibitor
(+)-Amosulalol is an adrenergic receptor inhibitor that serves as an orally active dual blocker of α1 and β1-adrenergic receptors. This compound demonstrates significant antihypertensive activity by selectively inhibiting α1-adrenergic receptors, while also reducing reflex tachycardia and plasma renin activity in spontaneously hypertensive rats through β1-adrenergic receptor inhibition. As a valuable research tool, (+)-Amosulalol can be employed in studies related to cardiovascular physiology and pharmacology. -
Adrenergic Receptor Inhibitor
Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission. -
Adrenergic Receptor Inhibitor
Moprolol is a beta-adrenergic receptor inhibitor that primarily targets beta-adrenergic receptors to modulate cardiovascular responses. This compound is useful in research related to essential hypertension studies, enabling investigations into its effects on blood pressure regulation and heart rate modulation. Its properties make it a valuable tool for exploring the role of adrenergic signaling in hypertensive conditions. -
Adrenergic Receptor Inhibitor
JNJ-7925476 hydrochloride is a triple monoamine uptake inhibitor that targets adrenergic receptors to modulate neurotransmitter availability. It demonstrates significant antidepressant activity, as evidenced by increased extracellular levels of serotonin, dopamine, and norepinephrine in the rat cerebral cortex. This compound is applicable in preclinical research to investigate the mechanisms underlying mood disorders and therapeutic interventions. Additionally, its rapid absorption and higher concentration in the brain support its potential for effective neurological studies. -
α2A/α2B AR Inhibitor
BRL-44408 is a selective antagonist of the α2A and α2B adrenergic receptors. It effectively inhibits the actions of norepinephrine and the agonist Clonidine on the release of [3H]norepinephrine and [3H]5-hydroxytryptamine in K+-stimulated conditions. With a higher affinity for α2A-adrenoceptors in human platelet membranes compared to other antagonists, BRL-44408 may play a significant role in modulating neurotransmitter release, making it a valuable tool for research in adrenergic signaling and related pharmacological studies. -
NET Inhibitor
XEN-2174 is a selective noradrenaline transporter (NET) inhibitor that functions through non-competitive inhibition of noradrenaline reuptake. By increasing the synaptic concentration of noradrenaline, it activates α2-adrenergic receptors at the spinal level, leading to pronounced analgesic effects. This compound demonstrates sustained analgesia in various models of neuropathic and postoperative pain in rats, making it a valuable tool for pain research applications. -
Adrenergic Receptor Inhibitor
(-)-Amosulalol is a selective inhibitor of α1/β1-adrenergic receptors, demonstrating dual action in pharmacological studies. It exhibits antihypertensive properties primarily through the blockade of α1-adrenergic receptors, effectively reducing peripheral vascular resistance. Additionally, (-)-Amosulalol decreases reflex tachycardia and plasma renin activity in models of hypertension, making it valuable for research in cardiovascular diseases and hypertension management.
