Catalog No.
Product Name
Application
Product Information
Citations
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Stable Isotope
Quetiapine-d4-1 fumarate is a deuterated analogue of Quetiapine, specifically designed to enhance analytical precision in research applications. As a serotonin (5-HT) receptor agonist, it exhibits a pEC50 of 4.77 at the human 5-HT1A receptor and acts as a dopamine receptor antagonist with a pIC50 of 6.33 for the human D2 receptor. Quetiapine-d4-1 fumarate demonstrates moderate to high affinity for several key receptors, including D2, 5-HT1A, 5-HT2A, and 5-HT2C, making it suitable for studies in neuropharmacology, particularly in exploring antidepressant and anxiolytic effects. -
5-HT1/D2 Agonist
Sarizotan hydrochloride is a potent agonist of the serotonin 5-HT1A receptor and dopamine receptors D2, D3, and D4. It demonstrates high affinity with IC50 values of 0.1 nM for human 5-HT1A, 15.1 nM for rat D2, and 2.4 nM for human D4.2, among others. This compound is primarily utilized in neurological research and pharmacological studies, particularly in the exploration of psychopharmacological interventions and the modulation of serotonergic and dopaminergic pathways. -
Antipsychotic Agent
PZ-1190 is a multitarget ligand that primarily interacts with serotonin and dopamine receptors, exhibiting potential antipsychotic activity. This compound has been studied in rodent models to explore its effects on psychotic behaviors. Its unique mechanism of action positions it as a valuable tool for research into psychiatric disorders and the underlying neurotransmitter systems. -
Dopamine Receptor Antagonist
Zicronapine fumarate is a potent dopamine receptor antagonist primarily targeting D1 and D2 receptors, as well as serotonin 5-HT2A receptors. It exhibits significant pro-cognitive effects in preclinical models, positioning it as a promising candidate for the treatment of various neurological and psychiatric disorders. Research applications include the exploration of its therapeutic potential in conditions such as schizophrenia and mood disorders. -
5-HT2A Receptor Inhibitor
Belaperidone is a selective 5-HT2A receptor inhibitor, demonstrating significant antidopaminergic and antiserotonergic properties. This compound is primarily employed in research related to neuropsychiatric disorders and may provide insight into therapeutic strategies for conditions such as schizophrenia and depression. Its mechanism of action makes Belaperidone a valuable tool in studying serotonin and dopamine receptor interactions within the central nervous system. -
5-HT4/Dopamine D2 Receptor Agonist
Lirexapride is an agonist of the 5-HT4 and Dopamine D2 receptors. It is primarily known for its stimulatory effects on gastrointestinal motility, making it a valuable tool for researching digestive system disorders. This compound facilitates the study of gastroenterological conditions and the mechanisms underlying gut health and function. -
Antipsychotic Agent
Thiothixene hydrochloride functions as an antipsychotic agent by antagonizing dopamine receptors in the central nervous system. This compound is particularly relevant for research in psychiatric disorders, including borderline personality disorder and schizotypal disorder, facilitating the study of their underlying mechanisms and potential therapeutic strategies. Its application in preclinical and clinical studies underscores its importance in understanding the efficacy and safety of antipsychotic treatments. -
Dopamine Receptor Antagonist
Zicronapine is a potent dopamine receptor antagonist targeting both D1 and D2 subtypes, as well as serotonin receptor 5-HT2A. This compound demonstrates notable pro-cognitive effects in animal models, suggesting its potential utility in the treatment of various neurological and psychiatric disorders. Zicronapine's pharmacological profile makes it a valuable tool for research into psychotropic drug mechanisms and cognitive enhancement strategies. -
5-HT7 Receptor Antagonist
Aramisulpride hydrochloride is a potent 5-HT7 receptor antagonist with a Ki value of 22 nM, demonstrating significant affinity for the D2 and D3 dopamine receptors as well, with Ki values of 140 nM and 13.9 nM, respectively. This compound is primarily utilized in psychiatric research to investigate the roles of serotonin and dopamine pathways in mental health disorders. Its unique pharmacological profile makes it a valuable tool for exploring therapeutic interventions and understanding neurobiological mechanisms. -
5-HT2A Agonist
ECPLA is a highly potent 5-HT2A agonist, exhibiting an EC50 value of 14.6 nM for Gq-mediated calcium signaling. As an analog of lysergic acid diethylamide (LSD), it demonstrates significant affinity for various serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors. ECPLA is valuable for research applications focused on neuropharmacology, receptor signaling pathways, and the exploration of serotonin-related mechanisms. -
D2 Receptor/5-HT Receptor Anagonist
Flumezapine is a potent antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine (5-HT) receptor. This compound has demonstrated the ability to inhibit conditioned avoidance responses in rodent models while maintaining a low risk of extrapyramidal side effects. Flumezapine is valuable in antipsychotic research, particularly in studies exploring the modulation of dopaminergic and serotonergic pathways without altering cortisol levels induced by κ-opioid receptor agonists. -
D2 Receptor Agonist
(Rac)-Rotigotine serves as a dopamine D2 receptor agonist, exhibiting a multifaceted mechanism of action. It is recognized as a full agonist at dopamine receptors and a partial agonist at the 5-HT1A receptor, while also functioning as an antagonist of the α2B-adrenergic receptor, demonstrating Ki values of 0.71 nM for dopamine D3 and 4-15 nM for D2, D5, D4, and dopamine D1 receptors. This compound is primarily utilized in research focused on neurological disorders, particularly in the context of Parkinson's disease and other dopamine-related pathologies. -
5-HT1A Agonist and D2/3 Antagonist
Adoprazine hydrochloride functions as a full agonist at the 5-HT1A receptor, demonstrating a high affinity with a pEC50 of 9 in cloned human receptors. Additionally, it acts as a full antagonist at D2 and D3 receptors, with pA2 values of 9.3 and 8.9, respectively. This compound showcases properties characteristic of atypical antipsychotics, making it relevant for research in neuropharmacology and the treatment of psychiatric disorders. -
Stable Isotope
(Rac)-Rotigotine-d3 hydrochloride is a deuterium-labeled analog of (Rac)-Rotigotine, primarily acting as a full agonist at dopamine receptors. It also serves as a partial agonist of the 5-HT1A receptor and acts as an antagonist at the α2B-adrenergic receptor, showcasing Ki values of 0.71 nM, 4-15 nM, and 83 nM for the respective targets. This stable isotope is vital for pharmacokinetic studies, isotope labeling experiments, and research related to neuropharmacology. -
Dopamine Stabilizer
(-)-OSU6162 hydrochloride is a dopamine stabilizer that functions as a partial agonist at the 5-HT2A receptor while acting as a dopamine D2 antagonist. This compound exhibits significant effects on modulating dopaminergic activity and is relevant for studies exploring aggression and irritability. Its unique mechanism makes it a valuable tool in research investigating neuropsychiatric disorders and dopaminergic regulation. -
5-HT₁A Receptor Agonist
U 93385 is a selective agonist of the 5-HT₁A receptor, primarily involved in neurotransmission modulation. This compound does not exhibit significant activity at α₂ adrenergic or D₂ dopamine receptors, making it suitable for specific studies targeting the 5-HT₁A pathway. U 93385 has been shown to influence heart rate by stimulating the vagus nerve, leading to bradycardia. This makes it a valuable tool for investigating the mechanisms underlying 5-HT₁A receptor-mediated vagal nerve tolerance. -
5-HT Receptor Agonist/Dopamine Receptor Antagonist
SDZ 208-912 is a dual-action compound functioning as a 5-HT1A/2 receptor agonist and a dopamine D1 receptor antagonist. It demonstrates partial dopamine agonism along with atypical neurosedative effects in rodent models. This reagent is valuable for investigating neurological disorders, particularly in the context of schizophrenia research. -
D2 receptor/5-HT2A receptor Antagonist
S18327 is a selective antagonist of the D2 and 5-HT2A receptors, primarily targeting multiple neurotransmitter systems in the brain. Its pharmacological profile suggests efficacy in countering excessive dopamine activity and addressing glutamate hypo-function. S18327 has been shown to reproduce discriminative stimuli similar to Clozapine and may improve cognitive filtering deficits associated with schizophrenia while also exhibiting anxiolytic effects. Additionally, its reduced affinity for histaminergic and muscarinic receptors minimizes the risk of side effects commonly associated with other antipsychotic medications. -
Antipsychotic Agent
PD 158771 is an antipsychotic agent that acts as a partial agonist at D2 and D3 dopamine receptors (Ki = 42.0 nM and 13.7 nM, respectively) and as an agonist at 5-HT1A receptors (Ki = 2.6 nM). This dual activity allows PD 158771 to demonstrate potential in modulating dopaminergic and serotonergic signaling. It is primarily utilized in research focused on understanding the mechanisms underlying psychotic disorders and the development of novel antipsychotic therapies. -
5-HT2A/D2 Antagonist
Blonanserin dihydrochloride is a potent antagonist of the 5-HT2A and dopamine D2 receptors, exhibiting Ki values of 0.812 nM and 0.142 nM, respectively. This compound is primarily utilized as an atypical antipsychotic agent and is relevant for research focused on extrapyramidal symptoms, sedation levels, and hypotensive effects. Its pharmacological profile makes it a valuable tool in the study of neuropsychiatric disorders and related therapeutic interventions. -
D2 Receptor Binder
Mosapramine is a D2 receptor binder that acts as an antipsychotic agent and is a metabolite of Clocapramine. It selectively binds to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, exhibiting a D2/5-HT2 receptor occupancy ratio of 7.4. This compound induces characteristic neuropharmacological effects in rat models, including extrapyramidal symptoms, hyperprolactinemia, and increased salivation, while displaying a lower incidence of weight loss. Mosapramine is valuable for research applications related to schizophrenia and its underlying mechanisms. -
Serotonin/Dopamine Receptor Modulator
Brexpiprazole S-oxide is the primary metabolite of the atypical antipsychotic Brexpiprazole, functioning as a serotonin and dopamine receptor modulator. It exhibits partial agonism at the human 5-HT1A receptor and antagonism at the 5-HT2A receptor, with affinities (Ki) of 0.12 nM and 0.47 nM, respectively, and a potent partial agonist effect at the dopamine receptor (Ki = 0.3 nM). This compound is utilized in research focused on neuropharmacology, psychopharmacology, and the modulation of serotonergic and dopaminergic signaling pathways. -
Dopamine Receptor Antagonist
Pimozide-d4 is a deuterated derivative of Pimozide, functioning primarily as a dopamine receptor antagonist. It demonstrates potent inhibitory activity with Ki values of 1.4 nM, 2.5 nM, and 588 nM against the dopamine D2, D3, and D1 receptors, respectively. Additionally, Pimozide-d4 exhibits affinity for the α1-adrenoceptor (Ki = 39 nM) and inhibits signaling pathways associated with STAT3 and STAT5. This compound is valuable for research focusing on neuropharmacology and the modulation of dopaminergic signaling pathways. -
Stable Isotope
Pimozide-d5 is a stable isotope-labeled form of Pimozide, a potent antagonist of dopamine receptors primarily targeting D2, D3, and D1 receptors with Ki values of 1.4 nM, 2.5 nM, and 588 nM, respectively. This compound also exhibits affinity for the α1-adrenoceptor with a Ki of 39 nM and has been shown to inhibit signaling pathways through STAT3 and STAT5. Pimozide-d5 is valuable in pharmacological studies and research involving dopamine signaling and receptor interaction. -
Stable Isotope
Pimozide-d5 N-Oxide is a deuterium-labeled derivative of Pimozide, which primarily functions as a dopamine receptor antagonist, exhibiting Ki values of 1.4 nM, 2.5 nM, and 588 nM for dopamine D2, D3, and D1 receptors, respectively. Additionally, this compound has notable affinity for the α1-adrenoceptor with a Ki of 39 nM. Pimozide also inhibits the signaling pathways of STAT3 and STAT5, making it relevant for research applications in neurobiology and cancer biology studies. -
Dopamine Receptor Agonist
Apomorphine is a potent dopamine receptor agonist with additional inhibitory effects on monoamine oxidases A and B. It demonstrates neuroprotective properties, evidenced by its ability to reduce reactive oxygen species production, inhibit DNA fragmentation, and downregulate JNK and ERK1/2 phosphorylation. Apomorphine also facilitates the degradation of intracellular Aβ40 and Aβ42, lowers tau protein levels, and suppresses MMP-9 expression. Its radical scavenging and iron chelating capabilities make it valuable for research in neurodegenerative conditions such as Alzheimer's disease and Parkinson's disease, as well as studies related to breast carcinoma and erectile dysfunction. -
D2/H1 Antagonist
Thiethylperazine is a potent antagonist of dopamine D2 and histamine H1 receptors. This phenothiazine derivative exhibits notable anti-emetic, antipsychotic, and antimicrobial properties, making it valuable in various therapeutic contexts. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β (Aβ) load in murine models, thus highlighting its potential relevance in neurodegenerative research. -
Anticholinergic Agent
Benztropine is an orally active anticholinergic agent that effectively crosses the blood-brain barrier. It serves as a dopamine re-uptake inhibitor and a human D2 dopamine receptor allosteric antagonist, making it relevant in Parkinson's disease research. Additionally, Benztropine demonstrates potential anti-cancer stem cell activity, enhancing its applicability in oncology studies. -
Antipsychotic Agent
Levomepromazine maleate is an N-substituted phenylthiazine compound that acts as an antipsychotic agent primarily targeting dopamine receptors. This compound exhibits significant sedative properties and is also a potent inhibitor of CYP2D6, making it a valuable tool for investigating the pharmacological mechanisms underlying schizophrenia. Its multifaceted receptor-blocking activity contributes to its role in research applications related to neuropsychiatric disorders. -
Dopamine Receptor Antagonist
Perphenazine dihydrochloride is a potent antagonist of dopamine receptors, primarily targeting D2 and D3 subtypes, with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it exhibits activity against 5-HT2A and α1A adrenergic receptors. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and inducing apoptosis. Perphenazine dihydrochloride is particularly useful in research focused on mental disorders, oncology, and inflammatory processes. -
5-HT2/D1/D2 Antagonist
Olanzapine hydrochloride is a selective antagonist of serotonin receptors (5-HT2A/2C, 5-HT3) and dopamine receptors (D1, D2). It exhibits high affinity binding to various targets, including H1, muscarinic M1-5, and adrenergic α1 receptors, contributing to its pharmacological profile. This atypical antipsychotic is primarily used in research focusing on neuropharmacology, the treatment of schizophrenia, and mood disorders, providing valuable insights into the modulation of neurotransmitter systems. -
Dopamine D4 Receptor Antagonist
L 741742 is a highly selective antagonist of the dopamine D4 receptor, exhibiting a Ki of 3.5 nM for this target and demonstrating significantly lower affinity for the D2 and D3 receptors. This compound effectively suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, disrupts lysosomal function, and impairs autophagic flux. L 741742 induces G0/G1 cell-cycle arrest and apoptosis, enhances neuronal differentiation in human neural stem cells, and selectively targets the growth of glioblastoma neural stem cells. Its potential therapeutic applications include research in schizophrenia and glioblastoma, with demonstrated synergy when combined with Temozolomide in vitro. -
Dopamine Receptor Antagonist
Flupentixol is an orally active antagonist of D1 and D2 dopamine receptors. This compound exhibits anti-proliferative effects on cancer cells, promoting apoptosis, and has potential applications in the study of schizophrenia, anxiety, and depression. Additionally, Flupentixol has been identified as a new inhibitor of PI3Kα, with an IC50 value of 127 nM, making it a valuable reagent for research in neuropsychiatric disorders and cancer biology. -
Monosaccharide
Rhamnose (L-Rhamnose) is a naturally occurring deoxysugar that primarily targets inflammatory pathways. It has been shown to inhibit pro-inflammatory interleukins and matrix metalloproteinases (MMPs) in models of skin aging, highlighting its potential in anti-aging research. Additionally, Rhamnose enhances the phosphorylation of protein kinase A (PKA) substrates and hormone-sensitive lipase (HSL) in adipocytes, promoting PKA signaling and fat metabolism. Its ability to stimulate dopamine receptors and induce thermogenesis makes Rhamnose a valuable compound in obesity studies, while Rhamnose monohydrate is also utilized in research involving Ehrlich’s solid tumors and sarcomas. -
hD4 Receptor Antagonist
L 741742 hydrochloride is a highly selective antagonist of the human D4 dopamine receptor, exhibiting a Ki value of 3.5 nM for the D4 receptor while demonstrating much lower affinity for D3 and D2 receptors. This compound disrupts signaling pathways associated with PDGFRβ, ERK1/2, and mTOR, and impairs autophagic processes by affecting lysosomal function. Biologically, it induces G0/G1 cell-cycle arrest and apoptosis in various cell types and promotes neuronal differentiation in human neural stem cells. L 741742 hydrochloride is particularly relevant for research on schizophrenia and glioblastoma, demonstrating efficacy against glioblastoma neural stem cells and enhancing the effects of Temozolomide in vitro. -
Histamine Receptor Antagonist
Pimethixene is a potent antagonist of multiple receptor types, primarily functioning as a histamine receptor antagonist. It demonstrates significant activity against serotonin receptors (5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C), dopamine receptors (D2, D4), and muscarinic receptors (M1, M2), with reported pKis of 7.63 to 10.44. This pharmacological profile positions pimethixene as an effective agent for migraine management and offers valuable insights for research into antihistaminic and antiserotonergic therapies. -
Dopamine Receptor Agonist
Proterguride is a potent agonist of dopamine receptors, demonstrating significant potential in modulating dopaminergic signaling. Additionally, it exhibits antagonistic activity at the histamine H(1) receptor and alpha(1)-adrenoceptor, while also partially activating serotonergic 5-HT2A/B receptors. This compound is valuable for research focused on neurological diseases, including Parkinson's disease, providing insights into dopaminergic mechanisms and receptor interactions. -
D2/H1 Antagonist
Norzine dimalate, a potent antagonist of dopamine D2 and histamine H1 receptors, exhibits significant anti-emetic and antipsychotic properties. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β load in murine models. Its diverse biological activities make Norzine dimalate a valuable reagent for research in neuropharmacology and Alzheimer's disease studies. -
Stable Isotope
Benztropine-d3 mesylate is a deuterium-labeled form of the centrally acting anticholinergic agent, Benztropine mesylate. This compound is primarily utilized in Parkinson's disease research and exhibits anti-histaminic properties alongside its function as a dopamine reuptake inhibitor. Additionally, Benztropine mesylate acts as an allosteric antagonist at the human D2 dopamine receptor and demonstrates effects against cancer stem cells (CSCs), making it valuable for studies in both neuropharmacology and oncology. -
Dopamine Receptor Antagonist
Thiothixene is a potent dopamine D2 receptor antagonist, exhibiting selectivity over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). This compound demonstrates significant biological activity by reducing spontaneous and amphetamine-induced locomotor activity in rodent models, thereby influencing behavioral paradigms. Additionally, thiothixene enhances latent inhibition and competitive behavior, suggesting potential applications in understanding psychotropic effects and selective attention. Its diverse receptor binding profile also includes interactions with serotonin, histamine, adrenergic, muscarinic acetylcholine, and sigma receptors, broadening its relevance in psychopharmacological research. -
5-HT Receptor Antagonist
Asenapine citrate is a 5-HT receptor antagonist that exhibits potent activity against serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4), and histamine receptors (pKi: 8.2-9.0). This atypical antipsychotic compound is primarily utilized in research focusing on schizophrenia and bipolar disorder, helping to elucidate the mechanisms of these neuropsychiatric conditions. -
Histamine Receptor Inhibitor
Perphenazine-d8 dihydrochloride is a deuterium-labeled derivative of Perphenazine, primarily functioning as a histamine receptor inhibitor. This compound exhibits potent antipsychotic properties by interacting with serotonin and dopamine receptors. It is valuable for research focused on neuropharmacology, chemical biology, and the study of receptor-ligand interactions in psychiatric disorders. -
Dopamine Receptor Inhibitor
BL-1020 mesylate is a dopamine receptor inhibitor with high affinity for D2L, D2S, and 5-HT2A receptors, exhibiting Ki values of 0.066, 0.062, and 0.21 nM, respectively. This compound functions as an antipsychotic agent and also acts as an agonist at the GABAA receptor, enhancing GABA release with a Ki of 3.74 μM. Furthermore, BL-1020 mesylate interacts effectively with histamine receptors (Ki of 0.47 nM) and demonstrates the ability to diminish amphetamine-induced hyperactivity while minimizing catalepsy and sedation. It penetrates the blood-brain barrier, making it suitable for neurological research applications. -
Drug Metabolite
Quetiapine sulfoxide dihydrochloride is a primary metabolite of the second-generation antipsychotic quetiapine. This compound functions as a 5-HT receptor agonist and a dopamine receptor antagonist, contributing to its pharmacological effects. It is commonly utilized in research related to neuropharmacology and metabolic profiling of antipsychotic drugs, offering insights into the drug's therapeutic activity and safety profile. -
Lurasidone Metabolite
Lurasidone Metabolite 14283 hydrochloride is a significant active metabolite of the antipsychotic agent Lurasidone, which targets serotonin and dopamine receptors. This compound plays a crucial role in the pharmacological activity of Lurasidone, contributing to its efficacy in the treatment of schizophrenia. Research applications include studying the metabolic profile of Lurasidone and its pharmacodynamics in neural systems. -
Drug Metabolite
Quetiapine sulfoxide hydrochloride is a primary metabolite of Quetiapine, a second-generation antipsychotic. This compound acts primarily as a 5-HT receptor agonist and dopamine receptor antagonist, contributing to the pharmacological profile of Quetiapine. It is valuable in research focusing on the metabolism and pharmacokinetics of antipsychotic medications, providing insights into their therapeutic effects and potential side effects. -
Quetiapine Metabolite
7-Hydroxyquetiapine is the primary active metabolite of the antipsychotic agent Quetiapine. It functions by modulating various neurotransmitter systems, particularly serotonin and dopamine receptors, contributing to its therapeutic effects in managing psychiatric disorders. This compound is valuable for studying the pharmacological profile of Quetiapine and investigating its metabolic pathways in both in vitro and in vivo research settings. -
Racemate of NNC 55-0396
(Rac)-NNC 55-0396 is a racemic mixture that targets the dopamine D2 receptor. This compound is of significant interest in neurological research due to its potential role in modulating dopaminergic signaling pathways. It is commonly utilized in studies investigating the pharmacological effects of dopamine receptor antagonists in various neurological disorders. -
DRD4 Antagonist
PD 168568 is a potent and orally active antagonist of the dopamine receptor D4 (DRD4), featuring an isoindolinone structure. It demonstrates strong selectivity for the D4 receptor over D2 and D3 receptors, with Ki values of 8.8 nM, 1842 nM, and 2682 nM, respectively. This compound is valuable for research applications focusing on glioblastoma (GBM), providing insights into the role of DRD4 in tumor biology. -
D3R Antagonist
PF-04363467 is a selective antagonist of the dopamine D3 receptor (D3R). It demonstrates dose-dependent modulation of the electroencephalogram (EEG) profile in freely moving rats, highlighting its potential to influence neural activity. This compound effectively reduces opioid drug-seeking behavior while minimizing undesired side effects associated with D2 receptor antagonism. PF-04363467 is valuable for research into addiction, cognitive disorders, and mental illness.
