Catalog No.
Product Name
Application
Product Information
Citations
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5-HT1A Receptor Agonist
Repinotan is a potent and selective agonist of the 5-HT1A receptor, exhibiting strong brain penetration and oral bioavailability. With Ki values of 0.19 nM in the calf hippocampus, 0.25 nM in rat and human cortex, and 0.59 nM in rat hippocampus, it displays high affinity for target sites while maintaining weak interaction with other related receptors. Repinotan is recognized for its significant neuroprotective properties, making it valuable for research in neuroscience and related therapeutic applications. -
5-HT3 Receptor Antagonist
(R)-Mirtazapine is a selective 5-HT3 receptor antagonist known for its antinociceptive properties demonstrated in animal models of acute thermal nociception. This R( )-enantiomer of Mirtazapine contributes to various neurological studies, particularly in the context of pain modulation and serotonin pathway interactions. (R)-Mirtazapine undergoes metabolism primarily by the enzyme CYP3A4, making it a relevant compound for pharmacokinetic studies in drug metabolism. -
5-HT4 Agonist
ML 10302 is a potent 5-HT4 receptor agonist with a Ki value of 1.07 nM. This compound enhances gut motility by stimulating cholinergic pathways, leading to significant prokinesia in both the small intestine and colon. Additionally, ML 10302 holds potential for research applications in neurological diseases, providing insights into therapeutic mechanisms targeting the gastrointestinal and nervous systems. -
5-HT Agonist
PNU-22394 hydrochloride is a potent agonist for the 5-hydroxytryptamine (5-HT) receptors, specifically engaging the 5-HT2C and 5-HT2A receptor subtypes with Ki values of 6.1 nM and 10 nM, respectively. This compound is valuable for studying the roles of 5-HT in neurobiology and its implications in various psychiatric disorders. Its selective action on serotonin receptors makes it a useful tool for investigating serotonin signaling pathways and potential therapeutic interventions. -
5HT3A Receptor Antagonist Ligand
GR119566X is a high-affinity antagonist of the 5HT3A receptor, effectively inhibiting receptor activity. This compound is suitable for use in affinity purification experiments involving 5-HT3 receptors, providing a valuable tool for investigating receptor function and pharmacology. Its specificity for the 5HT3A receptor makes it useful for diverse applications in neurobiology and drug discovery research. -
5-HT2 Receptor Antagonist
Fananserin is a potent and selective antagonist of the 5-hydroxytryptamine 2 (5-HT2) receptor, exhibiting a Ki value of 0.37 nM for the rat 5-HT2A receptor. Additionally, Fananserin serves as a selective antagonist for the dopamine D4 receptor, with a Ki of 2.93 nM for the human variant. This compound is valuable for research exploring the modulation of serotonin and dopamine pathways, offering insights into potential therapeutic applications in neuropsychiatric disorders. -
5-HT Receptor Antagonist
5-HT2A antagonist 1 is a selective antagonist of the 5-HT2A receptor, playing a crucial role in modulating serotonin signaling. This compound demonstrates potential in alleviating gastrointestinal disorders and may also have applications in addressing circulatory system irregularities. Its pharmacological profile makes it a valuable tool for research in serotonergic pathways and their implications in various biological systems. -
5-HT4 Receptor Partial Agonist
CJ033466 is a selective partial agonist of the 5-HT4 receptor, exhibiting an EC50 of 9 nM. This compound demonstrates significant gastroprokinetic effects, making it a valuable tool for research applications related to gastrointestinal motility and related disorders. Its specificity towards the 5-HT4 receptor aids in elucidating receptor-mediated pathways and potential therapeutic interventions. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole (hydrochloride) functions as an α2-adrenoceptor antagonist and a serotonin (5-HT) reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is particularly relevant for research into depression and related neuropsychiatric disorders, facilitating studies on serotonin modulation and adrenergic signaling pathways. Its dual action can provide insights into the mechanisms underlying mood regulation and therapeutic interventions. -
5-HT1A Agonist
R(+)-8-OH-DPAT hydrobromide is a selective agonist of the 5-HT1A receptor, known for its significant efficacy in modulating serotonergic signaling. This compound enhances dopamine release in the medial prefrontal cortex, thereby providing valuable insights into the relationship between serotonin and dopamine neurotransmission. R(+)-8-OH-DPAT is widely utilized in research focused on neuropharmacology and behavioral studies related to mood disorders and cognition. -
5-HT Receptor
(R,R)-Palonosetron Hydrochloride is a selective antagonist of the 5-HT3 receptor. This compound exhibits significant antiemetic properties, making it valuable in the prevention of chemotherapy-induced nausea and vomiting. Its high affinity for the 5-HT3 receptor can also facilitate research on serotonin signaling pathways and their role in gastrointestinal function and neurological disorders. -
5-HT Receptor Agonist
Revexepride is a selective agonist of the 5-HT4 receptor, exerting effects on gastrointestinal motility and potentially influencing CYP3A4 enzyme induction. Its primary biological activity includes the enhancement of gastrointestinal function, making it a candidate for research in digestive disorders such as gastroesophageal reflux disease. This compound is relevant for studies investigating serotonergic modulation in gastrointestinal diseases and the metabolic implications associated with CYP3A4 activity. -
5-HT2C Receptor Agonist
Ro60-0175 fumarate acts as a potent and selective agonist of the 5-HT2C receptor, which is involved in various neurophysiological processes. This compound has demonstrated significant activity in modulating serotonin signaling pathways, making it a valuable tool for research into mood regulation, anxiety, and appetite control. It is suitable for studies focused on the pathophysiology of psychiatric disorders and the development of novel therapeutic strategies. -
D3R/5-HT2AR Antagonist/5-HT1AR Agonist
D3/5-HT receptor modulator-1 is a selective antagonist for dopamine D3 receptors and 5-HT2A receptors, while also functioning as a partial agonist at 5-HT1A receptors. With measured Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the respective targets, this compound exhibits a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. Its unique pharmacological profile suggests potential applications in the development of atypical antipsychotic therapies and for studying dopaminergic and serotonergic signaling pathways. -
5-HT2C/2B Receptor Antagonist
SB228357 is a selective and potent antagonist of the 5-HT2C and 5-HT2B receptors, exhibiting pKi values of 6.9, 8.0, and 9.0 for the 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. This compound demonstrates significant antidepressant and anxiolytic effects, making it valuable for research focused on mood disorders and anxiety-related conditions. Its oral bioavailability further enhances its utility in pharmacological investigations. -
5-HT Antagonist
(S)-WAY 100135 dihydrochloride is a highly selective and potent antagonist of the 5-HT 1A receptor, exhibiting an IC50 of 33.9 nM. This compound demonstrates anxiolytic effects in animal models, making it a valuable tool for research in anxiety disorders and related neuropharmacological studies. Its specificity for the 5-HT 1A target enables investigations into serotonin receptor-mediated signaling pathways and their implications in various psychiatric conditions. -
5-HT2A Receptor Agonist
LPH-5 is a selective agonist of the 5-HT2A receptor, exhibiting an EC50 of 190 nM. Through its activation of the 5-HT2A receptor, LPH-5 plays a critical role in modulating mood, perception, and various central nervous system processes. This compound is valuable for investigating the involvement of the 5-HT2A receptor in psychiatric disorders such as depression, anxiety, and substance use disorders. -
5-HT4 Receptor Agonist
Relenopride hydrochloride is a selective agonist of the 5-HT4 receptor, exhibiting a Ki value of 4.96 nM, which confirms its high affinity for this target. With significantly lower affinities for the 5-HT2A and 5-HT2B receptors, Relenopride hydrochloride is a valuable tool for studying gastrointestinal physiology. It is primarily utilized in research on enhancing gastrointestinal motility and investigating conditions related to digestive function. -
α2B/C-Adrenergic Receptor Antagonist
ARC 239 is a selective antagonist of the α2B and α2C adrenergic receptors, exhibiting a pKi of 7.06 for rat kidney α2B and 6.95 for human α2C. In addition, ARC 239 inhibits the 5-HT1A receptor with a Ki value of 63.1 nM. This compound is valuable in research involving adrenergic signaling pathways and the modulation of neurotransmitter systems, making it suitable for studies on cardiovascular function and psychiatric disorders. -
5-HT2C Agonist
5-HT2C agonist-3 is a selective agonist for the 5-HT2C receptor, exhibiting an EC50 of 24 nM and a Ki of 78 nM. This compound demonstrates antipsychotic-like properties and effectively inhibits amphetamine-induced hyperactivity. It serves as a valuable tool for research into neuropharmacology and the modulation of serotonergic systems. -
5-HT/Serotonin Receptors Ligand
1-(2-Methoxyphenyl)piperazine hydrochloride is a ligand targeting 5-HT (serotonin) receptors, crucial for the development of various antipsychotic agents. Its high affinity for serotonin receptors makes it a valuable compound in synthesizing pharmacological agents, such as Piperazine phosphate, Piperazine citrate, and Fluphenazine dihydrochloride. Additionally, this reagent can be utilized in the synthesis of Rifampicin, contributing to studies in neuroscience and psychiatric research. -
Ziprasidone Impurity
Keto Ziprasidone is a known impurity of the antipsychotic agent Ziprasidone, which functions primarily as a combined antagonist of serotonin (5-HT) and dopamine receptors. This compound is crucial for research applications focusing on drug metabolism and pharmacokinetics, particularly in understanding the potential effects of impurities on therapeutic efficacy and safety profiles. Its analysis can aid in the development of quality control measures in pharmaceutical formulations. -
5-HT(6/7/2A)/ Dopamin D2 Receptors Antagonist
5-HT6/7 Antagonist 1 is a potent antagonist of the 5-HT6, 5-HT7, and D2 receptors, exhibiting selectivity that spares M1 receptors and hERG channels. This compound's multifunctional activity makes it valuable for research into neuropharmacology and the modulation of serotonergic and dopaminergic systems. It provides a useful tool for studying disorders related to these receptor pathways, including anxiety, depression, and schizophrenia. -
5HT-4/5HT-3 Antagonist
Lintopride is a benzamide that acts as a potent antagonist of the 5HT-4 receptor, with moderate antagonistic properties at the 5HT-3 receptor. This compound enhances gastric emptying, stimulates motility in the antrum and duodenum, and accelerates intestinal transit in animal models. Additionally, Lintopride significantly increases the basal tone of the lower oesophageal sphincter, highlighting its potential applications in gastrointestinal research and therapy. -
Ziprasidone Impurity
Hydroxy ziprasidone is a known impurity of the antipsychotic agent ziprasidone, which functions primarily as a combined antagonist of both serotonin (5-HT) and dopamine receptors. This compound is useful for researchers studying the pharmacological properties and metabolic pathways of ziprasidone, as well as for quality control in the synthesis of pharmaceutical formulations. Its presence can provide insights into the drug's safety, efficacy, and potential side effects. -
Cannabinoid Receptor Agonist
AM9405 is a selective agonist for cannabinoid receptor type 1 (CB1) and serotonin type 3 (5-HT3) receptors. It demonstrates potent inhibitory effects on twitch contractions in the ileum and colon, with half-maximal inhibitory concentrations (IC50) of 45.71 nM and 0.076 nM, respectively. AM9405 is valuable for research in gastrointestinal motility and cannabinoid signaling pathways. -
5-HT5A Receptor Probe
UCSF648 is a chemical probe targeting the 5-HT5A serotonin receptor. It demonstrates weak activation of the ADRA2A and MTNR1A receptors, making it valuable for studies investigating serotonin signaling pathways. This reagent is suitable for research applications related to neuropharmacology and the modulation of serotonin receptor activity. -
5-HT1A Receptor Agonist
Tandospirone hydrochloride is a selective partial agonist of the 5-HT1A receptor, exhibiting a Ki value of 27 nM. This compound displays notable anxiolytic and antidepressant properties, making it valuable in the study of central nervous system disorders. Its unique action at the 5-HT1A receptor contributes to the understanding of underlying mechanisms related to anxiety and depression, facilitating research aimed at developing novel therapeutic approaches. -
Dopamine D2/D3/5-HT7 Receptor Inhibitor
LB-102 is an orally bioavailable inhibitor of dopamine D2, D3, and 5-HT7 receptors. It exhibits significant antagonistic activity, making it a valuable tool for investigating the neurochemical pathways involved in schizophrenia and other psychiatric disorders. This compound is useful for studies aimed at understanding the role of these receptors in various neuropsychiatric conditions. -
5-HT/DA Receptor Antagonist
Ziprasidone mesylate trihydrate is an orally active antagonist of serotonin (5-HT) and dopamine (DA) receptors, primarily targeting the 5-HT2A and D2 receptor subtypes. With a high affinity for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM), and 5-HT1A (Ki=3.4 nM), this compound is significant for studies related to mood disorders, schizophrenia, and neuropharmacology. Ziprasidone mesylate trihydrate serves as a valuable tool for exploring receptor mechanisms and assessing therapeutic effects in relevant biological models. -
TAAR1/5-HT1A Agonist
Ulotaront is a novel TAAR1 and 5-HT1A agonist that operates through a distinct mechanism separate from traditional D2 and 5-HT2A pathways. This compound exhibits significant antipsychotic-like properties, making it a valuable tool for researching schizophrenia and related neuropsychiatric disorders. Its unique profile allows for exploration of alternative treatment strategies that may enhance therapeutic options for psychiatric conditions. -
5-HT Receptor Antagonist
Clocapramine is a selective antagonist of the 5-HT2A receptor, with additional inhibitory effects on D2 dopamine receptors. This compound exhibits notable properties in modulating serotonin and dopamine signaling, making it relevant for neuropharmacological research. Clocapramine can be utilized in studies related to psychiatric disorders, including depression and schizophrenia, as well as the characterization of receptor interactions in neural pathways. -
PKC Inhibitor
NA 0345 is a potent protein kinase C (PKC) inhibitor, exhibiting IC50 values of 70 nM in the presence of 12-O-tetradecanoyl-13-acetate and 110 nM in its absence. This compound selectively inhibits PKC activity, effectively reducing the positive inotropic effects associated with α1-adrenergic receptors. NA 0345 is useful in research applications aimed at elucidating the role of PKC in cardiovascular function and signal transduction pathways. -
Protein Kinase C Inhibitor/LTD4 Antagonist
LY 170198 is a potent protein kinase C inhibitor and LTD4 antagonist. This compound exhibits significant biological activity relevant to studies on tumor promotion, oncogene activation, and protein phosphorylation. Additionally, it is valuable for investigating feedback mechanisms in signal transduction pathways and cellular responses to growth factors, making it a useful tool for cancer research and related fields. -
PAD4 Inhibitor
JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research. -
Dopamine D2 Receptor Modulator
PAOPA is an allosteric modulator of the dopamine D2 receptor, derived from the analog of L-proline-L-leucine-glycine amide (PLG) peptide. This compound demonstrates significant potential in mitigating behavioral abnormalities in rodent models of schizophrenia. PAOPA enhances the receptor's affinity and promotes its binding to agonists, making it a valuable tool for research focused on neuropsychiatric disorders. -
Dopamine Receptor Antagonist
Dopamine D2 receptor antagonist-1 is a negative allosteric modulator of the dopamine D2 receptor (D2R) that exhibits sub-micromolar affinity. This compound is utilized in research studying dopaminergic signaling pathways and provides insights into neurological disorders associated with D2R dysfunction. Its role in modulating receptor activity makes it a valuable tool for exploring pharmacological interventions in the central nervous system. -
Dopamine Receptor
Quinpirole is a selective agonist of the dopamine D2 and D3 receptors, primarily targeting central nervous system functions. It is known to reduce hypothalamic norepinephrine concentrations, influencing dopaminergic signaling pathways. Quinpirole's unique mechanism results in decreased dopamine metabolites and potential increased levels of 3-methoxy-4-hydroxyphenylglycol (MHPG) sulfate, making it valuable for research on neuropharmacology and the modulation of mood and behavior. -
Dopamine D4 Receptor Agonist
CP 226269 is a potent agonist of the dopamine D4 receptor, demonstrating significant calcium flux induction with an EC50 of 32 nM. This compound also stimulates phospholipid methylation (PLM) in SK-N-MC neuroblastoma cells, exhibiting an EC50 of 2.9 nM. CP 226269 is utilized in research related to schizophrenia and other neuropsychiatric disorders, providing valuable insights into dopamine receptor functions. -
Dopamine Receptor Modulator
OPC 4392 hydrochloride is a modulator of dopamine receptors, acting as an agonist at presynaptic receptors while antagonizing postsynaptic D2 receptors. This compound has demonstrated the ability to reverse dopamine accumulation induced by Reserpine and inhibit stereotypic and climbing behaviors triggered by Apomorphine in mouse models. It serves as a valuable tool for investigating dopamine-related pathways and behaviors in neurological research. -
D1-like Dopamine Receptor PAM
MLS1082 is a pyrimidone-derived positive allosteric modulator targeting the D1-like dopamine receptors. It exhibits an EC50 of 123 nM for enhancing dopamine-stimulated G protein signaling. This compound is valuable for research applications focused on dopamine receptor pharmacology and the modulation of neurotransmitter systems. -
Dopamine Receptor Antagonist
Odapipam (NNC 756) is a selective dopamine D1 receptor antagonist, exhibiting high affinity with a Kd of 0.18 nM. This compound serves as a valuable tool in neuroscience research, particularly for studying dopaminergic signaling pathways and related neuropsychiatric disorders. In addition, Odapipam functions as an effective radiotracer for positron emission tomography (PET) imaging, enhancing the investigation of receptor dynamics in vivo. -
Dopamine Autoreceptor Agonist
Preclamol hydrochloride is a selective dopamine autoreceptor agonist, primarily targeting the D2 dopamine receptor. This compound exhibits significant biological activity in modulating dopamine signaling, making it a valuable tool for investigating the pathophysiology of schizophrenia. Its applications extend to neuropharmacology studies, aiding in the development of therapeutic strategies for dopaminergic dysregulation. -
D3 Receptor Antagonist
YQA14 is a high-affinity antagonist of the dopamine D3 receptor. It exhibits significant anti-opioid addiction activity, demonstrating the ability to inhibit morphine- and cocaine-induced conditioned place preference (CPP) in preclinical models. This compound is valuable for research into the mechanisms of addiction and the development of therapeutic strategies for substance use disorders. -
Dopamine Receptor Inhibitor
7-Hydroxy-DPAT hydrobromide is a selective agonist for the D3 dopamine receptor, primarily impacting dopamine signaling pathways. This compound demonstrates significant biological activity in modulating locomotor behavior and influencing dopamine metabolism within the central nervous system. It serves as a valuable tool for research applications related to neuropharmacology and the study of dopamine-related disorders. -
Dopamine Receptor Agonist
Talipexole is a selective dopamine receptor agonist primarily targeting D2-like receptors. It is proposed for use as an antiparkinsonian agent, demonstrating potential in improving motor function in Parkinson's disease models. Research applications include studying dopaminergic signaling pathways and exploring therapeutic options for neurodegenerative disorders. -
D3 Receptor Antagonist
Mesdopetam hemitartrate is a selective antagonist of the dopamine D3 receptor, exhibiting a Ki value of 90 nM and an IC50 of 9.8 μM for human recombinant D3 receptors. This compound demonstrates psychomotor stabilizing effects, making it a valuable tool in the investigation of motor and psychiatric complications associated with Parkinson's disease. Its unique properties contribute to research aimed at understanding the underlying mechanisms of dopamine-related disorders. -
Dopamine D3 Receptor Antagonist
Mesdopetam is a selective antagonist of the dopamine D3 receptor, displaying a Ki value of 90 nM and an IC50 of 9.8 μM for the human recombinant D3 receptor. This compound exhibits psychomotor stabilizing properties and is utilized in research focused on motor and psychiatric complications associated with Parkinson's disease. Its role in modulating dopamine signaling makes it valuable for studying therapeutic strategies in this context. -
DRD4 Antagonist
PD 168568 dihydrochloride is a potent and orally active antagonist of the dopamine receptor D4 (DRD4). This compound exhibits selectivity for the D4 receptor, with Ki values of 8.8 nM for DRD4 compared to 1842 nM for DRD2 and 2682 nM for DRD3. PD 168568 dihydrochloride is applicable in glioblastoma (GBM) research, making it a valuable tool for investigating the role of DRD4 in cancer biology and potential therapeutic strategies. -
Dopamine
AJ-76 hydrochloride is a potent antagonist of dopamine autoreceptors, exhibiting pKi values of 6.95, 6.67, 6.37, 6.21, and 6.07 for human D3, D4, D2 short, D2 long, and rat D2 receptors, respectively. This compound is valuable for research focused on dopamine receptor modulation and its implications in neurological disorders. Its specific receptor affinity allows for investigations into the roles of dopamine signaling in various physiological and pathological processes.
