Catalog No.
Product Name
Application
Product Information
Citations
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5-HT2A Receptor Agonist
5-HT2A receptor agonist-8 is a highly effective agonist of the 5-HT2A receptor, exhibiting an EC50 of 0.6784 nM. This compound is valuable for investigating the neuropharmacological mechanisms underlying depressive disorders and bipolar disorders. Its potency makes it a significant tool for research in psychiatric and neurological studies focused on serotonin signaling pathways. -
5-HT2A/D4 Antagonist
Pipamperone dihydrochloride is a potent antagonist of the 5-HT2A (pKi=8.2) and D4 (pKi=8.0) receptors, derived from the butyrophenone class. It exhibits low-affinity antagonism at the D2 receptor (pKi=6.7) and is known to influence neurotransmitter systems, contributing to its antipsychotic effects. This compound is utilized in research focused on mental health disorders, including autism-related behavioral conditions and Alzheimer's disease. -
MT1/2 Agonist and 5-HT2C Antagonist
7-Desmethyl-3-hydroxyagomelatine is an MT1/2 agonist and a 5-HT2C antagonist. As a metabolite of Agomelatine, it demonstrates reduced biological activity compared to its parent compound. This reagent can be utilized in research focusing on circadian rhythms, mood regulation, and the interaction of melatonergic and serotonergic pathways in neuropharmacology. Its unique profile makes it a valuable tool for studying various neuropsychiatric disorders. -
5-HT2B Antagonist
VU0530244 is a highly potent antagonist of the serotonin 5-HT2B receptor, exhibiting an IC50 of 17.3 nM. Due to its predicted properties, VU0530244 is expected to have minimal brain penetration in human subjects and is likely a substrate for P-glycoprotein-mediated efflux. This compound is useful for research applications focused on serotonin receptor signaling and its implications in various physiological and pathological processes. -
5-HT Receptor
Renzapride hydrochloride is a benzamide derivative primarily targeting 5-HT receptors. It exhibits antagonistic activity at 5-HT(3) receptors and agonistic activity at 5-HT(4) receptors, which contributes to its efficacy in treating irritable bowel syndrome. Additionally, Renzapride hydrochloride shows antagonistic properties at 5-HT(2B) receptors and demonstrates significant affinity for 5-HT(2A) and 5-HT(2C) receptors, making it a valuable tool in gastrointestinal research and the study of serotonin receptor mechanisms. -
Stable Isotope
Arotinolol-d5 hydrochloride is a deuterated analog of Arotinolol, a nonselective α/β-adrenergic receptor blocker with vasodilatory properties. This compound exhibits notable activity in inhibiting the binding of the radioligand 125I-ICYP to 5HT1B serotonergic receptor sites. Arotinolol serves as an effective antihypertensive agent and is utilized in research related to various cardiovascular and non-cardiovascular diseases. -
5-HT2 Antagonist
AT1015 hydrochloride is a potent antagonist of the 5-HT2 receptor, exhibiting a pKi value of 7.94. This compound has been shown to inhibit vasoconstriction and effectively block platelet aggregation, making it a valuable research tool for studies related to cardiovascular and hemostatic functions. Its properties render it suitable for investigating the physiological and pathological roles of serotonin signaling in various biological systems. -
5-HT6 Agonist
WAY-181187 oxalate is a selective full agonist of the 5-HT6 receptor, exhibiting a binding affinity with a Ki of 2.2 nM and an effective concentration for half-maximal activation (EC50) of 6.6 nM. This compound engages 5-HT6 receptor-mediated signaling pathways, influencing cAMP, Fyn, and ERK1/2 kinase activity. It serves as a valuable tool for research into neuropharmacology and potential therapeutic applications targeting cognitive disorders. -
TAAR1/5-HT1A Agonist
SEP-363856 mesylate is a selective agonist for the trace amine-associated receptor 1 (TAAR1) and the 5-HT1A receptor, exhibiting unique psychotropic effects through a non-dopaminergic mechanism of action. This compound demonstrates antipsychotic-like activity, making it a valuable tool for investigating the pathophysiology and treatment of schizophrenia. Its distinct mechanism provides a novel approach to research in mental health disorders, particularly in areas where traditional therapies may be ineffective. -
5-HT Receptor Antagonist
Xylamidine is a peripheral 5-HT receptor antagonist that serves as a valuable tool for studying the appetite suppressant effects associated with 5-hydroxytryptophan (5-HTP) and fenfluramine. Experimental results indicate that xylamidine attenuates the decrease in food intake caused by 5-HT and 5-HTP, while showing no significant effect on fenfluramine. This suggests that the appetite-suppressing properties of 5-HTP may be mediated partially through peripheral 5-HT receptors. Additionally, xylamidine has been shown to reverse the impact of 5-HTP on food intake rate, highlighting its role in dissecting the underlying mechanisms of peripheral appetite regulation. -
5-HT2C Receptor Agonist
Org37684 is a potent agonist of the 5-HT2C receptor, displaying a pEC50 value of 8.17. It demonstrates a preferential selectivity, being approximately 2.5 times more potent at the 5-HT2C receptor compared to the 5-HT2B receptor (pEC50=7.96) and ten times more potent than the 5-HT2A receptor (pEC50=7.11). This compound is utilized in research applications focused on the regulation of mood, appetite, and other neuropharmacological processes mediated by serotonin receptors. -
5-HT1AR Agonist/α1-Adrenergic Receptor Antagonist
Enciprazine dihydrochloride is an orally active non-benzodiazepine anxiolytic that functions as a 5-HT1A receptor agonist and α1-adrenergic receptor antagonist. This compound demonstrates key biological activity by inducing electroencephalogram changes, characterized by a reduction in δ and θ wave power and an increase in α and fast β wave power. Enciprazine dihydrochloride exhibits anti-aggressive properties, alongside minimal sedative and ataxic effects. It also modulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis, making it a valuable reagent for research into anxiety disorders, generalized anxiety syndrome, and psychosis. -
5-HT Receptor
Gevotroline is a potent antagonist of the 5-HT receptor. It demonstrates significant affinity for this target, making it a valuable tool in researching psychotomimetic effects. This compound is particularly useful in studies exploring the modulation of serotonin-related pathways and their impact on neurological functions. -
5-HT Receptor Antagonist
Alosetron-d3 is a deuterium-labeled derivative of Alosetron, which acts as a serotonin 5-HT3 receptor antagonist. This compound plays a critical role in the study of gastrointestinal disorders, particularly in research focused on irritable bowel syndrome (IBS). Its unique isotopic labeling allows for advanced utilization in pharmacokinetic and metabolic studies, enhancing the understanding of drug behavior in biological systems. -
5-HT Receptor Agonist
Lesopitron (E-4424) is a potent agonist of the 5-HT receptor, exhibiting significant anxiolytic-like effects. It inhibits forskolin-stimulated adenylate cyclase activity with an IC50 value of 125 nM, making it a valuable tool for research in neuropharmacology and anxiety disorders. This compound is suitable for studies investigating serotonin signaling pathways and their impact on mood regulation. -
5-HT3 Receptor Antagonist
(S)-Ramosetron is an orally active antagonist of the 5-hydroxytryptamine 5-HT3 receptor. It exhibits significant antiemetic properties, making it valuable for research into conditions associated with nausea and vomiting, as well as irritable bowel syndrome (IBS). Its antagonistic action allows for investigations into the modulation of gastrointestinal motility and neurochemical signaling pathways involved in these disorders. -
5-HT1A Receptor Inhibitor
LY 178210 is a selective partial agonist of the 5-HT1A receptor, exhibiting Ki values of 0.67 nM for 5-HT1A and 380 nM for 5-HT1D receptors, thereby demonstrating its specificity. Its minimal activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors makes it a valuable tool in neuropharmacology. Additionally, LY 178210 effectively inhibits forskolin-stimulated cyclase activity, though with lower potency compared to full agonists like 8-OH-DPAT. This compound is significant for studies on serotonergic modulation, as it markedly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the hypothalamus while increasing serum corticosterone concentrations. -
5-HT2A Antagonist
AT-1015 is a selective, orally active antagonist of the 5-HT2A serotonin receptor. It demonstrates significant antithrombotic properties by prolonging arterial occlusion time in thrombus formation. Additionally, AT-1015 inhibits platelet aggregation and vasoconstriction, making it a valuable compound for research in cardiovascular and hematological applications. -
5-HT4 Receptor Ligand
R 116712 is a selective ligand for the 5-HT4 receptor, demonstrating high affinity and specificity. This compound plays a key role in research applications related to neuropharmacology and gastrointestinal motility. Additionally, R 116712 can be utilized in the development of isotopic markers to further enhance studies in receptor pharmacology and signaling pathways. -
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-HT1A Receptor Agonist
Org 13011 is a selective 5-HT1A receptor agonist that acts on the central nervous system. It has been shown to induce conditioned taste aversion, making it a valuable tool for studying the mechanisms underlying learning and memory processes. This compound is relevant for research focused on anxiety, depression, and other neuropsychiatric disorders. -
5-HT Receptor Modulator
ML10375 is a modulator of the 5-HT4 and 5-HT2 serotonin receptors, impacting gap junction coupling in rat atrial myocytes. It plays a significant role in the regulation of intracellular cAMP levels and influences L-type calcium currents. This compound is useful for investigating serotonergic pathways and their effects on cardiac physiology. -
5-HT4 receptor Antagoinst
GR125487 is a highly selective antagonist of the 5-HT4 receptor, exhibiting a Kd value of 0.1 nM. It demonstrates minimal binding affinity for 5-HT3 receptors (Kd > 1 μM), ensuring specificity in its action. GR125487 effectively inhibits the memory-enhancing effects of BIMU1 without significantly affecting baseline social memory. This compound is valuable for investigating mechanisms underlying social olfactory memory and related cognitive processes. -
5-HT Receptor Agonist
(RS)-Minesapride is a selective agonist of the 5-HT receptor, primarily targeting the serotonin pathways involved in gastrointestinal motility. This compound demonstrates potential therapeutic efficacy in treating irritable bowel syndrome with predominant constipation (IBS-C). Its pharmacological profile makes it a valuable tool for research into gastrointestinal disorders and the modulation of serotonin receptor activity. -
5-HT1A Receptor Agonist
AP-521 free base is a benzothienopyridine derivative that functions as a potent agonist of the 5-HT1A receptor. Its primary mechanism involves enhancing serotonergic transmission, leading to significant anxiolytic effects in the medial prefrontal cortex (mPFC). This compound holds promise for research applications focused on anxiety disorders and related neurobiological mechanisms. -
5-HT1A Receptor Agonist
LY-228729 is a selective agonist of the 5-HT1A receptor, known for its significant effects on behavior. This compound has been shown to decrease rearing frequency and overall activity in rats during open field tests, as well as reduce immobility and enhance swimming time in forced swim tests. LY-228729 serves as a valuable tool in the investigation of neurological disorders and the modulation of serotonin-related pathways. -
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. -
h5-HT1D Antagonist
BRL-15572 is a selective antagonist of the h5-HT1D receptor, exhibiting high affinity for this target. It is a valuable pharmacological tool for the characterization of 5-HT1D receptor-mediated responses, aiding in the understanding of its role in various biological processes. Research applications include studies on serotonergic signaling pathways and the exploration of potential therapeutic interventions. -
5-HT Receptor Agonist
2-Methyl-5-HT hydrochloride is a selective agonist of the 5-HT3 receptor. This compound exhibits significant biological activity, notably demonstrating anti-depressive-like effects in various models. Its properties make it a valuable tool for research into serotonin receptor pharmacology and the investigation of potential therapeutic applications in mood disorders. -
5-HT1A Receptor Agonist
Alnespirone is a selective, orally active 5-HT1A receptor agonist with a binding affinity (K0.5) of 0.2 nM. It exhibits significant antidepressant-like and anxiolytic properties, making it a valuable tool for research into mood disorders and anxiety-related conditions. Alnespirone may be useful in understanding the therapeutic potential of 5-HT1A receptor modulation in pharmacological studies. -
5-HT1A Receptor Agonist
Org-13011 fumarate is a selective 5-HT1A receptor agonist that exhibits central nervous system activity. This compound has been shown to induce conditioned taste aversion, making it a valuable tool for studying behavioral neuroscience and the mechanisms of aversion learning. Its specific action on serotonin receptors also positions Org-13011 fumarate as a potential candidate for research into anxiety and mood disorders. -
5-HT Receptor
Binospirone hydrochloride is a selective antagonist of the 5-HT1A receptor, a key target in serotonergic signaling pathways. This compound is primarily used in research to investigate the role of serotonin in mood regulation and anxiety disorders. Its activity provides insights into the mechanisms underlying various neurological conditions, making it a valuable reagent in pharmacological studies. -
5-HT2/5-HT7 Antagonist
LY215840 is a selective antagonist of the 5-HT2 and 5-HT7 serotonin receptors. This compound effectively inhibits serotonin-induced vasorelaxation in the canine coronary artery, demonstrating significant potential for research in cardiovascular pharmacology and serotonin receptor signaling. Its application extends to studies exploring the role of serotonin receptors in various physiological and pathological processes. -
r5-HT1B Receptor Antagonist
NAS-181 is a potent and selective antagonist of the rat 5-hydroxytryptamine 1B (r5-HT1B) receptor, exhibiting an Ki value of 47 nM. This compound has demonstrated an ability to increase 5-hydroxytryptophan (5-HTP) accumulation in various rat brain regions. Its significant biological activity makes NAS-181 a valuable tool for investigating serotonergic signaling pathways and their implications in neuropharmacological research. -
5-HT2C Agonist
5-HT2C agonist-9 is a high-affinity agonist for the 5-HT2C receptor, displaying an EC50 of 1.4 nM for human 5-HT2C. This compound serves as a valuable tool in the investigation of various neuropsychiatric disorders, including depression, drug addiction, alcoholism, post-traumatic stress disorder (PTSD), and neuropathic pain. Its potent activity at the 5-HT2C receptor may facilitate research aimed at understanding the therapeutic potentials within these conditions. -
5-HT2 Receptor Antagonist
SUN C5174 is a selective antagonist of the 5-HT2 receptor that demonstrates mild sympathomimetic activity. This compound has been shown to alleviate disorders in experimental models related to peripheral circulatory disturbances. Additionally, SUN C5174 exhibits favorable pharmacokinetic properties, making it a valuable tool for investigations into cardiovascular functions and related pathologies. -
5-HT6/5-HT2AR Antagonist
5-HT6/5-HT2AR antagonist-1 is a potent dual antagonist targeting the 5-HT6 and 5-HT2A receptors, exhibiting Ki values of 11 nM and 39 nM, respectively. This compound's inhibition of serotonergic signaling pathways is relevant in the study of neuropsychiatric disorders and cognitive function. Its dual-action mechanism makes it a valuable tool for researchers exploring the therapeutic potential in conditions such as schizophrenia and Alzheimer's disease. -
5-HT1A Receptor Antagonist
SDZ 216-525 is a selective silent antagonist of the 5-HT1A receptor, which plays a critical role in serotonin neurotransmission. This compound exhibits potent inhibition of 5-HT1A receptor activity, making it valuable for research into anxiety, depression, and schizophrenia. Its specificity allows for precise studies of serotonin-related pathways in various biological systems. -
h5-HT1D Antagonist
BRL-15572 hydrochloride is a selective antagonist of the h5-HT1D receptor, exhibiting high affinity for this target. This compound can be utilized as a pharmacological tool to investigate h5-HT1D receptor-mediated responses, contributing to research in neuropharmacology and serotonin signaling pathways. Its specificity makes it an important reagent for studying the role of h5-HT1D in various physiological and pathological processes. -
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. -
5-HT2C/2B Receptor Antagonist
SB-221284 is a selective antagonist of the 5-HT2C and 5-HT2B receptors, exhibiting pKi values of 6.4, 7.9, and 8.6 for the 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. This compound is valuable in studying the role of serotonergic signaling in neurological diseases and may contribute to the development of therapeutic strategies targeting these receptors. Its specificity makes it a useful tool for researching the physiological and pathological functions associated with serotonin receptors. -
5-HT2C Receptor Agonist
5-HT2C Agonist-11 is a selective agonist of the 5-HT2C receptor, demonstrating significant potency with an EC50 of 15 nM. This compound activates the Gq protein signaling pathway, leading to intracellular calcium release. 5-HT2C Agonist-11 holds potential for research applications related to depression, post-traumatic stress disorder (PTSD), and neuropathic pain. -
5-HT2AR Agonist
5-HT2A receptor agonist-11 is a specific agonist for the 5-HT2A receptor, exhibiting an EC50 of 22 nM. This compound plays a significant role in studying the mechanisms underlying mental illnesses and central nervous system disorders. Its efficacy in activating the 5-HT2A receptor makes it a valuable tool for researchers investigating therapeutic strategies for various neuropsychiatric conditions. -
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. -
5-HT1A Receptor Agonist
NLX-266 is a selective 5-HT1A receptor agonist that exhibits biased signaling towards ERK1/2 pathways. This compound demonstrates significant potential in research related to neurodegenerative diseases, particularly Parkinson's disease. Its unique mechanism may facilitate the investigation of receptor-mediated pathways and their implications in disease progression. -
5-HT2A Agonist
5-HT2A Agonist 8 is a potent agonist of the 5-HT2A receptor, exhibiting an EC50 of 4 nM. This compound is relevant for studies investigating neuropsychiatric disorders and neurodegenerative diseases, making it a valuable tool for research in these areas. Its ability to modulate serotonin signaling provides insight into the underlying mechanisms of neurological conditions. -
5-HT1B Antagonist
Isamoltane hemifumarate is a selective antagonist of the 5-HT1B receptor, exhibiting an IC50 value of 39 nM for the inhibition of [125I]ICYP binding to 5-HT1B recognition sites in rat brain membranes. Additionally, it functions as a β-adrenoceptor ligand with an IC50 of 8.4 nM. Due to its mechanism of action, Isamoltane hemifumarate demonstrates significant anxiolytic activity, making it a valuable tool for studies in anxiety disorders and related neuropharmacological research. -
5-HT4 Receptor Agonis
Relenopride is a potent partial agonist of the 5-HT4 receptor, with a weak binding affinity for the 5-HT2B receptors (Ki = 31 nM). This compound exhibits significant biological activity in modulating gastrointestinal motility and is primarily utilized in research related to neuropharmacology and gastrointestinal disorders. Its selective action on the 5-HT4 receptor makes it a valuable tool for studying serotonin receptor pathways and their implications in various physiological functions. -
5-HT(1A/B/D) Receptor Antagonist
GSK-588045 is a potent antagonist of the 5-HT(1A/B/D) receptors, demonstrating a high degree of selectivity for these targets while sparing human ether-a-go-go related gene (hERG) potassium channels. This specificity makes GSK-588045 a valuable tool in the study of neurological disorders, particularly in the context of depression and anxiety research applications. Its unique profile can aid in elucidating the role of serotonin receptors in various neuropsychiatric conditions. -
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.
