Catalog No.
Product Name
Application
Product Information
Citations
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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. -
5-HT1D Receptor Agonist
Lerimazoline is a selective agonist of the 5-HT1D receptor, exhibiting Ki values of 72 nM and 3480 nM for h5-HT1D and h5-HT1B receptors, respectively. This compound effectively inhibits Forskolin-induced cAMP production and stimulates contractions in rabbit saphenous vein preparations. Lerimazoline's pharmacological profile makes it a valuable tool for research into migraine pathophysiology and related therapeutic strategies. -
Stable Isotope
Palonosetron-d3 hydrochloride is a deuterium-labeled derivative of Palonosetron hydrochloride, functioning primarily as a 5-HT3 receptor antagonist. It is widely utilized in research to investigate mechanisms of chemotherapy-induced nausea and vomiting and is known for its ability to prevent both acute and delayed episodes. Additionally, Palonosetron hydrochloride demonstrates moderate activity against flavivirus and potent efficacy against Zika virus in mammalian cells, contributing to its relevance in virology studies. Its potential antidepressant properties also make it a compound of interest in neuropharmacology research. -
5-HT3 Receptor Antagonist
Dehydro Palonosetron hydrochloride is a potent 5-HT3 receptor antagonist. It is primarily utilized for its antiemetic properties, making it effective in the prevention and treatment of nausea and vomiting associated with chemotherapy and surgery. This compound is valuable for researchers investigating the modulation of serotonin receptors and their role in gastrointestinal function and antiemetic therapies. -
5-HT2 Receptor Antagonist
R-96544 free base is a potent and selective competitive antagonist of the 5-HT2 receptor. This compound effectively inhibits platelet aggregation induced by serotonin and blocks 5-HT2A receptor-mediated contractions in guinea pig trachea. R-96544 free base is valuable in research investigating serotonergic signaling and related physiological processes. -
5-HT1C/5-HT2 Agonist
MK-212 is a potent agonist of the 5-HT1C and 5-HT2 serotonin receptors. It is known to stimulate phosphoinositide hydrolysis in the cerebral cortex, making it valuable for research into neuropharmacology and the functional role of serotonergic pathways in the brain. This compound is often utilized in studies seeking to elucidate the mechanisms underlying mood regulation and other central nervous system functions. -
5-HT Receptor Agonist
Almotriptan hydrochloride is a selective agonist of the 5-HT 1B and 1D receptors, primarily targeting serotonin receptors involved in vascular regulation. This compound demonstrates significant efficacy in the treatment of migraine attacks by promoting vasoconstriction and inhibiting pro-inflammatory neuropeptide release. Almotriptan hydrochloride is utilized in various research applications focused on migraine mechanisms and the physiological role of serotonin in headache disorders. -
5-HT1A Receptor Agonist
LY 293284 is a highly selective agonist of the 5-HT1A receptor. It demonstrates notable biological activity by inducing a significant reduction in core temperature and increasing food intake in cholestatic rats following bile duct resection. This compound is valuable for research applications focused on the modulation of serotonergic pathways and studying the effects of 5-HT1A receptor activation in various physiological conditions. -
5-HT7 Receptor Ligand
5-HT7 receptor ligand 1 is a selective ligand targeting the 5-HT7 receptor, exhibiting a Ki value of 8 nM. This compound demonstrates significant biological activity and has potential applications in neuropharmacology research, particularly in exploring serotonin signaling pathways. Additionally, 5-HT7 receptor ligand 1 shows low hepatotoxicity and a moderate potential for interaction with agents metabolized by CYP3A4 or CYP2D6, making it suitable for various experimental conditions. -
5-HT6 Receptor Antagonist
5-HT6R antagonist 2 is a selective antagonist of the 5-HT6 receptor, a G protein-coupled receptor involved in central nervous system processes. This compound exhibits potential to modulate neurotransmission and is utilized in research on neurological and psychiatric disorders, including depression and cognitive dysfunction. Its role in investigating the therapeutic effects of serotonin modulation makes it a valuable tool for exploring novel treatment strategies. -
5-HT Receptor
LP-20 hydrochloride functions as a ligand for the 5-HT7 receptor, a subtype of the serotonin receptor family. This compound selectively modulates serotonin signaling pathways and has implications in the study of neuropsychiatric disorders and circadian rhythms. LP-20 hydrochloride can be utilized in research exploring the therapeutic potential of 5-HT7 receptor antagonism or agonism, contributing to a deeper understanding of serotonin-related mechanisms. -
5-HT1B Receptor Antagonist
AZD1134 is a highly selective antagonist of the 5-HT1B receptor, demonstrating oral bioavailability and significant brain penetration. With IC50 values of 2.9 nM in humans and 0.108 nM in guinea pigs, AZD1134 effectively increases synaptic serotonin levels, indicating its potential in modulating serotonergic activity. This compound is particularly relevant for research into psychiatric disorders, including depression and anxiety. -
5-HT2A Receptor Antagonist
Iferanserin hydrochloride is a selective 5-HT2A receptor antagonist. It exhibits significant potential in alleviating symptoms associated with internal hemorrhoids, including bleeding and pruritus, as evidenced by ongoing Phase IIb clinical trials. This compound is valuable for research applications focusing on serotonin modulation and gastrointestinal disorders. -
5-HT7/5-HT2A Receptor Antagonist
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity ligand targeting both the 5-HT7 and 5-HT2A receptors, demonstrating oral bioavailability and significant brain permeability with a pKi of 8.1. This compound functions as an antagonist in in vitro assays for the 5-HT2A receptor and as an inverse agonist for the 5-HT7 receptor. In vivo studies have shown that it effectively blocks 5-Carboxamidotryptamine (5-CT)-induced hypothermia in rats and DOI-induced head-twitches in mice, while it also occupies 5-HT2A receptor binding sites in the frontal cortex. 5-HT7/5-HT2A receptor antagonist 1 is suitable for investigating neuropharmacological disorders. -
5-HT Agonist
5-MeO-MET (5-Methoxy-N-methyl-N-ethyltryptamine) functions primarily as a 5-HT1A and 5-HT2A receptor agonist. This compound exhibits significant psychoactive properties, demonstrating sedative effects and inhibition of locomotor activity in murine models. Due to its influence on serotonergic pathways, 5-MeO-MET is valuable for research into the role of serotonin in behavior and potential therapeutic applications in studying mood disorders. -
5-HT7 Receptor Antagonist
SB 258719 hydrochloride is a selective antagonist of the 5-HT7 receptor, exhibiting high affinity with a pKi of 7.5. This compound is instrumental in the exploration of various biological pathways, particularly in cancer research and the study of neurological disorders. Its unique mechanism of action makes it a valuable tool for investigating the therapeutic potential of 5-HT7 receptor modulation in relevant disease models. -
5-HT3 Receptor Antagonist
Dehydro Palonosetron is a potent and selective 5-HT3 receptor antagonist known for its oral activity. It effectively inhibits the 5-HT3 receptor without influencing the functions of 5-HT1, 5-HT2, or 5-HT4 receptors. This compound is widely utilized in research applications focusing on the management of nausea and vomiting, particularly in chemotherapy settings. Its specific targeting makes it a valuable tool for studies exploring serotonergic modulation in various physiological and pathological contexts. -
5-HT Receptor Agonist
(rac)-AL-37350A is a potent agonist of the 5-HT2 receptor, known for its ability to lower intraocular pressure. With a high affinity and selectivity for this receptor, (rac)-AL-37350A demonstrates significant efficacy in reducing intraocular pressure in conscious hypertensive cynomolgus monkeys. This compound is valuable for research applications exploring glaucoma treatments and the physiological mechanisms of 5-HT receptor activation. -
β-adrenoceptor Blocker
Tiprenolol is a selective β-adrenoceptor blocker that primarily targets β-adrenergic receptors. It has demonstrated efficacy in abolishing adrenaline-induced ventricular arrhythmias in canine models exposed to halothane anesthesia. This compound is valuable in pharmacological research related to cardiac function and the study of arrhythmias. -
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. -
Rat 5-HT1B Antagonist
NAS-181 free base is a potent and selective antagonist of the rat 5-HT1B receptor, exhibiting a Ki value of 47 nM. This compound demonstrates a 13-fold selectivity for the rat 5-HT1B over the bovine 5-HT1B receptor, which has a Ki of 630 nM. NAS-181 free base effectively enhances serotonin turnover and increases synaptic serotonin levels by inhibiting the terminal rat 5-HT1B autoreceptors, making it a valuable tool for research in neuropharmacology and serotonergic signaling. -
5-HT2A Agonist
5-HT2A agonist 9 is a potent agonist of the 5-HT2A receptor, exhibiting an EC₅₀ of 34 nM. This compound plays a crucial role in research focusing on mental disorders and central nervous system pathologies. Its ability to selectively activate the 5-HT2A receptor makes it a valuable tool for investigating the mechanisms underlying neuropsychiatric conditions. -
5-HT Receptor Agonist
CGS-12066 maleate is a selective agonist for the 5-HT receptor family, specifically targeting 5-HT1A, 5-HT1B, 5-HT1C, and 5-HT1D receptors with pEC50 values of 6.41, 7.56, 4.05, and 7.11, respectively. This compound exhibits significant biological activity in modulating serotonergic signaling and has been utilized in research focused on neurological disorders. CGS-12066 maleate provides valuable insights into the pharmacological role of serotonin receptors in various neurophysiological processes. -
5-HT4 Receptor Agonist
RS 67506 hydrochloride is a selective agonist of the 5-HT4 receptor, which is involved in neurotransmitter signaling in the central nervous system. With a pKi value of 8.8 for the 5-HT4 receptor in guinea pig striatum, this compound demonstrates significant binding affinity. RS 67506 hydrochloride is primarily used in neurobiology research to explore the role of 5-HT4 receptors in modulation of neuronal function and potential therapeutic applications in neuropsychiatric disorders. -
5-HT2BR Antagonist
MW073 is a potent and selective antagonist of the 5-HT2B receptor, exhibiting an IC50 of 70 nM. This compound inhibits receptor activity and β-arrestin-1 recruitment in a concentration-dependent manner. MW073 has demonstrated the ability to improve synaptic plasticity and alleviate behavioral deficits, including aggression, in mouse models of Alzheimer’s disease. It is suitable for research applications focused on Alzheimer’s disease and related neurological conditions. -
5-HT1A Antagonist
GSK-958108 is a highly selective antagonist of the 5-HT1A receptor. This compound exhibits significant biological activity in modulating serotonin pathways, making it valuable for research into various neurological conditions and disorders. Its specificity allows for detailed investigations into the role of 5-HT1A receptors in neuropharmacology and behavioral studies. -
5-HT4 Agonist
Y-36912 is a highly selective agonist of the 5-HT4 receptor, with a binding affinity of Ki = 1.5 nM. This compound is known to accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 is a valuable tool for research applications related to gastrointestinal disorders. -
5-HT2C Agonist
5-HT2C agonist-10 is a potent 5-HT2C receptor agonist with an EC50 of less than 10 nM. This compound is utilized in the investigation of psychiatric disorders, contributing to the understanding of serotonergic signaling and its implications in mental health research. Its strong efficacy makes it valuable for studies aimed at developing new therapeutic strategies targeting the 5-HT2C receptor.
