Catalog No.
Product Name
Application
Product Information
Citations
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D2 Receptor/5HT2A Receptor Antagonist
5-HT2A Antagonist 4 Methanesulfonate is a selective antagonist of both dopamine D2 receptors and serotonin 5HT2A receptors. This compound is primarily utilized in research concerning central nervous system disorders, facilitating the exploration of neuropharmacology and the modulation of neurotransmitter activity. Its dual receptor targeting makes it a valuable tool for studying the pathophysiology and treatment strategies for various neuropsychiatric conditions. -
5-HT Receptor Agonist
N-Desmethyl Zolmitriptan is an active metabolite that selectively targets the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D. It acts as an agonist of the 5-HT1B receptor, facilitating vasoconstriction in isolated human cerebral arteries, with an EC50 of approximately 100 nM. This compound is valuable for research into migraine mechanisms and the exploration of serotonin signaling pathways. -
5-HT Receptor Inhibitor
5-IAI hydrochloride is a selective 5-HT receptor inhibitor that modulates serotonin signaling. This compound has been shown to significantly reduce serotonin uptake sites and decrease hippocampal serotonin levels in rat models. It serves as an important tool for research into serotonin-related pathways and their implications in neuropharmacology. -
5-HT1A Receptor Agonist
Xaliproden free base is a selective agonist of the 5-HT1A receptor, exhibiting oral bioactivity. This compound demonstrates significant analgesic effects in models of acute tonic nociceptive pain and possesses neuroprotective properties. Additionally, Xaliproden free base effectively mitigates paclitaxel-induced mechanical allodynia by reducing the hyperactive responses of primary afferent neurons, making it valuable in pain and neuroprotection research. -
5HT Receptor Antagonist
ICI 169369 free base is a selective and non-competitive antagonist of the 5-HT receptor. This compound effectively diminishes vasopressin responses to insulin-induced hypoglycemia without affecting ACTH, prolactin, or growth hormone release. ICI 169369 also modulates centrally mediated 5-HT activity and has been shown to reduce portal pressure in portal hypertensive models, making it a valuable tool for research in neuroendocrine regulation and vascular physiology. -
5-HT3 Antagonist
Zacopride is a potent orally active antagonist of the 5-HT3 receptor, with a Ki value of 0.38 nM, and an agonist of the 5-HT4 receptor, exhibiting a Ki of 373 nM. This compound demonstrates significant biological activities, including the regulation of gastrointestinal motility, modulation of cardiac function, and the provision of anxiolytic and antiemetic effects. Zacopride is primarily utilized in research focusing on gastrointestinal disorders, cardiovascular conditions, and psychiatric diseases such as anxiety. -
5-HT Receptor Agonist
25E-NBOMe hydrochloride is a potent agonist of the 5-HT2A receptor, derived from 2C-E with an N-(2-methoxybenzyl) modification at the amine. It exhibits significant binding affinity for the 5-HT receptor family, making it useful in neuropharmacological research. This compound serves as a valuable tool for studying receptor mechanism and the physiological impacts of serotonergic signaling. -
5-HT2 Receptor Antagonist
LY53857 is a potent antagonist of the 5-HT2 receptor, effectively inhibiting vasoconstriction mediated by serotonin. In preclinical studies, LY53857 demonstrated the ability to block the depressor response to serotonin without significantly affecting mean arterial blood pressure in spontaneously hypertensive rats. Furthermore, LY53857 enhances neurotransmitter release in rat vas deferens and guinea pig ileal nerves, indicating its potential utility in elucidating serotonergic signaling pathways and exploring therapeutic applications in related cardiovascular and neural disorders. -
5-HT1A Receptor Agonist
Binospirone is a selective agonist of the 5-HT1A receptor. It exhibits significant anxiolytic activity, making it useful in the exploration of anxiety-related conditions. Additionally, Binospirone serves as a valuable tool in research investigating movement disorders, providing insights into the underlying mechanisms of these conditions. -
5-HT Receptor Inhibitor
PF-05212377 is a selective inhibitor of the serotonin receptor 5-HT6. This compound serves as a substrate for the P-glycoprotein non-BCRP human transporter and demonstrates blood-brain barrier permeability in non-human primates. PF-05212377 holds potential for research applications related to Alzheimer's Disease, enabling exploration of its role in neurodegenerative mechanisms and therapeutic strategies. -
5-HT Receptor Agonist
Pumosetrag is a selective 5-HT receptor agonist that modulates serotonin activity in the central nervous system. This compound exhibits notable biological activity in neuropharmacological research, serving as a valuable tool in studies related to mood disorders, anxiety, and other serotonin-related conditions. Pumosetrag's mechanism of action provides insights into receptor function and potential therapeutic pathways in serotonergic signaling. -
5-HT2 Receptor Antagonist
Tiospirone is a potent 5-HT2 receptor antagonist, demonstrating additional affinity for D2, 5-HT1A, 5-HT7, and sigma receptors. This compound has been shown to decrease ethanol consumption while enhancing food intake in rat models. Additionally, Tiospirone can diminish the reinforcing effects of cocaine, as evidenced in the conditioned place preference paradigm, making it a valuable tool for research into addiction and feeding behavior. -
5-HT1a Receptor Ligand
MDL 72832 (hydrochloride) is a selective ligand for the 5-HT1a receptor, a crucial target in neuropharmacology. This compound exhibits high affinity for the receptor, making it a valuable tool for studying serotonergic signaling pathways. It is primarily utilized in research applications related to anxiety, depression, and other neuropsychiatric disorders. -
Stable Isotope
Melperone-d4 hydrochloride is a deuterium-labeled derivative of Melperone hydrochloride, a butyrophenone with atypical antipsychotic properties. It acts as a multireceptor antagonist, exhibiting binding affinities (Kd values) of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Additionally, Melperone-d4 displays weak interactions with several other receptors and inhibits CYP2D6. This reagent is particularly valuable for investigating schizophrenia and managing agitation in geriatric populations. -
D2/5-HT2 Antagonist
Iloperidone hydrochloride is a dual D2 and 5-HT2 receptor antagonist. It is classified as an atypical antipsychotic and is primarily utilized in the treatment of schizophrenia symptoms. This compound is valuable for research focused on neuropharmacology and the elucidation of antipsychotic mechanisms. -
5-HT2 Receptor Antagonist
W-2451 is a selective antagonist of the serotonin 5-HT2 receptor. It exhibits potential neuroprotective effects, making it a valuable tool for investigating neurological disorders and their underlying mechanisms. This compound may aid in the elucidation of serotonin-related pathways in various neurological contexts. -
5-HT Receptor Agonist
2,6-DMA hydrochloride is a selective agonist for the serotonin 5-HT2 receptor, demonstrating an apparent pA2 value of 5.09. This compound plays a significant role in neurotransmission and has applications in studying serotonergic signaling pathways. It is useful in research investigating mood disorders, anxiety, and various neuropsychiatric conditions. -
5-HT2C Agonist
WAY 629 is a potent and selective agonist of the 5-HT2C receptor, demonstrating an EC50 of 426 nM for 5-HT2C and a significantly higher EC50 of 260,000 nM for 5-HT2A. This compound has been shown to effectively reduce feeding behavior, making it a valuable tool for studies related to appetite regulation and metabolic research. Its specificity and efficacy underscore its potential for use in pharmacological investigations involving serotonergic modulation. -
5-HT3 Receptor Antagonist
Lurosetron is a potent 5-HT3 receptor antagonist, specifically developed as a 6-fluoro analogue of Alosetron. This compound demonstrates significant biological activity through the inhibition of recombinant cytochrome P450 isoforms, including rbtCYP1A2 with an IC50 of 0.1 μM, as well as rbtCYP2C9 and rbtCYP3A4, exhibiting IC50 values ranging from 3.5 μM to 16 μM. Lurosetron is primarily utilized in research focused on gastrointestinal disorders and the modulation of serotonin pathways. -
5-HT6 Receptor Agonist
WAY 208466 is a selective agonist of the 5-HT6 receptor, exhibiting an EC50 of 7.3 nM. This compound promotes the elevation of GABA levels in the dorsolateral frontal cortex following both acute and chronic administration in rat models. WAY 208466 is primarily utilized in research related to anxiety disorders, particularly obsessive-compulsive disorder (OCD). -
5-HT1AR Regulator
Cannabidiolic acid methyl ester is a potent regulator of the 5-HT1A receptor. This orally active analogue enhances receptor activation and promotes the expression of c-Fos and NeuN in certain hypothalamic nuclei in rat models. Its biological activity suggests potential applications in anti-nausea, anti-anxiety, and tissue injury studies. -
5-HT4 Receptor Agonist
ML 10302 hydrochloride is a highly selective agonist for the 5-HT4 receptor, exhibiting an EC50 of 4 nM. This compound demonstrates over 680-fold selectivity for the 5-HT4 receptor compared to the 5-HT3 receptor in binding assays. ML 10302 hydrochloride is useful for research applications related to gastrointestinal motility disorders and central nervous system function, providing insights into the therapeutic potential for conditions influenced by serotonergic signaling. -
5-HT6 Receptor Antagonist
NPS ALX Compound 4a dihydrochloride is a highly potent and selective antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor, demonstrating an IC50 of 7.2 nM and a Ki of 0.2 nM. This compound is valuable for research applications targeting neuropsychiatric disorders, where modulation of 5-HT6 receptor activity may be of therapeutic interest. Its specificity and potency make it an essential tool for elucidating the role of the 5-HT6 receptor in various biological processes. -
5-HT Receptor Agonist
LEK 8804 is a selective 5-HT1A receptor agonist and 5-HT2 receptor antagonist. This compound demonstrates the ability to modulate receptor-mediated behavioral responses, as evidenced by its induction of a dose-dependent spontaneous tail-flick response in rats, showcasing robust 5-HT1A agonist activity. Additionally, LEK 8804 effectively inhibits 5-HTP-induced head twitch responses in mice, likely through its antagonistic effect on 5-HT2 receptors. This compound is useful for exploring serotonergic mechanisms in behavioral studies and neuropharmacology research. -
5-HT Receptor Agonist
5-HT2A Agonist 6 is a potent agonist of the 5-HT2A receptor, exhibiting an EC50 of 1.7 nM. This compound is utilized in research focused on stress-related disorders, including depression, anxiety, and post-traumatic stress disorder. Its specific action on the 5-HT2A receptor makes it a valuable tool for investigating the underlying mechanisms of these conditions and exploring potential therapeutic interventions. -
5-HT2 Agonist
5-HT2 Agonist-1 Free Base is a potent agonist of the 5-HT2A, 5-HT2B, and 5-HT2C serotonin receptors, exhibiting IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively. This compound is valuable for investigating various neuropsychiatric and neurological disorders, including depression, addiction (alcohol and drugs), inflammation, cluster headaches, PTSD, and seizure disorders. Its targeted activity makes it a useful tool for researchers exploring the roles of serotonergic pathways in central nervous system conditions. -
5-HT3 Receptor Antagonist
Ramosetron is a potent 5-HT3 receptor antagonist that plays a critical role in modulating gastrointestinal function. It enhances gastrointestinal motility and reduces symptoms such as dysphoria and food avoidance, making it a valuable tool in the study of irritable bowel syndrome with diarrhea. Research applications include exploring its effects on nausea, vomiting, and other gastrointestinal disorders. -
5-HT Receptor Antagonist
SB 207710 is a highly selective antagonist of the 5-HT4 receptor, primarily targeting serotonin-mediated signaling pathways. It effectively inhibits the positive inotropic effect of serotonin in human right atrial appendage preparations. This compound is valuable for research applications investigating the role of serotonergic modulation in cardiovascular physiology and related disorders. -
Antipsychotic agent
Rilapine is an atypical antipsychotic agent that primarily targets serotonin and dopamine receptors in the brain. It demonstrates significant efficacy in managing symptoms of schizophrenia and bipolar disorder. This compound is valuable for research into neuropsychiatric disorders and the development of novel therapeutic strategies in psychiatry. -
5-HT Receptor Inhibitor
DSP-6745 is a potent and orally active inhibitor of the 5-HT receptor. This compound exhibits significant biological activity in modulating serotonergic signaling, making it a valuable tool for research into depressive disorders. Its ability to selectively target 5-HT receptors enables the investigation of their role in mood regulation and related pathologies. -
5-HT1 Receptor Agonist
BMS-181885 is a selective agonist of the 5-HT1 receptor, specifically targeting the 5-HT1B and 5-HT1D subtypes. It demonstrates significant anti-migraine activity, making it a valuable tool for research into neurological disorders related to migraine. This compound can aid in elucidating the underlying mechanisms of migraine pathophysiology and exploring new therapeutic strategies. -
5-HT6R Antagonist
Diphenyl sulfone acts as a selective antagonist of the 5-HT6 receptor, demonstrated by its inhibitory constant (Ki) of 1.6 μM. This compound has been utilized in research focused on neurological disorders and cognitive functions, particularly in the context of serotonergic modulation. Its capability to influence serotonin pathways makes it a valuable tool for investigating potential therapeutic strategies. -
5-HT/NA reuptake Inhibitor
5-HT/NA Reuptake Inhibitor-1 is a selective dual inhibitor of serotonin (5-HT) and norepinephrine (NA) reuptake, exhibiting IC50 values of 660 nM and 70 nM, respectively. This compound demonstrates favorable in vitro metabolic stability in humans, along with high hERG selectivity and passive membrane permeability. It is primarily utilized in research focused on mood disorders and neuropharmacology, providing valuable insights into the modulation of neurotransmitter systems. -
5-HT2B/2C Receptor Antagonist
SB-200646 is a selective antagonist of the 5-HT2B and 5-HT2C receptors, exhibiting pKi values of 7.5, 6.9, and 5.2 against these targets and the 5-HT2A receptor, respectively. This compound demonstrates oral bioactivity and displays notable electrophysiological and anxiolytic effects in vivo. It serves as a valuable tool for research into serotonergic modulation and its implications in anxiety-related disorders. -
5-HT Receptor Antagonist
Elzasonan citrate is a selective antagonist of the 5-hydroxytryptamine 1B (5-HT1B) receptor. This compound has demonstrated potential in modulating serotonergic signaling, making it relevant for research in depression and related mood disorders. Its ability to inhibit the 5-HT1B receptor provides a valuable tool for investigating therapeutic approaches in the treatment of psychiatric conditions. -
Serotonin/Norepinephrine/Dopamine Reuptake Inhibitor
Bicifadine is a serotonin/norepinephrine/dopamine reuptake inhibitor that demonstrates oral bioavailability. It exhibits significant antinociceptive properties across various models of acute, persistent, and chronic pain. Bicifadine is primarily utilized in research related to pain mechanisms and therapeutic interventions for pain management. -
5-HT Receptor Antagonists
Trelanserin is a selective antagonist of the 5-HT receptors, exhibiting significant effects on smooth muscle contraction. This compound effectively inhibits contractions induced by sumatriptan, demonstrating a pA2 value of 8.17±0.36 in vitro. Trelanserin is utilized in pharmacological research to explore the modulation of serotonin pathways and their implications in various physiological and pathological processes. -
5-HT6R Antagonist
AVN-322 is a highly selective antagonist of the 5-HT6 receptor, targeting mechanisms within the central nervous system. This compound's oral bioactivity makes it a valuable tool for investigating neurological disorders and related biological pathways. AVN-322 can be utilized in research focused on cognition, memory, and other CNS-related functions. -
5-HT6R/5-HT3R Antagonist
PZ-1922 free base is a centrally-active antagonist of the 5-HT6 receptor and the 5-HT3 receptor, exhibiting binding affinities of Ki values of 17 nM and 0.45 nM, respectively. This compound also reversibly inhibits monoamine oxidase B, with a pIC50 of 8.93. PZ-1922 free base has demonstrated efficacy in reversing memory deficits induced by Scopolamine in novel object recognition tests in rats, as well as preventing beta-amyloid-induced cognitive decline in T-maze assessments. These properties make it a valuable tool for investigating neuropharmacology and disorders related to memory impairment. -
5-HT1B Antagonist/5-HT1D Agonist
Carpindolol is a selective antagonist of the 5-HT1B receptor and an agonist of the 5-HT1D receptor, demonstrating a pKd of 8.53 and pKB of 8.0 for its antagonistic activity, as well as a pEC50 of 5.91 for its agonistic effects. This compound has significant implications in neuropharmacology research, particularly in studies investigating serotonin receptor dynamics and related pathways. It serves as a valuable tool for exploring the modulation of neurotransmitter systems and their physiological roles. -
5-HT Receptor Agonist
Lesopitron hydrochloride is a potent 5-HT receptor agonist that exhibits significant anxiolytic-like properties. It effectively inhibits forskolin-stimulated adenylate cyclase activity, demonstrating an IC50 value of 125 nM. This compound is valuable for research applications investigating serotonin receptor signaling and its implications in anxiety disorders. -
5-HT1D Agonist
PNU109291 is a potent and selective agonist of the 5-HT1D receptor. This compound is known to effectively reduce dural plasma extravasation induced by trigeminal ganglion stimulation, making it a valuable tool for research in migraine and pain pathways. Its specificity for the 5-HT1D receptor positions it as a promising candidate for investigating therapeutic strategies in neurovascular conditions. -
5-HT Receptor Agonist
S(-)-8-OH-DPAT hydrobromide is a selective agonist of the 5-HT1A receptor, demonstrating a high affinity with a pIC50 value of 8.19. Its mechanism involves the activation of serotonin receptors, contributing to various neurological effects. This compound is primarily utilized in research focused on neuropharmacology and the modulation of serotonin-related pathways, making it a valuable tool for studying mood disorders and anxiety. -
5-HT6R/MAO-B Inhibitor
5-HT6R/MAO-B modulator 1 is a selective antagonist of the 5-HT6 receptor with Gs signaling activity and serves as an irreversible inhibitor of monoamine oxidase B (MAO-B). This compound demonstrates glioprotective effects and has the capability to reverse memory deficits induced by scopolamine. Additionally, it features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a versatile tool for chemical biology applications. -
5-HT2CR Agonist
(S)-5-HT2CR agonist 1 is a selective agonist for the 5-HT2C receptor, exhibiting an EC50 of 14 nM. This compound is valuable for investigating the role of 5-HT2CR in various physiological processes, particularly in studies related to hyperlocomotion. It serves as a key reagent for neuroscience research focused on serotonin signaling pathways. -
5-HT2C Agonist
WAY 629 hydrochloride is a potent and selective agonist of the 5-HT2C receptor. With an EC50 of 426 nM for 5-HT2C and a much higher EC50 of 260,000 nM for 5-HT2A, it exhibits a strong affinity for its target. This compound has been shown to decrease feeding behavior, making it a valuable tool in research related to appetite regulation and the potential treatment of obesity and related disorders. -
5-HT2A/5-HT2C Receptors Agonist
25N-NBOMe hydrochloride is a potent agonist of the 5-HT2A and 5-HT2C receptors, exhibiting Ki values of 0.144 nM and 1.06 nM, respectively. This compound is primarily utilized in neuroscience research to explore the modulation of serotonin receptors and their role in various neurological disorders. It demonstrates minimal efficacy in stimulating the release of preloaded neurotransmitters from dopamine, serotonin, and norepinephrine transporters, making it a selective tool for investigating serotonergic signaling pathways. -
5-HT6 Antagonist
SB-737050A is a potent antagonist of the 5-HT6 receptor, which plays a crucial role in modulating neurotransmitter release and cognitive functions. This compound has shown promise in research focused on addiction, particularly in preventing relapse. Its inhibitory effects on the 5-HT6 receptor may contribute to potential therapeutic strategies for addressing substance use disorders and related cognitive impairments. -
5-HT Receptor Agonist
25B-NBF hydrochloride is a potent agonist of the 5-HT2C receptor, demonstrating significant binding affinity to the human 5-HT2A receptor and the rat 5-HT2C receptor, with pKi values of 8.57 and 7.73, respectively. This compound facilitates key research into serotonin receptor modulation, making it useful for studies in neuropharmacology and behavioral neuroscience. Its strong activity at these targets aids in the exploration of therapeutic approaches for various psychiatric disorders. -
5-HT1A Agonist
RS-64459-193 is a selective partial agonist of the 5-HT1A receptor, exhibiting a Ki of 24.9 nM. It demonstrates substantial affinity for additional serotonin receptors, including 5-HT2C, 5-HT2A, and 5-HT7, with pKi values of 6.87, 7.02, and 7.18, respectively. RS-64459-193 is characterized by minimal activity at the 5-HT3 receptor, making it a useful tool for studies focused on serotonin signaling pathways and potential therapeutics for disorders related to serotonergic dysregulation.
