Catalog No.
Product Name
Application
Product Information
Citations
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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. -
5-HT1A antagonist
DU125530 is a potent and selective antagonist of the 5-HT1A receptor, demonstrating Ki values of 0.7 nM for 5-HT1A and significantly higher values for other serotonin receptors. This compound exhibits antidepressant properties, making it a valuable tool for research into mood disorders and serotonin signaling pathways. It is particularly relevant for studies aimed at understanding the role of 5-HT1A receptor modulation in behavioral and neurochemical responses. -
5-HT6 Antagonist
5-HT6 Inverse Agonist 1 is a selective antagonist of the 5-HT6 receptor, exhibiting a Ki of 23 nM and a Kb of 6.62 nM. This compound effectively inhibits the 5-HT6R-mediated signaling pathways, including Cdk5 and mTOR. Additionally, 5-HT6 Inverse Agonist 1 has demonstrated efficacy in reducing tactile hypersensitivity in a rat model of spinal nerve ligation, making it a valuable tool for research into pain management and neurobiology. -
5-HT Receptor Agonist
TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. It enhances serotonin (5-HT)-mediated signaling through the 5-HT3A receptor, making it a valuable tool for studying 5-HT3 receptor pharmacology. TMPPAA is applicable in research related to neurotransmission, pain pathways, and gastrointestinal functioning. -
5-HT Inhibitor
Femoxetine hydrochloride is a selective serotonin (5-HT) inhibitor known for its antidepressant properties. By inhibiting the reuptake of serotonin, it elevates serotonin levels within the synaptic cleft, thereby enhancing serotonergic signaling. This compound is valuable in research focusing on the role of serotonin in mood regulation and its implications in depression and related emotional disorders. -
5-HT2A Receptor Antagonist
Temanogrel hydrochloride is a selective antagonist of the 5-HT2A receptor, exhibiting a Ki value of 4.9 nM. This compound is primarily utilized in research related to serotonergic pathways and their implications in various neuropsychiatric disorders. Its use in pharmacological studies can provide insights into the modulation of serotonin receptors and their role in cardiovascular and central nervous system functions. -
5-HT2C Agonist
5-HT2C agonist-5 is a potent 5-HT2C receptor agonist with an EC50 of less than 1 nM. This compound demonstrates significant biological activity through modulating serotonin signaling pathways, making it a valuable tool for investigating neuropsychiatric and neurodegenerative disorders. Its application in research may provide insights into the therapeutic potential of targeting 5-HT2C receptors in various brain-related conditions. -
5-HT2C Receptor Agonist
PF-4479745 is a potent and selective agonist of the 5-HT2C receptor, demonstrating an EC50 of 10 nM and a Ki of 15 nM. This compound has significant biological activity relevant to cardiovascular research, particularly in the study of conditions such as hypertension. Its selectivity for the 5-HT2C receptor makes it an invaluable tool for elucidating the role of serotonin signaling in cardiovascular disease mechanisms. -
5-HT Receptor Inhibitor
Org 6582 is a competitive and selective inhibitor of the 5-HT receptor, demonstrating a Ki value of 89 nM. This compound exhibits a long-lasting inhibitory effect on serotonin uptake, persisting for over 48 hours. Org 6582 is primarily utilized in research focusing on depressive disorders, providing valuable insights into serotonergic modulation in various neuropsychological studies. -
Antidepressant Agent
Captodiame, a 5-HT2c receptor antagonist, exhibits significant antidepressant activity by modulating serotonin signaling. In addition, it acts as an agonist at sigma-1 and D3 dopamine receptors, enhancing its therapeutic potential. This compound is of interest for researchers focused on neuropharmacology and the development of novel antidepressant therapies. -
5-HT Receptor Antagonist
Alverine is a selective 5-HT1A receptor antagonist, exhibiting an IC50 value of 101 nM. This compound is primarily utilized in research focused on gastrointestinal disorders and the modulation of serotonin signaling pathways. Its antagonistic activity at the 5-HT1A receptor may provide insights into the mechanisms underlying dysregulation of serotonin-related pathologies. -
5-HT2A/dopamine D2 Antagonist
Abaperidone hydrochloride is a potent antagonist of the 5-HT2A receptor and dopamine D2 receptor, exhibiting IC50 values of 6.2 nM and 17 nM, respectively. This compound demonstrates significant affinity in modulating serotonergic and dopaminergic signaling pathways, making it a valuable tool for studying neuropharmacology and the treatment of psychiatric disorders. Research applications include investigations into schizophrenia, anxiety, and mood disorders. -
5-HT2A Agonist
5-HT2A agonist 3 is a highly selective agonist for the 5-hydroxytryptamine 2A receptor (5-HT2A), exhibiting an EC50 value of 13.80 nM. This compound is valuable for investigating various mental health disorders, including depression, post-traumatic stress disorder, and obsessive-compulsive disorder. Its specific action on the 5-HT2A receptor provides a crucial tool for studying central nervous system functions and the underlying mechanisms of these conditions. -
5-HT Receptor Antagonist
5-HT3 antagonist 2 is a selective antagonist of the 5-HT3 receptor, a subtype of the serotonin receptor. This compound exhibits significant biological activity by inhibiting the effects of serotonin, making it useful in research focused on neurotransmission, gastrointestinal function, and the treatment of nausea and anxiety disorders. Its application in pharmacological studies supports the development of therapeutic strategies targeting the 5-HT3 receptor pathway. -
5-HT Receptor Antagonist
Zatosetron maleate is a potent and selective antagonist of the 5-HT3 receptor. This compound exhibits strong inhibitory effects on serotonin signaling, making it valuable in exploring gastrointestinal functions and managing nausea and vomiting. Its utility extends to various research applications, including studying neuropharmacology and the role of serotonin in mood regulation. -
5-HT Receptor Antagonist
Alosetron-d3 hydrochloride is a deuterium-labeled derivative of Alosetron, functioning as a selective antagonist of the serotonin 5-HT3 receptor. This compound exhibits significant potency in modulating gastrointestinal activity and is primarily utilized in research focused on understanding and treating disorders related to serotonin signaling, such as irritable bowel syndrome. Alosetron-d3 hydrochloride serves as a valuable tool for investigating the role of 5-HT receptors in various biological processes. -
Adrenergic Receptor Antagonist
(4E)-SUN9221 is a potent antagonist of the α1-adrenergic receptor and the 5-HT2 receptor, demonstrating significant biological activity in modulating cardiovascular responses. This compound exhibits antihypertensive effects and inhibits platelet aggregation, making it a valuable tool for research in hypertension and thrombosis. Its ability to selectively target these receptors provides insights into adrenergic signaling and related pathological conditions. -
5-HT Receptor Inhibitor
5-HT3-In-1 is a selective inhibitor of the 5-HT3 receptor, effectively blocking serotonin's action at this target. This compound demonstrates notable efficacy in inhibiting 5-HT3-mediated signaling pathways, making it valuable for research focused on neuropharmacology and gastrointestinal function. Its use extends to studying various conditions, including anxiety, depression, and nausea-related disorders. -
5-HTIDβ Receptor Agonist
5-(Nonyloxy)tryptamine oxalate is a selective agonist for the 5-HTIDβ receptor, demonstrating a high affinity with an ED50 value of 68 nM. This compound exhibits significant antitumor activity in vivo and has been shown to enhance the efficacy of T cell-mediated targeting of tumor cells. Its applications in cancer research and immunotherapy make it a valuable tool for studying receptor signaling and cellular responses in tumor microenvironments. -
D3 Receptor Antagonist
RGH-1756 is a selective antagonist of the human D3 dopamine receptor, exhibiting pronounced effects in modulating dopaminergic pathways. This compound demonstrates lesser antagonistic activity on the human D2L and 5HT1A receptors. RGH-1756 is primarily utilized in research focusing on neuropharmacology and the mechanism of antipsychotic treatments, particularly in understanding conditions related to dopamine dysregulation. -
5-HT Receptor Agonist
Donitriptan mesylate is a potent agonist of the 5-HT1B and 5-HT1D receptors, demonstrating high efficacy with pKis of 9.4 and 9.3, respectively. This compound is primarily utilized in research focused on migraine treatments and neurological disorders, enabling studies on serotonin receptor signaling pathways. Its strong affinity for 5-HT receptors makes it a valuable tool for exploring the role of serotonin in various biological processes. -
5-HT/DA Receptor Antagonist
Ziprasidone mesylate is a potent antagonist of the 5-HT and dopamine receptors, specifically targeting the Rat D2 receptor (Ki=4.8 nM), the 5-HT2A receptor (Ki=0.42 nM), and the 5-HT1A receptor (Ki=3.4 nM). This compound demonstrates significant activity in modulating serotonergic and dopaminergic pathways, making it valuable for research in psychiatric disorders, such as schizophrenia and mood disorders. Its unique pharmacological profile allows for a better understanding of the interplay between these neurotransmitter systems in various biological contexts. -
5-HT Receptor Agonist
RS 67333 is a selective agonist of the 5-HT4 receptor, known for its stress-preventive properties. This compound has been shown to mitigate stress-induced changes in body weight and to alleviate depression- and anxiety-like behaviors across various mouse models. Its potential applications include studies on stress response, mood disorders, and the neurobiological mechanisms underlying anxiety and depression. -
5-HT6 Receptor Antagonist
Ro 04-6790 di(hydrochloride) is a potent and selective antagonist of the 5-HT6 receptor, exhibiting pKi values of 7.26 and 7.35 for rat and human 5-HT6 receptors, respectively. This compound demonstrates a high degree of specificity, showing no significant affinity for other receptors. Ro 04-6790 di(hydrochloride) is primarily utilized in neurological research to elucidate the role of 5-HT6 receptor modulation in various physiological and pathological processes.
