Catalog No.
Product Name
Application
Product Information
Citations
-
α/β Adrenergic Receptor Blocker
Primidolol is an orally active α/β Adrenergic Receptor blocker that exhibits antihypertensive properties. This compound demonstrates significant antibacterial and antioxidant activities, making it relevant in studies focused on both cardiovascular diseases and infectious processes. Its dual mechanism of action positions Primidolol as a valuable tool for research aimed at understanding the interplay between adrenergic signaling and microbial resistance. -
β2-Drenergic Receptor Agonist
Terbutaline is an orally active β2-adrenergic receptor agonist that effectively stimulates the β2-adrenergic receptors. Its primary biological activity includes bronchodilation, making it relevant for research on asthma symptoms and respiratory disorders. Terbutaline is commonly used in studies investigating the therapeutic effects of β2-agonists in pulmonary conditions. -
β2-Drenergic Receptor Agonist
Terbutaline sulfate is an orally active β2-adrenergic receptor agonist, primarily utilized in the treatment of asthma and other bronchospastic conditions. As an active metabolite of bambuterol, it promotes bronchodilation by relaxing smooth muscle in the airways. This compound is essential for research applications focused on respiratory pharmacology and the therapeutic evaluation of β2-adrenergic systems in asthma symptom management. -
Antibiotic
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic primarily targeting bacterial growth inhibition. It exhibits significant antibacterial activity, particularly against methicillin-resistant Staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 5 μg/mL. In addition to its antibacterial properties, Kendomycin acts as a potent antagonist of the endothelin receptor and a calcitonin receptor agonist, highlighting its potential applications in anti-osteoporotic research. -
Endothelin Receptor Antagonist
Sulfisoxazole diethanolamine is an endothelin receptor antagonist, exhibiting IC50 values of 0.60 μM and 22 μM for endothelin receptor A and endothelin receptor B, respectively. This sulfonamide antibacterial compound, characterized by its oxazole substituent, demonstrates significant inhibition of breast cancer exosome release through the selective targeting of endothelin receptor A. Its mechanism of action holds potential for applications in cancer research and related therapeutic studies. -
5-HT2A Regulator
2-Bromo-LSD D-Tartrate is a selective 5-HT2A receptor partial agonist and competitive antagonist. It exhibits significant biological activity, displaying an EC50 of 0.81 nM for Gq dissociation and a KB of 0.18 nM, making it a valuable tool for studying serotonergic signaling pathways. Additionally, it promotes dendritogenesis and spinogenesis while effectively reversing the behavioral impacts of chronic stress in animal models, enhancing active coping behaviors. This compound is suitable for research involving neurological and behavioral studies related to serotonin modulation. -
5-HT2A/5-HT2C Receptor Agonist
DOI hydrochloride is a potent agonist of the serotonin 5-HT2A and 5-HT2C receptors, exhibiting Ki values of 0.7 nM and 2.4 nM, respectively, while also targeting the 5-HT2B receptor with a Ki of 20 nM. This compound effectively crosses the blood-brain barrier, making it valuable for neurological research. DOI hydrochloride has been shown to induce head twitches in murine models, providing insight into its psychotropic effects and facilitating the study of serotonergic signaling pathways. -
5-HT2B Agonist
BW-723C86 is a selective agonist of the 5-HT2B receptor, demonstrating significant anxiolytic-like effects. In animal models, it has been shown to induce hyperphagia and decrease grooming behavior in rats. Additionally, BW-723C86 exhibits the ability to dilate pulmonary arteries and inhibit gastric accommodation following liquid meal intake, making it a useful reagent for research into anxiety, appetite regulation, and gastrointestinal physiology. -
5-HT4 Receptor Antagonist
GR 113808 is a potent and highly selective antagonist of the 5-HT4 receptor, exhibiting a pKb of 8.8. It demonstrates substantial selectivity, being 300-fold more effective against the 5-HT4 receptor compared to 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors. This compound is widely utilized in research applications focusing on gastrointestinal motility and cognitive function related to serotonin signaling pathways. -
5-HT2B Antagonist
SB 204741 is a selective high-affinity antagonist of the 5-HT2B receptor, exhibiting a pKi value of 7.1. This compound is utilized in research exploring the role of 5-HT2B in various physiological and pathological processes. Its antagonistic properties make it valuable for studies on cardiac function, pulmonary effects, and potential therapeutic interventions in diseases related to serotonergic dysregulation. -
5-HT Biosynthesis Inhibitor
4-Chloro-L-phenylalanine is a potent inhibitor of serotonin (5-HT) biosynthesis, acting as a nonspecific antagonist of the tryptophan hydroxylase isoforms TPH1 and TPH2. This compound is valuable for studying serotonin-related pathways and their implications in psychiatric and neurological disorders. It serves as an important tool for researchers investigating the regulation of serotonin levels and the biochemical basis of 5-HT modulation. -
Dopamine Receptor Antagonist
Spiperone is a potent antagonist of dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A receptors. With its capability to enhance intracellular calcium levels and inhibit the Wnt signaling pathway, Spiperone serves as a valuable tool in the study of neurological disorders. Its role as a labeled ligand for neuroleptic receptors further underscores its utility in receptor binding studies and neurotransmitter research. This compound is particularly relevant for investigating the mechanisms underlying various neuropsychiatric conditions. -
5-HT2C Receptor Agonist
Bexicaserin is a selective agonist of the 5-HT2C receptor, primarily involved in the regulation of appetite and mood. This compound demonstrates potential therapeutic applications in the study of obesity and psychiatric disorders, such as epilepsy. Its unique mechanism of action makes it a valuable tool for researchers investigating the role of serotonin receptors in these conditions. -
5-HT Receptor Agonist
8-OH-DPAT hydrobromide is a potent and selective 5-HT1A receptor agonist with a high pIC50 of 8.19. This compound demonstrates exceptional selectivity, being nearly 1000 times more selective for the 5-HT1A subtype compared to other serotonin receptor subtypes. It is primarily utilized in neuropharmacological research to investigate serotonin-mediated signaling pathways and to explore its effects on various neurological conditions. -
5-HT1A Agonist
Gepirone is a selective 5-HT1A agonist that binds specifically to the 5-HT1A receptor binding site. Its primary biological activity includes acting as an antidepressant, making it a valuable tool in research related to anxiety and major depressive disorders. Gepirone can be utilized to explore the underlying mechanisms of these conditions and aid in the development of new therapeutic strategies. -
5-HT2A Receptor Antagonist
Lumateperone is a potent 5-HT2A receptor antagonist with a Ki of 0.54 nM, exhibiting dual action as a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM). Additionally, it modulates dopamine D1 receptors. This compound demonstrates significant antipsychotic properties and supports research in schizophrenia and bipolar depression, while also presenting potential anticancer activity. -
5-HT Receptor Agonist
2-Methyl-5-HT is a selective agonist for the 5-HT3 receptor. This compound exhibits significant biological activity, particularly in demonstrating anti-depressive-like effects in preclinical models. It is utilized in research to explore serotonergic pathways and contribute to studies on mood regulation and anxiety disorders. -
5-HT Receptor Agonist
Bretisilocin is a selective agonist for the 5-HT2A receptor and functions as a serotonin releaser. This compound demonstrates significant antidepressant activity, making it an important tool for the investigation of depression and related neuropsychiatric disorders. Its role in modulating serotonin pathways provides valuable insights into the underlying mechanisms of mood regulation and potential therapeutic approaches. -
Dopamine D1/D5 Receptor Antagonist
SKF-83566 is a selective antagonist of the D1-like dopamine receptors, specifically targeting the dopamine D1 and D5 receptors. This compound exhibits potent inhibition of the dopamine transporter (DAT) with an IC50 of 5.7 μM, and shows competitive antagonism at the vascular 5-HT2 receptor. In addition, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it relevant for research into neurological disorders such as Parkinson's disease and studies focused on alleviating nicotine cravings. -
5-HT3 Receptor Agonist
SR 57227A is a potent, orally active selective agonist of the 5-HT3 receptor, capable of crossing the blood-brain barrier. This compound exhibits binding affinities (IC50) ranging from 2.8 to 250 nM for 5-HT3 receptor sites in rat cortical membranes and NG 108-15 cell membranes. SR 57227A is primarily utilized in research focused on neuropharmacology and has demonstrated potential anti-depressant effects. -
5-HT Uptake Inhibitor
Norfluoxetine hydrochloride is a potent 5-HT uptake inhibitor, serving as an active N-demethylated metabolite of Fluoxetine. It inhibits serotonin reuptake and has been shown to inhibit CaV3.3 T current with an IC50 of 5 μM. Due to its mechanism of action, Norfluoxetine hydrochloride is relevant in research focusing on mood disorders and anticonvulsant activity, providing insights into serotonin modulation and potential therapeutic applications. -
5-HT4 Receptor Agonist
RS 67333 hydrochloride is a selective partial agonist of the 5-HT4 receptor, demonstrating a pKi of 8.7 in guinea pig striatum. This compound exhibits lower affinities for various other receptors, including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2, and muscarinic M1-M3 receptors. RS 67333 hydrochloride is known for its neuroprotective properties, making it a valuable tool for research in Alzheimer's disease and related neurodegenerative disorders. -
5-HT Receptor Agonist
CP94253 hydrochloride is a selective agonist of the 5-HT1B receptor, demonstrating a Ki value of 2 nM in radioligand binding assays. It exhibits lower affinity for other serotonin receptor subtypes, with Ki values of 89 nM for 5-HT1A, 49 nM for 5-HT1D, 860 nM for 5-HT1C, and 1600 nM for 5-HT2. This compound is known for its central activity when administered systemically in vivo, making it valuable for research in neuropharmacology and the study of serotonin-related pathways. -
5-HT3 Agonist
m-CPBG hydrochloride is a selective agonist of the 5-HT3 receptor, influencing serotonin signaling pathways. It has demonstrated potential in research related to neurological diseases, allowing for the investigation of serotonin's role in various neurophysiological processes. This compound is valuable for studies aiming to elucidate the mechanisms underlying anxiety, depression, and other psychiatric conditions. -
D2R Agonist
UNC9994 hydrochloride is a functionally selective agonist of the dopamine D2 receptor (D2R), exhibiting β-arrestin–biased signaling and selectively activating β-arrestin recruitment. With a binding affinity of Ki 79 nM for D2R, it functions as an antagonist of Gi-mediated cAMP production and a partial agonist for D2R/β-arrestin-2 interactions. This compound demonstrates antipsychotic-like effects, making it a valuable tool for research in neuropharmacology and the study of dopamine receptor signaling pathways. -
5-HT Receptor Agonist
TCB2 is a potent agonist of the serotonin 5-HT2A receptor. It demonstrates significant activation of this receptor, crucial for mediating various psychological and physiological responses. TCB2 is utilized in research exploring the role of 5-HT2A activation in neuropsychiatric disorders and receptor signaling pathways. -
5-HT7 Receptor Antagonist
SB 258719 is a selective antagonist of the 5-HT7 receptor, exhibiting a high affinity with a pKi value of 7.5. This compound demonstrates significant potential in the research of various neurological disorders and cancer. Its targeted mechanism allows for the exploration of 5-HT7 receptor signaling pathways, contributing to a deeper understanding of their role in these diseases. -
5-HT2C Receptor Agonist
(Rac)-WAY-161503 is a selective agonist of the 5-HT2C receptor, exhibiting a Ki of 4 nM and an EC50 of 12 nM. This compound demonstrates significantly higher affinity for the 5-HT2C receptor compared to the 5-HT2A and 5-HT2B receptors. Due to its biological activity, (Rac)-WAY-161503 is valuable for research applications aimed at understanding obesity and depressive disorders. -
5-HT2C Receptor Antagonist
RS-102221 hydrochloride is a selective antagonist of the 5-HT2C receptor, exhibiting a Ki value of 10 nM. This compound demonstrates approximately 100-fold selectivity over the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride has been shown to stimulate the differentiation of new nerve cells and is associated with increased food intake and weight gain in rodent models, making it a useful tool for research in neurobiology and appetite regulation. -
5HT4 Agonist
Mosapride is a selective 5HT4 agonist known for its gastroenterokinetic properties. This compound enhances gastrointestinal motility and is used in research related to gastrointestinal diseases. Additionally, Mosapride acts as a CYP inducer and exhibits a concentration-dependent inhibitory effect on Kv4.3 with an IC50 value of 15.2 μM. Its pharmacological profile makes it a valuable tool for investigating gut-related disorders. -
Dopamine D3 Receptor Antagonist
SB-277011 hydrochloride is a selective antagonist of the dopamine D3 receptor (D3R), demonstrating potent inhibition with Ki values of 10.7 nM in rodents and 11.2 nM in humans. This compound exhibits significant selectivity, with an 80- to 100-fold preference for D3R over other dopamine receptors, including D2, 5-HT1B, and 5-HT1D. Due to its ability to penetrate the brain and oral bioavailability, SB-277011 hydrochloride is valuable in research investigating the role of D3R in various neurological and psychiatric disorders. -
Dopamine/5-HT2A Antagonist
Paliperidone palmitate is a competitive antagonist of dopamine D2 and 5-hydroxytryptamine 2A (5-HT2A) receptors with the capability to cross the blood-brain barrier. By binding to these receptors, it modulates the activity of dopamine and serotonin, thereby exerting antipsychotic effects. This compound is primarily utilized in research related to schizophrenia and other neuropsychiatric disorders, contributing to the understanding of antipsychotic mechanisms and therapeutic strategies. -
5-HT2B Receptor Agonist
(+)-Norfenfluramine hydrochloride is a selective agonist of the 5-HT2B receptor, exhibiting a Ki value of 11.2 nM. This compound effectively stimulates the hydrolysis of inositol phosphates and enhances intracellular calcium levels. Its biological activity makes it a valuable tool for studies related to primary pulmonary hypertension and valvular heart disease. -
Rat 5-HT1B Antagonist
NAS-181 dimesylate is a selective antagonist of the rat 5-HT1B receptor, exhibiting a Ki value of 47 nM. With a notable 13-fold selectivity for the r5-HT1B receptor compared to the bovine equivalent (Ki=630 nM), NAS-181 effectively enhances serotonin (5-HT) turnover and improves synaptic 5-HT concentration by blocking terminal r5-HT1B autoreceptors. This compound is valuable for research involving serotonin modulation and related neuropharmacological studies. -
5-HT Receptor Inhibitor
Ansofaxine hydrochloride is a potent triple reuptake inhibitor that targets the serotonin, dopamine, and norepinephrine transporters. It demonstrates inhibition with IC50 values of 723 nM for serotonin, 491 nM for dopamine, and 763 nM for norepinephrine. This compound is primarily used in research to investigate the mechanisms underlying mood disorders and has potential applications in studies focused on neuropharmacology and the treatment of depression and anxiety. -
β-arrestin-biased 5-HT2AR Agonist
IHCH-7086 is a partial β-arrestin-biased agonist of the 5-HT2A receptor, exhibiting a Ki value of 12.59 nM, and capable of crossing the blood-brain barrier. This compound has demonstrated effectiveness in blocking D-lysergic acid diethylamide-induced head-twitch responses in murine models and alleviating depression-like behaviors in mice subjected to acute restraint stress or corticosterone administration. IHCH-7086 is particularly relevant for research focused on depression and related neuronal signaling pathways. -
α/β-Adrenergic Receptor Blocker
Arotinolol is a nonselective α/β-adrenergic receptor blocker that also acts as a vasodilating β-blocker. It exhibits significant inhibitory activity against the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is primarily utilized as an antihypertensive agent in the management of various cardiovascular conditions, as well as for certain non-cardiovascular diseases, facilitating research in cardiovascular pharmacology and receptor interaction studies. -
Dopamine Receptor Antagonist
2-Bromo-LSD (BOL-148; Bromolysergide) is a potent dopamine receptor antagonist specifically targeting dopamine neurons in the substantia nigra and neostriatum. It enhances the hydroxylation of tyrosine within the striatum and mitigates the reduction of Apomorphine-induced DOPA accumulation. Additionally, 2-Bromo-LSD inhibits 5-HT receptor-mediated DOPA formation, making it valuable for research on neurotransmitter regulation and potential therapeutic applications in neuropharmacology. -
5HT4 Agonist
Mosapride citrate dihydrate is a 5-HT4 receptor agonist that serves as a gastroprokinetic agent. It enhances gastrointestinal motility by selectively stimulating upper gastrointestinal function. Additionally, Mosapride demonstrates a concentration-dependent inhibition of Kv4.3 channels, with an IC50 value of 15.2 μM, making it valuable in research related to various gastrointestinal disorders. -
5-HT Agonist
Quipazine is a potent 5-HT3 receptor agonist, exhibiting a Ki value of 1.4 nM for the displacement of [3H]GR65630 from the receptor in rat models. In addition to its central nervous system applications, Quipazine demonstrates antiviral activity against SARS-CoV-2, with an EC50 of 31.64 μM. This compound is valuable for investigating neurological diseases and understanding serotonergic signaling pathways. -
5-HT1D/5-HT1B Receptor Antagonist
GR127935 hydrochloride is a potent antagonist of the 5-HT1D and 5-HT1B receptors, demonstrating pKis of 8.5 for both isoforms. It exhibits a significant 100-fold selectivity for the 5-HT1B and 5-HT1D receptors compared to other serotonin receptor subtypes, including 5-HT1A, 5-HT2A, and 5-HT2C. This compound is valuable for research involving neurological diseases and exploring serotonin receptor dynamics. -
5-HT7 Agonist
LP44 hydrochloride is a selective agonist of the 5-HT7 receptor, exhibiting a Ki value of 0.22 nM. This compound induces a dose-dependent hypothermic response when administered via intracerebroventricular injection, although it does not elicit significant hypothermia when given intraperitoneally. LP44 hydrochloride is valuable for studying the physiological roles of 5-HT7 receptors and their potential therapeutic applications in neurological research. -
5-HT2B Receptor Agonist
(+)-Norfenfluramine is a selective agonist of the 5-HT2B receptor, with a binding affinity (Ki) of 11.2 nM. This compound effectively stimulates the hydrolysis of inositol phosphates, resulting in enhanced intracellular calcium levels. (+)-Norfenfluramine is utilized in research focused on primary pulmonary hypertension and valvular heart disease, providing insight into pathology and potential therapeutic avenues. -
5-HT1A Modulator
5-HT1A modulator 2 hydrochloride is a selective modulator of the serotonin 5-HT1A receptor, demonstrating a Ki value of 53 nM for 5-HT1A binding. This compound is primarily utilized in research related to neuropharmacology and psychiatric disorders, providing insights into serotonin signaling pathways. Its modulation of the 5-HT1A receptor makes it a valuable tool for studying anxiety, depression, and other mood-related conditions. -
5-HT7 Receptor Agonist
AS19 is a highly potent and selective agonist of the 5-HT7 receptor, with an IC50 value of 0.83 nM and a Ki of 0.6 nM. It demonstrates significant selectivity over other serotonin receptors, including 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A, with Kis values ranging from 6.6 nM to 490 nM. AS19 has been shown to enhance memory consolidation and effectively reverse amnesia induced by Scopolamine or Dizocilpine, making it a valuable tool for research in cognitive function and neuropharmacology. -
GlyT2/5HT2A Antagonist
Opiranserin hydrochloride is a dual antagonist targeting glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), exhibiting IC50 values of 0.86 and 1.3 μM, respectively. In addition, it demonstrates antagonistic activity on recombinant P2X3 receptors with an IC50 of 0.87 μM. This compound is under development as an injectable analgesic for postoperative pain management, making it relevant for research in pain pathways and therapeutic interventions. -
5-HT Modulator
13,14-Dihydro-15-keto-PGE2 functions as a 5-HT modulator, playing a crucial role in the serotonergic pathway. This compound has been demonstrated to alleviate opioid-induced constipation by modulating gastrointestinal activity through the action on 5-HT receptors. It is valuable in research applications related to gastrointestinal motility and the management of opioid side effects. -
Dopamine D2/5-HT2A Receptor Antagonist
Spiperone hydrochloride is a potent antagonist of dopamine D2 and 5-HT2A receptors, exhibiting Ki values of 0.06 nM and 1 nM, respectively. In addition, it selectively antagonizes the α1B-adrenoceptor and activates calcium-activated chloride channels (CaCC). This compound has demonstrated significant antipsychotic and anti-inflammatory properties, making it a valuable tool for research in neuropharmacology and inflammation studies. -
5-HT2A receptor Antagonist
Pruvanserin is a selective antagonist of the 5-HT2A receptor, demonstrating significant potential in modulating serotonergic pathways. This compound has been shown to alleviate tactile allodynia in diabetic rat models, indicating its usefulness in pain research. Additionally, Pruvanserin is being explored for its applications in studying insomnia and related sleep disorders. -
5-HT2C Receptor Antagonist
SB 243213 is a selective and high-affinity antagonist of the 5-HT2C receptor, exhibiting a pKi of 9.37 and a pKb of 9.8 for the human receptor. This compound demonstrates over 100-fold selectivity against a variety of neurotransmitter receptors, enzymes, and ion channels. SB 243213 shows an improved anxiolytic profile, making it a potential candidate for research applications related to schizophrenia and motor disorders.
