Catalog No.
Product Name
Application
Product Information
Citations
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5-HT Receptor Antagonist
Methiothepin (Metitepine; Ro 8-6837) is a potent, non-selective antagonist of the 5-HT receptors, primarily targeting 5-HT2A, 5-HT2B, and 5-HT2C. It exhibits high affinity with pKi values of 8.50, 8.68, and 8.35 for these receptors, respectively. Methiothepin's antagonistic properties make it valuable for research in neuropharmacology, particularly in studies exploring serotonin signaling pathways and their implications in various mood disorders and psychotic conditions. -
5-HT2 Agonist
ALEPH hydrochloride is a partial agonist of the 5-HT2A and 5-HT2B receptors, exhibiting EC50 values of 10.3 nM and 19.2 nM, respectively. This compound induces a head twitch response in mice, with an ED50 of 0.80 mg/kg. ALEPH hydrochloride is suitable for research applications investigating serotonin receptor functions and their roles in neuropharmacology. -
5-HT3 Serotonin Receptor Agonist
Amanozine is a potent agonist of the 5-HT3 serotonin receptor, playing a critical role in mediating serotonin signaling within the nervous system. This compound exhibits potential therapeutic applications in the study of various neurological disorders, making it a valuable tool for research in psychopharmacology and neuropharmacology. Its ability to influence serotonin receptor activity could provide insights into the mechanisms underlying mood regulation and anxiety. -
5-HT4 Receptor Antagonist
GR125487 sulfamate is a selective antagonist of the 5-HT4 receptor, which plays a significant role in various cognitive and gastrointestinal functions. This compound effectively inhibits cognitive enhancement, making it valuable for researching memory disorders, mood disorders, gastrointestinal dysfunctions, and urinary tract issues. Its oral bioactivity allows for convenient administration in preclinical studies. -
5-HT(1B/1D) Receptor Agonist
Naratriptan-d3 hydrochloride is a selective agonist of the 5-HT1B/1D receptors. This deuterium-labeled derivative exhibits effective vasoconstrictive properties on cranial arteries through activation of these receptors, with an EC50 value of 0.11 μM observed in dog basilar arteries. Additionally, it is known to inhibit trigeminal nerve-mediated dural neurogenic plasma extravasation and mitigate sterile inflammation. Naratriptan-d3 hydrochloride is primarily utilized in research focusing on acute migraine, particularly related to cranial vascular dynamics and neuroinflammatory responses. -
5-HT2A/D2 Antagonist
Blonanserin dihydrochloride is a potent antagonist of the 5-HT2A and dopamine D2 receptors, exhibiting Ki values of 0.812 nM and 0.142 nM, respectively. This compound is primarily utilized as an atypical antipsychotic agent and is relevant for research focused on extrapyramidal symptoms, sedation levels, and hypotensive effects. Its pharmacological profile makes it a valuable tool in the study of neuropsychiatric disorders and related therapeutic interventions. -
5-HT2 Receptor Agonist
CYB210010 is a long-acting agonist of the serotonin 5-HT2 receptors, specifically targeting the 5-HT2A and 5-HT2C subtypes (EC50: 4.1 nM and 7.3 nM, respectively). This compound is orally bioavailable and capable of penetrating the central nervous system, leading to a notable head twitch response (HTR) without the development of behavioral tolerance following chronic administration. Its selectivity and consistent biological activity make CYB210010 a valuable tool for research into the roles of serotonin receptors in various neuropsychiatric conditions. -
5-HT1F Receptor Agonist
LY334370 hydrochloride is a highly selective agonist of the 5-HT1F receptor, demonstrating a binding affinity with a Kd value of 0.446 nM. This compound exhibits noteworthy anti-migraine activity, making it valuable for research in migraine pathophysiology and treatment exploration. Its mechanism of action highlights the therapeutic potential of targeting the serotonergic system in neurological disorders. -
Stable Isotope
Paliperidone-d4 is the deuterated form of Paliperidone, a major active metabolite of Risperidone, acting as a dopamine D2 antagonist and 5-HT2A antagonist. This compound also exhibits antagonistic properties at alpha-1 and alpha-2 adrenergic receptors as well as H1-histaminergic receptors. Paliperidone's primary application is in the treatment of schizophrenia, making it valuable for pharmacological research and development of antipsychotic therapies. -
5-HT Deamination Inhibitor
RS 2232 is a competitive inhibitor of 5-hydroxytryptamine (5-HT) deamination, demonstrating a Ki of 0.054 μM. This compound selectively and reversibly inhibits type A monoamine oxidase, making it a valuable tool in neurological research. RS 2232 is utilized to gain insights into the role of serotonin metabolism in various brain functions and disorders. -
D2 Receptor Binder
Mosapramine is a D2 receptor binder that acts as an antipsychotic agent and is a metabolite of Clocapramine. It selectively binds to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, exhibiting a D2/5-HT2 receptor occupancy ratio of 7.4. This compound induces characteristic neuropharmacological effects in rat models, including extrapyramidal symptoms, hyperprolactinemia, and increased salivation, while displaying a lower incidence of weight loss. Mosapramine is valuable for research applications related to schizophrenia and its underlying mechanisms. -
5-HT6 Receptor Agonist
ST1936 is a selective agonist of the 5-HT6 receptor, exhibiting nanomolar affinity with a Ki value of 13 nM for human 5-HT6 receptors. It also demonstrates notable selectivity across related serotonin receptors, with Ki values of 168 nM for 5-HT7 and 245 nM for 5-HT2B. Additionally, ST1936 has moderate affinity for human and rat α2 adrenergic receptors, with a Ki of 300 nM. This compound is valuable for neuroscience research, particularly in studies related to cognitive function and mood disorders. -
5-HT2 Antagonist
Spiramide is a potent and selective antagonist of the 5-HT2 receptor and dopamine D2 receptor, demonstrating Ki values of 2 nM and 3 nM, respectively. It exhibits over 2000-fold selectivity for the 5-HT2 receptor compared to the 5-HT1C receptor (Ki = 4300 nM). Due to its pharmacological properties, Spiramide is valuable for research applications in the fields of neuropharmacology and the study of antipsychotic mechanisms. -
5-HT2 Receptor Antagonist
(S)-Mirtazapine is a stereoselective antagonist of the 5-HT2 receptor, showing significant pronociceptive effects in animal models of acute thermal nociception. This S(+)-enantiomer exhibits distinct pharmacological properties, contributing to its potential applications in pain research and neuropharmacology. Additionally, (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2, which may influence its therapeutic efficacy and safety profile. -
Serotonin/Dopamine Receptor Modulator
Brexpiprazole S-oxide is the primary metabolite of the atypical antipsychotic Brexpiprazole, functioning as a serotonin and dopamine receptor modulator. It exhibits partial agonism at the human 5-HT1A receptor and antagonism at the 5-HT2A receptor, with affinities (Ki) of 0.12 nM and 0.47 nM, respectively, and a potent partial agonist effect at the dopamine receptor (Ki = 0.3 nM). This compound is utilized in research focused on neuropharmacology, psychopharmacology, and the modulation of serotonergic and dopaminergic signaling pathways. -
5-HT6/5-HT2A Antagonist
Landipirdine is a potent antagonist of the 5-HT6 and 5-HT2A receptors. This orally active compound is primarily investigated for its potential therapeutic effects in the context of Parkinson's disease. Its mechanism of action provides a valuable tool for researchers exploring receptor interactions and neuropharmacology related to neurodegenerative conditions. -
5HT4 Receptor Agonist
Renzapride is a full agonist of the 5-HT4 receptor, exhibiting a Ki value of 115 nM. Additionally, it acts as an antagonist at both the 5-HT2b and 5-HT3 receptors. This compound is primarily utilized in research focusing on constipation-predominant irritable bowel syndrome (C-IBS), making it valuable for exploring therapeutic interventions in gastrointestinal disorders. -
5-HT1A Receptor Agonist
Lauroscholtzine, also known as N-Methyllaurotetanine, acts as an agonist of the 5-HT1A receptor. This natural alkaloid is known for its modulatory effects on serotonergic signaling, making it a valuable tool for studying the role of serotonin in various physiological processes. Its biological activity is relevant for research into neuropharmacology, particularly in the context of anxiety and depression-related disorders. -
5-HT Receptor Antagonist
Seganserin is a potent orally active antagonist of the 5-HT receptor, exhibiting a plasma half-life of 26.1 ± 12.9 hours. This compound plays a crucial role in neurological research, offering insights into serotonin-mediated pathways and their implications in various neuropsychiatric conditions. Its selectivity for the 5-HT receptor makes it a valuable tool for exploring serotonin receptor signaling and pharmacology. -
5-HT Receptor Antagonist
Dolasetron Mesylate hydrate is a serotonin 5-HT3 receptor antagonist that primarily functions by blocking the action of serotonin at these receptors. This compound is widely utilized in research focused on understanding and mitigating chemotherapy-induced nausea and vomiting. Its efficacy in targeting the 5-HT3 receptor makes it a valuable tool in pharmacological studies related to antiemetic therapy. -
5-HT Receptor Control
2C-B-FLY hydrochloride is a selective 5-HT receptor agonist, functioning primarily on the serotonin receptor system. This compound exhibits significant hallucinogenic properties, making it valuable for research into psychoactive mechanisms and the modulation of serotonergic pathways. Its unique structure as a dihydrodifuran analog of 4-bromo-2,5-dimethoxyphenethylamine (2C-B) enhances its potential applications in behavioral and neuropharmacological studies. -
Vasopressin Receptor Agonist
Argipressin acetate is a potent vasopressin receptor agonist, primarily targeting the V1, V2, and V3 receptors. It exhibits high affinity for the V1 receptor, with a dissociation constant (Kd) of 1.31 nM in A7r5 rat aortic smooth muscle cells. This compound is valuable for research applications exploring vascular physiology, fluid balance, and the modulation of blood pressure. -
Stable Isotope
Anandamide-d8 is a deuterated form of the endocannabinoid Anandamide, primarily known for its interaction with cannabinoid receptors CB1 and CB2. This compound modulates various neuronal and immune functions and can also engage additional receptors, including PPARs, TRPV1, and GPR18/GPR55. Anandamide-d8 exhibits potential anti-fungal and anti-inflammatory properties, making it valuable for research applications in fields such as neurodegenerative diseases, including Alzheimer's disease, and inflammatory conditions like ulcerative colitis. -
PARP-1 Inhibitor
Benzo[c][1,8]naphthyridin-6(5H)-one is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1) and aurora kinase A, exhibiting IC50 values of 0.311 μM and 5.5 μM, respectively. This compound demonstrates low micromolar affinity for human adenosine receptors AR A1 and hA2A, with Ki values of 4.6 and 4.8 μM. Due to its mechanistic action, Benzo[c][1,8]naphthyridin-6(5H)-one is valuable for research applications targeting DNA repair pathways and cancer therapies. -
Histamine H2-Receptor Antagonist
Ranitidine hydrochloride is a selective histamine H2-receptor antagonist that effectively inhibits gastric secretion. It demonstrates significant antagonism of histamine-induced cardiac and uterine responses in isolated animal models, with pA2 values of 7.2 and 6.95, respectively. Additionally, ranitidine hydrochloride has been shown to inhibit the development and metastasis of breast tumors in murine models, indicating its potential utility in cancer research. -
5-HT1 Agonist
Rizatriptan benzoate is a selective agonist of the 5-HT1B and 5-HT1D serotonin receptors. It exhibits vasoconstrictive properties that affect peripheral blood flow and effectively penetrates the blood-brain barrier, thereby inhibiting pain neurotransmission within the central nervous system. This compound is primarily utilized in research focused on migraine pathophysiology and the modulation of serotonergic signaling. -
5-HT1 Receptor Agonist
Sumatriptan succinate is a selective agonist for the 5-HT1 receptor subtype, notably demonstrating IC50 values of 7.3 nM, 9.3 nM, and 17.8 nM for the 5-HT1D, 5-HT1B, and 5-HT1F receptors, respectively. This compound is primarily utilized in the study of migraine pathophysiology and therapeutics, providing insights into serotonin modulation during migraine attacks. Its pharmacological profile makes it an essential reagent for research investigating the efficacy of triptans in headache relief. -
A2A Receptor/HDAC Inhibitor
IHCH-3064 is a dual-target compound that inhibits the Adenosine A2A Receptor and histone deacetylase (HDAC). It demonstrates potent binding affinity for the A2A receptor (Ki = 2.2 nM) and selectively inhibits HDAC1 with an IC50 of 80.2 nM. This compound exhibits significant antiproliferative activity against various tumor cell lines in vitro, making it a valuable tool for tumor immunotherapy research applications. -
Dopamine D2/D3 Agonist
Piribedil maleate is a potent agonist of dopamine D2 and D3 receptors, with additional activity as an α2-adrenoceptor antagonist. It has been shown to inhibit MLL1 methyltransferase activity with an EC50 of 0.18 μM. Piribedil maleate is of interest for research applications related to Parkinson’s disease, circulatory disorders, and various cancers. -
Dopamine D2/D3 Agonist
Piribedil hydrochloride is a potent agonist of dopamine D2 and D3 receptors, serving as a valuable tool for investigating dopaminergic signaling pathways. In addition to its agonistic activity, it acts as an antagonist at α2-adrenoceptors and inhibits MLL1 methyltransferase with an EC50 of 0.18 μM. This compound is primarily utilized in research related to Parkinson's disease, circulatory disorders, and certain types of cancer, making it an important reagent for studies focused on neurodegeneration and tumor biology. -
Dopamine D2/D3 Agonist
Piribedil dihydrochloride is a potent dopamine D2 and D3 agonist, also functioning as an antagonist at α2-adrenoceptors. This compound exhibits inhibitory activity on MLL1 methyltransferase with an EC50 of 0.18 μM. It is primarily utilized in research focused on Parkinson's disease, circulatory disorders, and various types of cancers. -
Histamine N-Methyltransferase Inhibitor
SKF 91488 dihydrochloride is a potent, noncompetitive inhibitor of histamine N-methyltransferase, exhibiting a Ki value of 0.9 μM. This compound effectively blocks the metabolism of histamine, leading to elevated concentrations of histamine in biological systems. SKF 91488 dihydrochloride plays a significant role in research focusing on infection, inflammation, and cardiovascular diseases, including studies on Mycoplasma pneumonia and hemorrhagic hypotension. Its influence on blood pressure and bronchoconstriction further underscores its utility in exploring related pathophysiological mechanisms. -
Stable Isotope
Dopamine-d5 hydrochloride is a deuterium-labeled analogue of dopamine, a catecholamine neurotransmitter primarily synthesized in the substantia nigra, ventral tegmental area, and hypothalamus. This compound retains the essential biological functions of dopamine, including its interaction with D2 dopamine receptors, which mediates the endocytosis of VEGFR2, a key process in angiogenesis. Dopamine-d5 hydrochloride is valuable for research applications involving neurotransmitter dynamics, neuropharmacology, and angiogenic pathways. -
Antipsychotic Agent
Penfluridol is a potent, long-acting antipsychotic agent that primarily targets D2-like dopamine receptors. It exhibits significant anti-inflammatory properties by inhibiting TNFα-induced NF-κB activation and demonstrates efficacy in models of arthritis and colitis. Additionally, Penfluridol acts as a Ca2+-calmodulin inhibitor, inducing apoptosis and autophagy in various cellular contexts. This compound is utilized in research focusing on chronic schizophrenia, acute psychosis, Tourette syndrome, autoimmune diseases, and it also shows antibacterial activity against E. faecalis with a minimum inhibitory concentration of 7.81 μg/ml. -
Dopamine Receptor Antagonist
Perphenazine is a potent dopamine receptor antagonist, specifically targeting D2 and D3 receptors with Ki values of 0.56 nM and 0.43 nM, respectively, while also interacting with the 5-HT2A receptor and the Alpha-1A adrenergic receptor. This compound demonstrates inhibitory effects on cancer cell proliferation and promotes apoptosis. Perphenazine is valuable for research into psychiatric disorders, cancer biology, and inflammatory processes. -
H1 Receptor Antagonist
Pheniramine maleate is a first-generation histamine H1 receptor antagonist that primarily targets the central nervous system to produce sedative and hypnotic effects. In addition to its antihistaminic activity, Pheniramine maleate exhibits antitumor properties by inducing apoptosis in leukemia cells. It also demonstrates effectiveness as a local agent to alleviate pain and provide antipruritic effects in various applications. -
5-HT4 Agonist
Prucalopride succinate is a selective 5-HT4 receptor agonist known for its high affinity for human 5-HT4a and 4b receptors, with pKis of 8.6 and 8.1, respectively. This compound enhances intestinal motility and promotes regeneration of the enteric nervous system, making it relevant for research in chronic constipation and pseudo-intestinal obstruction. Additionally, Prucalopride succinate exhibits anticancer properties by inhibiting the PI3K/AKT/mTOR signaling pathway, thereby facilitating its application in cancer studies. -
Antibiotic
Adenoregulin, also known as Dermaseptin b2, is an antimicrobial peptide antibiotic that targets a broad spectrum of microorganisms. It exhibits activity against both Gram-negative and Gram-positive bacteria, as well as yeast and fungi. Additionally, Adenoregulin enhances the binding of agonists to the A1 adenosine receptor, making it valuable for research applications in microbiology and pharmacology. -
CXCR Inhibitor
Corydalmine, a CXCR inhibitor, demonstrates significant antifungal activity by inhibiting spore germination in various plant pathogenic and saprophytic fungi. Additionally, it serves as an oral analgesic agent, exhibiting potent analgesic effects. Corydalmine has been shown to alleviate Vincristine-induced neuropathic pain in murine models through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, making it a valuable tool for pain research and therapeutic applications. -
CXCR Inhibitor
Corydalmine hydrochloride is a potent CXCR inhibitor that demonstrates significant biological activity by inhibiting spore germination in certain plant pathogenic and saprophytic fungi. Additionally, it exhibits notable analgesic properties, effectively alleviating Vincristine-induced neuropathic pain in murine models. This effect is mediated through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, highlighting its potential applications in pain management research and fungal inhibition studies. -
Stable Isotope
Rimonabant-d10 is a deuterium-labeled analog of Rimonabant, a highly potent and selective antagonist of the central cannabinoid receptor (CB1) with a Ki of 1.8 nM. This compound not only exhibits strong brain penetration but also inhibits Mycobacterial membrane protein Large 3 (MMPL3). Rimonabant-d10 serves as a valuable tool for studying cannabinoid receptor signaling and the role of CB1 in various biological processes, as well as for applications in mycobacterial research. -
Cannabinoid
O,O-Dimethyl-cannabigerol primarily targets cannabinoid receptors and is derived from Cannabis sativa. It exhibits antibacterial activity against drug-resistant strains of Staphylococcus aureus, demonstrating a minimum inhibitory concentration (MIC) of 1 to 2 μg/mL. As a nonpsychoactive constituent, O,O-Dimethyl-cannabigerol is valuable for research into therapeutic applications of cannabinoids, particularly in antimicrobial studies. -
Stable Isotope
(R)-Propranolol-d7 is a deuterated derivative of (R)-Propranolol, serving as a stable isotope-labeled compound. This reagent is invaluable for pharmacokinetic studies and metabolic pathway analysis, enabling the tracking of drug metabolism and distribution in biological systems. Researchers can utilize (R)-Propranolol-d7 in studies focused on cardiovascular research, anxiety treatments, and the mechanisms of action associated with beta-adrenergic receptors. -
Platelet Aggregation Inhibitor
SCH 38519 is a potent platelet aggregation inhibitor that effectively inhibits thrombin-induced aggregation of human platelets, exhibiting an IC50 of 68 μg/mL. In addition to its antiplatelet activity, SCH 38519 demonstrates antibacterial properties against both Gram-positive and Gram-negative bacteria. This compound is valuable for research applications focused on thrombosis, cardiovascular diseases, and bacterial infections. -
D4R Antagonist
Dopamine D4 receptor ligand 3 is a selective antagonist of the dopamine D4 receptor (D4R), exhibiting a pKi of 8.86. It demonstrates significant activity with pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 signaling pathways in HEK-293T cells, respectively. Additionally, this compound has been shown to inhibit cell viability in three human glioma cell lines—U87 MG, T98G, and U251 MG—while also inducing reactive oxygen species (ROS) production and mitochondrial dysfunction in these glioma cells. This makes it a valuable tool for studying the role of D4R antagonism in cancer biology and neuropharmacology. -
β1-adrenoceptor Antagonist
Landiolol is a highly selective, ultra-short-acting antagonist of β1-adrenergic receptors. By competitively inhibiting these receptors, Landiolol effectively reduces heart rate and myocardial oxygen demand while minimally affecting cardiac ion channels and exhibiting a weak negative inotropic effect. Its ability to inhibit TNF-α-induced mitochondrial hyperactivity and reactive oxygen species production makes it valuable in models of sepsis, where it can mitigate renal injury. Landiolol is applicable in research involving perioperative tachycardia management and investigations into sepsis-related acute kidney injury. -
CB1 Receptor Inhibitor
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a selective inhibitor of the cannabinoid CB1 receptor. This neurosteroid, a key precursor in steroid hormone synthesis, can mitigate the effects of tetrahydrocannabinol (THC) by blocking its action at CB1 receptors. Additionally, Pregnenolone monosulfate sodium serves as a TRPM3 channel activator and has been shown to weakly activate TRPM1 channels. Its unique properties make it a valuable tool for investigating cannabinoid signaling and neuroprotective strategies against cannabis-related effects. -
Dopamine Receptors Blocker
Trifluoperazine is an antipsychotic agent primarily acting as a blocker of central dopamine receptors. It exhibits significant activity as a potent α1-adrenergic receptor antagonist and a NUPR1 inhibitor, demonstrating anticancer properties. Additionally, Trifluoperazine functions as a calmodulin inhibitor and inhibits P-glycoprotein, contributing to its diverse biological effects. This compound is utilized in research on schizophrenia and shows potential as a reversible inhibitor of influenza virus morphogenesis. -
CB1 Receptor Inhibitor
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a selective inhibitor of the cannabinoid CB1 receptor. By inhibiting the effects of tetrahydrocannabinol (THC) mediated through the CB1 receptors, it offers potential neuroprotective properties against cannabis intoxication. Additionally, Pregnenolone monosulfate serves as a TRPM3 channel activator and exhibits weak activation of TRPM1 channels, making it valuable for research in neuropharmacology and cannabinoid signaling pathways. -
Icmt Inhibitor
Cysmethynil is an inhibitor of Isoprenylcysteine carboxylmethyltransferase (Icmt) with an IC50 of 2.4 μM. It disrupts RAS membrane binding and interferes with EGF signal transduction, leading to cell cycle arrest in the G1 phase and the induction of autophagy. Cysmethynil effectively inhibits the proliferation of PC3 prostate cancer cells and demonstrates synergistic effects with chemotherapeutic agents such as Paclitaxel and Doxorubicin. This compound is applicable for research into solid tumors, including prostate cancer.
