Catalog No.
Product Name
Application
Product Information
Citations
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5-HT1D receptor antagonist
BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.
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5-HT3 antagonist
Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy. -
5-HT2/D1/D2 Antagonist
Olanzapine-d3 is a deuterated form of olanzapine, targeting multiple receptors, including serotonin receptors 5-HT2A, 5-HT2C, and dopamine receptors D1 to D4. This selective and orally active monoaminergic antagonist exhibits high affinity binding with Ki values ranging from 4 to 57 nM for relevant targets. It is primarily utilized in research related to psychopharmacology and the treatment of schizophrenia and bipolar disorder, enabling detailed pharmacokinetic studies and investigation of receptor interactions. -
5-HT6R Antagonist
PUC-10 is a potent antagonist of the 5-HT6 receptor, exhibiting a Ki value of 14.6 nM and an IC50 of 32 nM. Computational studies indicate that PUC-10 is orally bioactive and capable of penetrating the blood-brain barrier. This compound effectively induces autophagy in SH-SY5Y neuronal cells by inhibiting the mTOR signaling pathway. PUC-10 is ideally suited for studies focused on neurological disorders and related therapeutic strategies. -
5-HT2/D1/D2 Antagonist
Olanzapine hydrochloride is a selective antagonist of serotonin receptors (5-HT2A/2C, 5-HT3) and dopamine receptors (D1, D2). It exhibits high affinity binding to various targets, including H1, muscarinic M1-5, and adrenergic α1 receptors, contributing to its pharmacological profile. This atypical antipsychotic is primarily used in research focusing on neuropharmacology, the treatment of schizophrenia, and mood disorders, providing valuable insights into the modulation of neurotransmitter systems. -
5-HT Receptor Modulator
1-(1-Naphthyl)piperazine hydrochloride is a potent modulator of the 5-HT receptor system, functioning as an agonist at the 5-HT1A receptor while antagonizing the 5-HT2A receptor. This compound has demonstrated significant biological activity by inducing apoptosis in various cell types. Additionally, it exhibits potential in combatting immunosuppression and preventing photocarcinogenesis, making it a valuable tool for research in neuroscience and cancer studies. -
5-HT Receptor Modulator
1-(1-Naphthyl)piperazine is a modulator of the 5-HT receptors, functioning as an antagonist at the 5-HT2A receptor and an agonist at the 5-HT1A receptor. It demonstrates a binding affinity for the human 5-HT6 receptor with a Ki value of 120 nM. Additionally, 1-(1-Naphthyl)piperazine has been shown to inhibit forskolin-stimulated adenylate cyclase activity in calf substantia nigra, and it mitigates UV-induced immunosuppression. This compound induces S-phase cell cycle delay and apoptosis while elevating ROS levels, ultimately leading to the inhibition of MNT-1 cell proliferation, making it a valuable tool for melanoma research. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine mesylate is an orally active tricyclic antihistamine and anti-5-HT agent that exhibits significant activity against decerebrate rigidity, demonstrating minimal sedative and soporific effects. This compound effectively reduces or eliminates the influence of both static and dynamic fusimotor activity on muscle spindles in decerebrate models. Dimethothiazine mesylate is relevant for research applications related to hemicrania and spasticity. -
5-HT Receptor Agonist
8 Hydroxy PIPAT oxalate is a selective agonist of the 5-HT1A receptor. This compound activates serotonergic signaling pathways, promoting the degranulation of enteric mast cells and enhancing spontaneous histamine release in both guinea pig and human intestinal preparations. Its ability to modulate histamine release suggests potential applications in understanding and addressing functional gastrointestinal disorders, including irritable bowel syndrome. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine is a tricyclic antihistamine and anti-5-HT agent primarily targeting histamine receptors and serotonin pathways. It exhibits significant activity against decerebrate rigidity with minimal sedative and soporific effects. This compound effectively modulates fusimotor activity on muscle spindles in decerebrate models, making it a valuable reagent for studying conditions such as hemicrania and spasticity. -
5-HT Receptor Antagonist
AVN-101 is a potent 5-HT7 receptor antagonist with a Ki of 153 pM, demonstrating significant brain penetration and oral bioavailability. It also interacts with 5-HT6, 5-HT2A, and 5-HT2C receptors, exhibiting Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively. Additionally, AVN-101 has a high affinity for histamine H1 and adrenergic α2A, α2B, and α2C receptors, with Ki values ranging from 0.41 to 3.6 nM. This compound is suitable for research related to general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis. -
5-HT2A/ Histamine H1 Receptor Antagonist
LY2624803 is a potent antagonist of the 5-HT2A and histamine H1 receptors. This compound exhibits significant biological activity in modulating serotonergic and histaminergic signaling pathways, making it valuable for research in neuropharmacology. LY2624803 is particularly relevant for studies investigating mood disorders, anxiety, and other conditions associated with dysregulated serotonin and histamine receptor activity. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine hydrochloride is an orally active tricyclic antihistamine and anti-5-HT agent. It exhibits notable efficacy against decerebrate rigidity, demonstrating minimal sedative and soporific effects. This compound has been shown to diminish or eliminate the influence of fusimotor activity on the muscle spindle in decerebrate cats. Dimethothiazine hydrochloride is valuable for research on hemicrania and spasticity. -
5-HT Receptor Antagonist
Asenapine citrate is a 5-HT receptor antagonist that exhibits potent activity against serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4), and histamine receptors (pKi: 8.2-9.0). This atypical antipsychotic compound is primarily utilized in research focusing on schizophrenia and bipolar disorder, helping to elucidate the mechanisms of these neuropsychiatric conditions. -
H2 Histamine Receptors/ α2-AR/5-HT2(B,C) Serotonin Receptors Ligand
Platelet aggregation-IN-3 is a ligand for H2 histamine receptors, α2-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. This compound effectively inhibits platelet aggregation induced by ADP and collagen and modulates tumor cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 shows potential for applications in antiplatelet therapy for cardiovascular diseases and in the prevention of cancer-related thrombosis and tumor metastasis. -
5-HT Receptor Inhibitor
Proxibarbal is a barbiturate derivative that acts as a selective inhibitor of the 5-HT receptor. It demonstrates notable anti-anxiety properties and is utilized in research focused on migraine headache mechanisms. This compound serves as a valuable tool for understanding serotonergic pathways and their implications in anxiety and migraine disorders. - 5-Hydroxytryptophan (5-HTP) is a naturally occurring amino acid and chemical precursor as well as a metabolic intermediate in the biosynthesis of the neurotransmitters serotonin and melatonin from tryptophan.
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5-HT Receptor antagonist
Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist. - Citalopram is a selective inhibitor of ST (5-hydroxytryptamine/serotonin transporter) and therefore is a potent and selective serotonin reuptake inhibitor.
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5-HT Receptor agonist
Clomipramine is a blocker of the following transporters:Serotonin transporter (SERT) (Ki = 0.14 nM),Norepinephrine transporter (NET) (Ki = 54 nM),Dopamine transporter (DAT) (Ki = 3,020 nM),Glycine transporter (GlyT/LeuT). - Dapoxetine works by inhibiting serotonin transporter, increasing serotonins action at the post synaptic cleft, and as a consequence promoting ejaculatory delay.
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5-HT3 receptor antagonist
Granisetron HCl is a serotonin 5-HT3 receptor antagonist -
5-HT2A serotonin receptor antagonist
Ketanserin (Vulketan Gel) is specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. -
5-HT2/5-HT1 antagonist
Mianserin hydrochloride is a 5-HT2/5-HT1 antagonist. Has moderate affinity for 5-ht6 Non-selective 5-HT2 receptor antagonist. Has moderate affinity for 5-HT6. Antidepressant. -
5-HT4-receptor agonist
Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist. -
5-HT1A and α1-adrenergic receptor antagonist
Naftopidil 2HCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively. -
5-HT Receptors/D2 dopamine receptor antagonist
Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. -
5-HT Receptors antagonist
Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting, often following chemotherapy. -
5-HT (serotonin) and dopamine receptor antagonist
Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
Serotonin reuptake inhibitor
Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%). -
5-HT1F receptor agonist
LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist. -
5-HT1F agonist
LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM. -
SSR inhibitor / 5-HT1A receptor partial agonist
Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist. -
5-HT7 receptor antagonist
SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pKi of 8.3, exhibits >50-fold selectivity against other receptors. -
5-HT1B receptor antagonist
SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect. -
5-HT2 receptor antagonist
Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. -
5-HT2 receptor antagonist
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors. -
serotonin reuptake inhibitor/5-HT2A receptor antagonist
Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1. -
5-HT / dopamine receptor antagonist
Ziprasidone D8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
human 5-HT1A receptor partial agonist
Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. -
5-HT3 receptor antagonist
5-HT3 antagonist-4i is a 5-HT3 receptor antagonist which modulates the serotonergic system. -
5-HT4 receptor partial agonist
PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg. -
5-HT7 receptor antagonist
AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders.
