Catalog No.
Product Name
Application
Product Information
Citations
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5-HT receptor agonist
MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively). -
5-HT receptor agonist
Quipazine maleate is a selective 5-HT receptor agonist that promotes the proliferation and apoptosis of human hepatocyte strain of L-02 strain and could also exert an excitatory effect on raphe neurons via stimulation of 5-HT2A receptors. -
norepinephrine reuptake inhibitor
(R)-Viloxazine Hydrochloride is the R-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant. -
norepinephrine reuptake inhibitor
(S)-Viloxazine Hydrochloride is the S-isomer of Viloxazine, a selective norepinephrine reuptake inhibitor (NRI) that can be used as an antidepressant. -
Serotonergic Receptor Antagonist
Hymenidin is a natural antagonist of serotonergic receptors, exhibiting significant inhibitory effects on voltage-gated potassium channels. This compound demonstrates the ability to induce apoptosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutics targeting serotonergic signaling pathways. Its dual action on ion channels and receptor antagonism positions Hymenidin as a noteworthy reagent for exploring complex cellular mechanisms in neurobiology and oncology. -
5-HT2BR Antagonist
PRX-08066 maleate is a selective antagonist of the 5-hydroxytryptamine receptor 2B (5-HT2BR) with a Ki value of 3.4 nM. It effectively inhibits the MAPK signaling pathway, as well as the release of serotonin and the expression of key fibrotic factors such as TGFβ1, CTGF, and FGF2. PRX-08066 maleate demonstrates the ability to inhibit the proliferation of KRJ-I cells and induce apoptosis via caspase-3 activation. This compound shows potential for research in the context of pulmonary arterial hypertension (PAH) and neuroendocrine tumors (NET). -
5-HT5A Receptor Antagonist
SB-699551 free base is a selective antagonist of the 5-HT5A receptor, characterized by a pKi of 8.2 nM, which allows for effective brain penetration. It exhibits significant selectivity over various serotonin receptor subtypes, dopamine receptors, and the α1B adrenoceptor. This compound disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, influencing the phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. SB-699551 free base is valuable for research into anxiety, breast cancer, and Alzheimer's disease. -
5-HT5A Antagonist
SB-699551 is a selective 5-HT5A receptor antagonist with a pKi of 8.2 nM, demonstrating significant brain penetrance. This compound exhibits high selectivity over various 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptors. By disrupting Gαi/o-coupled signaling and the PI3K/AKT/mTOR pathways, SB-699551 influences phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. It serves as a valuable tool in the study of anxiety, breast cancer, and Alzheimer's disease. -
5-HT antagonist
Pimethixene maleate is a potent antihistamine and antiserotonergic compound used as an antimigraine agent. It exhibits strong antagonistic activity at multiple receptors, including serotonin 5-HT1A (pKi 7.63), 5-HT2A (pKi 10.22), 5-HT2B (pKi 10.44), 5-HT2C (pKi 8.42), histamine H1 (pKi 10.14), dopamine D2 (pKi 8.19), dopamine D4.4 (pKi 7.54), muscarinic M1 (pKi 8.61), and muscarinic M2 (pKi 9.38) receptors. Its broad receptor-binding profile contributes to its therapeutic efficacy in migraine management. -
5-HT1A receptor agonist
Buspirone is an orally active anxiolytic agent that acts as a partial agonist at 5-HT1A receptors and an antagonist at dopamine D2 autoreceptors. It is commonly used in the research and treatment of generalized anxiety disorder (GAD), offering anxiolytic effects without the sedative or dependence-forming properties of benzodiazepines. -
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. -
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. -
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. -
CGRP Receptor Antagonist/5-HT1F Receptor Agonist
PCC0105005 is a potent CGRP receptor antagonist, exhibiting an IC50 of 1.01 nM, coupled with partial agonist activity at the 5-HT1F receptor, with an EC50 of 77.91 nM. This compound demonstrates significant efficacy in preclinical migraine models, effectively reducing the expression levels of CGRP and c-Fos proteins and inhibiting ERK and CREB phosphorylation. PCC0105005 is suitable for research focused on migraine pathophysiology and potential therapeutic interventions. -
5-HT Reuptake Inhibitor
Mesembrine, also known as (+)-Mesembrine, is a potent inhibitor of the 5-HT transporter with a Ki value of 1.4 nM. This alkaloid, characterized by its aryloctahydroindole structure, also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM. Due to its selective targeting of serotonin reuptake, Mesembrine is valuable for studies related to mood regulation and various neuropsychiatric disorders, as well as investigations into PDE4B's role in inflammatory processes. -
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. -
Serotonin 5HT3-receptor antagonist
Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome. - Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
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5-HT6 receptor antagonist
SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9. -
serotonin transporter (SER) inhibitor
Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist. - Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic (to treat nausea and vomiting). Ondansetron reduces the activity of the vagus nerve, which deactivates the vomiting center in the medulla oblongata, and also blocks serotonin receptors in the chemoreceptor trigger zone.
- Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA) . Structurally, mirtazapine can also be classified as a tetracyclic antidepressant (TeCA).
- Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor (SARI) class. It is a phenylpiperazine compound. Trazodone also has anti-anxiety (anxiolytic) and sleep-inducing (hypnotic) effects.
- Urapidil hydrochloride is an α1-adrenoceptor antagonist, 5-HT1A serotonin receptor partial agonist and anti-hypertensive.
- Duloxetine Hydrochloride is a dual serotonin and norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of stress urinary incontinence, as well as depression.
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5-HT antagonist
Tegaserod functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist. -
D2/5-HT2 receptor antagonist
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic. - Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
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5-HT2c receptor agonist
PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1. -
5-HT4 receptor antagonist
5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6. -
5-HT2A receptor antagonist
Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). -
5-HT6R antagonist
Lu AE58054 is a potent and selective 5-HT6 receptor antagonist. -
5-HT Receptor modulator
Lu-AA21004 is an oral multimodal serotonergic agent, inhibits 5-HT(1A), 5-HT(1B), 5-HT(3A), 5-HT(7) and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. -
5-HT1A receptor agonist
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. -
5-HT3 receptor antagonist
Pancopride is a new potent and selective 5-HT3 receptor antagonist. -
5-HT2A and 5-HT2C receptors antagonist
Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist. -
5-HT1B receptor agonist
Eletriptan is a selective 5-hydroxytryptamine 1B/1D (5-HT1B) receptor agonist -
5-HT1A receptor antagonist
NAD 299 hydrochloride (Robalzotan) is a selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro). -
5-HT1B/1D receptors agonist
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively. -
5-HT Receptor antagonist
Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner.
