Catalog No.
Product Name
Application
Product Information
Citations
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5-HT2A/dopamine D2 antagonist
Abaperidone is a potent antagonist of 5-HT2A?receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM. -
5-HT1A modulator
5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively. -
5-HT7 receptor antagonist
JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively. -
5-HT3 partial agonist
Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease. -
5-HT1B receptor antagonist
SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity. -
5-HT2/sigma 2 receptor antagonist
Roluperidone, also known as MIN-101, CYR-101, and MT-210, is a 5-HT2A and sigma 2 receptor antagonist potentially for the treatment of schizophrenia. -
5-HT3 receptor selective agonist
Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM. -
5-HT1A/5-HT1B/5-HT1C agonist
Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. -
5-HT2B receptor antagonist
RS 127445 is a novel high affinity, selective 5-HT2B receptor antagonist with pKi of 9.5. -
5-HT1A/5-HT1B/5-HT3A/5-HT7 receptor/SERT inhibitor
Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. -
5-HT(2C) receptor agonist
WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a Ki of 10.5??1.1 nM. -
5-HT2C receptor antagonist
SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. -
5-HT6 receptor antagonist
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). -
5-HT2A inverse agonist
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively. -
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. -
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). - SEP-363856, also known as SEP-856, is an orally active and CNS active psychotropic agent.
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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. -
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. -
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-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-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-HT1B/1D Agonist
Zolmitriptan is a selective partial agonist of the 5-HT1B and 5-HT1D receptors, demonstrating high affinity with Ki values of 5.01 nM and 0.63 nM, respectively. It effectively crosses the blood-brain barrier, making it a valuable tool in migraine research. This compound is primarily utilized for studying the pathophysiology of migraines and developing targeted therapeutic interventions.
