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5-HT Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S1333 Fluoxetine HCl Fluoxetine HCl is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.
Cell Rep, 2024, 43(10):114818
Int Immunopharmacol, 2024, 128:111524
Front Psychiatry, 2023, 14:1198502
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S4749 Citalopram HBr Citalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.
Cell Rep, 2024, 43(10):114818
Chem Biol Interact, 2024, 403:111246
Aging (Albany NY), 2021, 13(11):14729-14744
S8183 Pimavanserin tartrate Pimavanserin tartrate(ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease.
Nat Neurosci, 2025, 28(11):2285-2295
Br J Pharmacol, 2021, 10.1111/bph.15756
Mol Ther Oncolytics, 2020, 19:19-32
S1483 Iloperidone Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
Anticancer Res, 2021, 41(2):687-697
bioRxiv, 2021, 10.1101/2021.11.14.468520
Sci Rep, 2018, 8(1):15753
E4953 Citalopram Citalopram is a selective serotonin reuptake inhibitor (SSRI) that selectively inhibits the 5-HT transporter, blocks the reuptake of 5-HT in the presynaptic membrane, prolongs and increases the effects of 5-HT, and enhances serotonin neurotransmission by potently and selectively inhibiting serotonin reuptake (SSRI).
Alzheimers Dement, 2025, 21(3):e70081
S2582 Trazodone HCl Trazodone HCl (AF-1161, KB-831) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
J Lipid Res, 2022, 63(8):100249
S3175 Atomoxetine HCl Atomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters.
Cell Commun Signal, 2024, 22(1):532
S5563 Thioridazine hydrochloride Thioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent.
Cell Syst, 2019, 8(2):97-108
S1869 Dapoxetine HCl Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.
S0282 YL 0919 YL0919, a novel structure compound, exerts dual effect on the serotonergic system, as both 5-hydroxytryptamine receptor 1A (5-HT1A) agonist and 5-HT uptake blocker, showing remarkable antidepressant effects in animal models.
S9239 Isocorynoxeine Isocorynoxeine (7-Isocorynoxeine), a major alkaloid found in Uncaria rhynchophylla, exhibits wide beneficial effects on the cardiovascular and cardiocerebral vascular systems. This compound suppresses 5-HT2A receptor-mediated current response with IC50 of 72.4 μM.
S9258 (+)-Isocorynoline Isocorynoxeine, a major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM and shows various beneficial effects, including lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage.
S0318 Ansofaxine hydrochloride Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.
E4812 Fluoxetine Fluoxetine (LY-110140 free base) is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. This compound is used widely in the treatment of depression, anxiety-related symptoms and also displays anticonvulsant activity.
E4866 Paroxetine Paroxetine is a potent and selective serotonin reuptake inhibitor (SSRI) used to treat depression and anxiety disorders. It inhibits pyroptosis and reduces osteoclast formation by blocking the NF-κB signalling pathway.
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S9039 Albiflorin Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity.
E7725 Doxepin Doxepin (MF 10) is a potent inhibitor of serotonin reuptake and noradrenaline reuptake with a Ki of 68 nM and 29.5 nM, respectively. It acts as a receptor antagonist for histamine H1, acetylcholine muscarinic, and α1 adrenoceptor with a Ki of 0.24 nM, 83 nM, and 24 nM, respectively and significantly inhibits CYP450.
S6465 Tafamidis Tafamidis is a kinetic stabilizer of transthyretin (TTR) that prevents amyloidogenesis by wild-type and mutant TTRs.
E4907 Clomipramine Clomipramine(Hydiphen, Anafranil base) blocks the production of norepinephrine in the central nervous system and 5-HT reuptake, thereby exerting sedative and anticholinergic effects, with IC50 of 1.5 nM. This compound is also a non-selective monoamine reuptake inhibitor that can affect the transmission of multiple neurotransmitters.
S9510 Protriptyline hydrochloride Protriptyline Hydrochloride is the hydrochloride salt form of protriptyline. Protriptyline is a tricyclic secondary amine with antidepressant property which acts by inhibition of serotonin and norepinephrine reuptake.
S3024 Lamotrigine Lamotrigine (BW-430C,LTG) 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 this compound also is a sodium channel blocker.
iScience, 2024, 27(10):110862
Front Pharmacol, 2024, 15:1489888
Nat Commun, 2022, 13(1):2785
S4053 Sertraline HCl Sertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM.
EMBO Mol Med, 2025, 17(4):625-644
Cell Rep, 2024, 43(10):114818
Antimicrob Agents Chemother, 2021, AAC.01146-20
S2084 Duloxetine HCl Duloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
Cancers (Basel), 2022, 14(19)4883
Drug Metab Dispos, 2015, 44(3):378-88
J Pharmacol Exp Ther, 2014, 349(3):402-7
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S4064 Escitalopram Oxalate Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.
Proc Natl Acad Sci U S A, 2025, 122(10):e2420499122
Cell Rep, 2024, 43(10):114818
J Matern Fetal Neonatal Med, 2023, 36(1):2183468
S3183 Amitriptyline HCl Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. This compound also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. It is a tricyclic antidepressant (TCA).
Environ Toxicol Chem, 2021, 10.1002/etc.5018
PLoS Pathog, 2020, 16;16(3):e1008341
Sci Rep, 2018, 8(1):15753
S4377 Imipramine HCl Imipramine (Melipramine,G 22355) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).
Cancer Drug Resist, 2022, 5(3):612-624
Antioxidants (Basel), 2021, 10(6)956
Biomedicines, 2021, 9(9)1230
S3817 Harmine hydrochloride Harmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs), PPARγ and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM.
Cell Death Discov, 2025, 11(1):282
Cancers (Basel), 2022, 14(2)326
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
J Immunother Cancer, 2024, 12(11)e009805
S5485 Desipramine Hydrochloride Desipramine hydrochloride (Desmethylimipramine, Norimipramine, EX-4355, G-35020, JB-8181, NSC-114901) is a dibenzazepine-derivative tricyclic antidepressant that acts as a selective norepinephrine reuptake inhibitor. It also shows weak serotonin reuptake inhibitory, α1-blocking, antihistamine, and anticholinergic effects.
S5071 Duloxetine Duloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake.