2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor
  5. 5-HT Receptor Isoform
  6. 5-HT Receptor Inhibitor

5-HT Receptor Inhibitor

5-HT Receptor Inhibitors (61):

Cat. No. Product Name Effect Purity
  • HY-B0527
    Amitriptyline
    		Inhibitor 99.94%
    Amitriptyline is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline has antidepressant activity.
  • HY-121675
    2-Bromo-LSD
    		Inhibitor
    2-Bromo-LSD (BOL-148; Bromolysergide) is a Dopamine Receptor antagonist that directly affects dopamine neurons in the substantia nigra neostriatum. 2-Bromo-LSD increases the hydroxylation of tyrosine in striatum and antagonizes the decrease of Apomorphine-induced DOPA accumulation. 2-Bromo-LSD also blocks the 5-HT Receptor mediated DOPA formation.
  • HY-100923
    H-9 Dihydrochloride
    		Inhibitor 98.98%
    H-9 Dihydrochloride is a PKA (protein kinase) inhibitor. H-9 Dihydrochloride (10 μM) significantly reduces the excitatory response to 5-HT. H-9 Dihydrochloride also has a direct effect on pharyngeal activity. H-9 Dihydrochloride inhibits signal-transduction and cell growth in EGF (epidermal growth factor)-dependent epithelial cell lines.
  • HY-W019599
    4-Chloro-L-phenylalanine
    		Inhibitor ≥98.0%
    4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2).
  • HY-12390
    Lofepramine
    		Inhibitor ≥99.0%
    Lofepramine (Lopramine) is a modified tricyclic and orally active antidepressant. Lofepramine inhibits the uptake of Noradrenaline (NA) (HY-13715) and 5-hydroxytryptamine (5-HT) with IC50s of 2.7 μM and 11 μM, respectively. Lofepramine exerts its antidepressant activity by promoting noradrenergic neurotransmission. Lofepramine also enhances serotonergic neurotransmission by inhibiting neuronal uptake of 5-HT and tryptophan pyrrolase. Lofepramine exhibits significant anxiolytic properties. .
  • HY-118166
    Gentisein
    		Inhibitor 98.13%
    Gentisein (NSC 329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM.
  • HY-108256
    Melitracen hydrochloride
    		Inhibitor 99.90%
    Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride
    		Inhibitor 99.65%
    Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
  • HY-12394
    Dothiepin
    		Inhibitor 98.22%
    Dothiepin (Dosulepin; Dothep) is an antidepressant agent with sedative/anxiolytic activity. Dothiepin is an inhibitor preferring of noradrenaline uptake than serotonin uptake. Dothiepin facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. Dothiepin is also an antagonist of histamine H1-receptor without cardiotoxicity. Dothiepin exhibits significant analgesic activity in psychogenic facial pain，idiopathic fibromyalgia syndrome or rheumatoid arthritis.
  • HY-110289
    (R)-Citalopram oxalate
    		Inhibitor 99.52%
    (R)-Citalopram oxalate is an anticonvulsant, antidepressant and muscle relaxant. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (Escitalopram; HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate functionally antagonises S-citalopram in vivo and in vitro. (R)-Citalopram oxalate has an effect on the association of Escitalopram with the high affinity primary site, and on its dissociation from the 5-HT transporter, via an allosteric mechanism.
  • HY-110023
    Zimelidine dihydrochloride
    		Inhibitor 98.27%
    Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine dihydrochloride is an antidepressant.
  • HY-135096
    Amitriptyline-d3 hydrochloride
    		Inhibitor 99.46%
    Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
  • HY-12392
    Iprindole
    		Inhibitor 98.02%
    Iprindole, a tricyclic indole antidepressant, is a weak inhibitor of the uptake of noradrenaline and 5-HT.
  • HY-B0901S1
    Bromperidol-d4-1
    		Inhibitor
    Bromperidol-d4-1 is deuterium labeled Bromperidol.
  • HY-118835
    Zimelidine
    		Inhibitor
    Zimelidine is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine is an antidepressant.
  • HY-106487
    Pridefine
    		Inhibitor
    Pridefine (AHR-1118) is an antidepressant agent.
  • HY-136860
    (R)-Venlafaxine
    		Inhibitor
    (R)-Venlafaxine is the R-enantiomer of venlafaxine (HY-B0196), an orally active and potent dual inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake. (R)-Venlafaxine can be utilized in antidepressant research.
  • HY-N0740R
    Jatrorrhizine chloride (Standard)
    		Inhibitor
    Jatrorrhizine (chloride) (Standard) is the analytical standard of Jatrorrhizine (chloride). This product is intended for research and analytical applications. Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
  • HY-A0175
    Butriptyline
    		Inhibitor
    Butriptyline (Butriptylene) is an orally active tricyclic antidepressant that slightly enhances central 5-HT effects. Butriptyline does not inhibit brain norepinephrine uptake.
  • HY-A0171
    Benzoctamine
    		Inhibitor
    Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline.