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

5-HT Receptor

5-HT receptors (5-hydroxytryptamine receptors) constitute a diverse neurotransmitter receptor family that regulates excitatory and inhibitory signaling across the central and peripheral nervous systems through G protein-coupled receptor pathways and ligand-gated ion channel mechanisms[1][4]. The receptor family controls intracellular second-messenger signaling, including cAMP, phospholipase C, inositol trisphosphate, and calcium mobilization, thereby influencing synaptic transmission, neuronal excitability, and neuroplasticity[1][5]. Mechanistically, most 5-HT receptor subtypes are G protein-coupled receptors, whereas 5-HT3 receptors form cation-selective ligand-gated ion channels that mediate rapid neuronal depolarization[1][2]. In disease-relevant models, dysregulated 5-HT receptor signaling has been associated with depression, psychosis, aggression, pain processing, and other neuropsychiatric disorders, supporting their importance as pharmacological targets[5][3][6]. Compared with related isoforms, receptor diversity is further expanded through alternative splicing and RNA editing, particularly within 5-HT2C, 5-HT4, 5-HT6, and 5-HT7 receptors, resulting in subtype-specific signaling and pharmacological properties[1]. For experimental applications, selective agonists and antagonists targeting 5-HT1A, 5-HT2A, and 5-HT7 receptors have been widely used to investigate synaptic plasticity, antidepressant mechanisms, psychotropic responses, and receptor-mediated cAMP signaling pathways[3][6][7].

5-HT Receptor 관련 제품 (551):

Cat. No. 상품명 효과 Purity
  • HY-B0072S
    Tropisetron-d5
    		Antagonist
    Tropisetron-d5 (SDZ-ICS-930-d5 (free base)) is deuterium labeled Tropisetron. Tropisetron (SDZ-ICS-930 free base) is an orally active anti-inflammatory and antiemetic agent. Tropisetron is 5-HT3R antagonists with a Ki of 5.3 nM. Tropisetron is also a partial agonist of α7 nicotinic receptor (α7 nAChR) with an EC50 of 1.3 μM. In addition, Tropisetron has antitumor and neuroprotective effects.
  • HY-N9374
    Bufotenidine
    		Agonist
    Bufotenidine, a natural indole alkaloid, is a blocking agent of the tryptaminic receptors.
  • HY-100658R
    Didesmethyl cariprazine (Standard)
    		Modulator
    Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
  • HY-B0670AR
    Dihydroergotamine mesylate (Standard)
    		Agonist
    Dihydroergotamine (mesylate) (Standard) is the analytical standard of Dihydroergotamine (mesylate). This product is intended for research and analytical applications. Dihydroergotamine mesylate is a BBB-permeable ergot alkaloid that can be used for the research of migraines.
  • HY-14151R
    Prucalopride (Standard)
    		Agonist
    Prucalopride (Standard) is the analytical standard of Prucalopride. This product is intended for research and analytical applications. Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.
  • HY-17410R
    Iloperidone (Standard)
    		Antagonist
    Iloperidone (Standard) is the analytical standard of Iloperidone. This product is intended for research and analytical applications. Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.
  • HY-W007223
    D-5-Hydroxytryptophan
    D-5-Hydroxytryptophan (D-5-HTP) is the D-isomer of 5-HTP and can be isolated from DL-5-hydroxytryptophan by continuous separation. Compared with intraperitoneal administration of L-5-Hydroxytryptophan, which can induce dose-dependent backward walking behavior in mice, D-5-Hydroxytryptophan has no significant effect on mouse behavior and is a negative control. D-5-Hydroxytryptophan is also a 5-HT ligand, capable of binding to the 5-HT site with affinity in the micromolar range.
  • HY-16687AR
    Eltoprazine hydrochloride (Standard)
    		Modulator
    Eltoprazine (hydrochloride) (Standard) is the analytical standard of Eltoprazine (hydrochloride). This product is intended for research and analytical applications. Eltoprazine (DU 28853) hydrochloride is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine hydrochloride shows antiaggressive and anxiogenic effects.
  • HY-W380450R
    Viloxazine (Standard)
    Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD).
  • HY-B1154R
    Penbutolol sulfate (Standard)
    		Antagonist
    Penbutolol (sulfate) (Standard) is the analytical standard of Penbutolol (sulfate). This product is intended for research and analytical applications. Penbutolol sulfate ((-)-Terbuclomine) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3.
  • HY-116554
    GYKI-46903
    		Antagonist
    GYKI-46903 is a non-competitive antagonist for 5-HT3 receptor, with the pIC50 of 6.91.
  • HY-B0071S2
    Granisetron-d6 (Standard)
    		Antagonist
    Granisetron-d6 (BRL 43694-d6) is deuterium labeled Granisetron. Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  • HY-100170R
    5-HT4 antagonist 1 (Standard)
    		Antagonist
    5-HT4 antagonist 1 (Standard) is the analytical standard of 5-HT4 antagonist 1 (HY-100170). This product is intended for research and analytical applications. 5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
  • HY-107836R
    Methiothepin mesylate (Standard)
    		Antagonist
    Methiothepin (mesylate) (Standard) is the analytical standard of Methiothepin (mesylate). This product is intended for research and analytical applications. Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
  • HY-170474
    2-Methyl-N,N-dimethyltryptamine
    		Ligand
    2-Methyl-N,N-dimethyltryptamine (2,N,N-TMT, compound 15) has binding affinity for serotonin (5-HT) receptor, with the pA2 of 6.04. 2-Methyl-N,N-dimethyltryptamine plays an important role in neurological disease research.
  • HY-10562AR
    Ketanserin tartrate (Standard)
    		Antagonist
    Ketanserin (tartrate) (Standard) is the analytical standard of Ketanserin (tartrate). This product is intended for research and analytical applications. Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
  • HY-108252
    SB-649915
    		Antagonist
    SB-649915 is a potent 5-HT1A/1B autoreceptor antagonist, with the pKi values of 8.6, 8.0, respectively and 5-HT reuptake inhibitor in native tissue systems and palys an important role in antidepressant research.
  • HY-103102R
    TCB2 (Standard)
    		Agonist
    TCB2 (Standard) is the analytical standard of TCB2 (HY-103102). This product is intended for research and analytical applications. TCB2 is an agonist of serotonin 5-HT2A receptor.
  • HY-18610R
    Diclofensine hydrochloride (Standard)
    		Inhibitor
    Diclofensine (Ro 8-4650) hydrochloride (Standard) is the analytical standard of Diclofensine hydrochloride. This product is intended for research and analytical applications. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.
  • HY-100665S
    Dehydroaripiprazole-d8
    		Agonist
    Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole.