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

5-HT Receptor Antagonist

5-HT Receptor Isoform Comparison

5-HT Receptor Antagonists (612):

Cat. No. Product Name Effect Purity
  • HY-B1213AR
    Trimipramine (Standard)
    		Antagonist
    Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy.
  • HY-10121S2
    Asenapine-13C,d3
    		Antagonist
    Asenapine-13C,d3 is 13C and deuterated labeled Asenapine (HY-10121). Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
  • HY-117799A
    LY-426965 hydrochloride
    		Antagonist
    LY-426965 hydrochloride is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders.
  • HY-15472A
    PRX-08066 maleate
    		Antagonist
    PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
  • HY-111491
    Methiothepin
    		Antagonist
    Methiothepin (Metitepine; Ro 8-6837) 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-103146
    GR125487 sulfamate
    		Antagonist
    GR125487 sulfamate is an orally active and selective antagonist of 5-HT4R. GR125487 sulfamate effectively blocks the cognition enhancing effect. GR125487 sulfamate can be used to study memory disorders, gastrointestinal disorders, mood disorders and urinary tract dysfunction.
  • HY-101105
    SB-224289
    		Antagonist
    SB-224289 is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
  • HY-107125A
    AVN-322 free base
    		Antagonist
    AVN-322 free base is an orally active, highly selective 5-HT6Rantagonist for central nervous system disease research.
  • HY-118836
    GSK215083
    		Antagonist
    GSK215083 is a high affinity 5-HT6 receptor antagonist. GSK215083 can serves as a promising 5-HT6 radioligand candidate by radiolabeled with (11)C via methylation.
  • HY-105449A
    KB R6933
    		Antagonist
    KB R6933 is a potent, selective and orally active 5-HT3 receptor antagonist. KB R6933 can inhibit the diarrhea induced by 5-HT (HY-B1473A), but not that by Castor Oil (HY-107799) or prostaglandin E2 (PGE2) (HY-101952). KB R6933 can inhibit 5-HT-induced bradycardia.
  • HY-19417
    Wf-516 hydrochloride
    		Antagonist
    Wf-516 hydrochloride is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively.Wf-516 hydrochloride has potent antidepressant activity.
  • HY-171235
    5-HT2A antagonist 3
    		Antagonist
    5-HT2A antagonist 3 (Formula (III)) is a 5-HT2A receptor antagonist and inverse agonist with a pIC50 of 8.7 and a pKi of 9. 5-HT2A antagonist 3 can be utilized in neurological reesearch.
  • HY-103115
    Pruvanserin hydrochloride
    		Antagonist
    Pruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT2A receptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2A receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia.
  • HY-19297
    SB-247853
    		Antagonist
    SB-247853 is a highly specific 5-HT2c receptor antagonist. SB-247853 induces orthostatic intolerance during head-up tilting. SB-247853 can be used in the research of cardiovascular diseases.
  • HY-172678
    PUC-10
    		Antagonist
    PUC-10 is a 5-HT6 receptor antagonist with a Ki of 14.6 nM and an IC50 of 32 nM. In silico predictions suggest that PUC-10 is orally active and can cross the blood-brain barrier. PUC-10 can induce autophagy in SH-SY5Y cells by inhibiting the mTOR pathway. PUC-10 can be used in the research of neurological disorders.
  • HY-106904
    Nexopamil
    		Antagonist
    Nexopamil is a calcium antagonist of Ca2+ channel, 5HT2, 5HT1A, 5HT1C and dopamine D2 receptors. Nexopamil exhibits vasodilatory, cardioprotective, and platelet aggregation inhibiting effects. Nexopamil can be used for researches of stable or unstable angina and possibly of peripheral arterial occlusive disease.
  • HY-106418A
    SGB-1534 hydrochloride
    		Antagonist
    SGB-1534 (hydrochloride) is an orally active, selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. SGB-1534 (hydrochloride) can inhibit vasoconstriction and lower blood pressure. SGB-1534 (hydrochloride) can be used for the research of cardiovascular disease, such as hypertension.
  • HY-136678
    SB 258741
    		Antagonist
    SB 258741 is an efficient and highly selective 5-HT7 receptor (pKi = 8.
  • HY-146077
    5-HT6/5-HT2A receptor ligand-2
    		Antagonist
    5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties.
  • HY-106605S
    Flumezapine-d8 hydrochloride
    		Antagonist
    Flumezapine-d8 (LY 120363-d8) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.