1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT2 Receptor Isoform
  5. 5-HT2 Receptor Inhibitor

5-HT2 Receptor Inhibitor

5-HT2 Receptor Inhibitors (33):

Cat. No. Product Name Effect Purity
  • HY-N0737A
    Harmine
    Inhibitor 99.97%
    Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
  • HY-11018
    Risperidone
    Inhibitor 99.87%
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-14557
    Pimavanserin
    Inhibitor 99.86%
    Pimavanserin is a selective, brain-penetrant, inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
  • HY-119209
    Nefazodone
    Inhibitor 98.01%
    Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction.
  • HY-N0737
    Harmine hydrochloride
    Inhibitor 99.98%
    Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
  • HY-125784
    Viloxazine hydrochloride
    Inhibitor 98.94%
    Viloxazine hydrochloride 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-124591
    TC-2153
    Inhibitor 98.19%
    TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and 5-HT1A receptors mRNA level in midbrain. TC-2153 also inhibits 5-HT2A receptor-mediated signaling.
  • HY-W050162
    (E)-3,4,5-Trimethoxycinnamic acid
    Inhibitor 99.90%
    (E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.
  • HY-N0775
    Isocorynoxeine
    Inhibitor 99.52%
    Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
  • HY-103094
    LY266097 hydrochloride
    Inhibitor 98.41%
    LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression.
  • HY-N0737AR
    Harmine (Standard)
    Inhibitor
    Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
  • HY-110232
    Risperidone-d4
    Inhibitor 99.34%
    Risperidone-d4 is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-14557R
    Pimavanserin (Standard)
    Inhibitor
    Pimavanserin (Standard) is the analytical standard of Pimavanserin. This product is intended for research and analytical applications. Pimavanserin is a selective and brain-penetrant inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
  • HY-11018S2
    Risperidone-d6
    Inhibitor
    Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-181977
    RPI-GLYT2-82
    Inhibitor
    RPI-GLYT2-82 is a reversible, blood-brain barrier-permeable allosteric inhibitor of GlyT2 with an IC50 value of 554 nM. RPI-GLYT2-82 also exhibits inhibitory activity against 5-HT2AR and SERT, with IC50 values of 1.9 μM and 4.7 μM, respectively. RPI-GLYT2-82 inhibits pain signals and alleviates allodynia, shows no target-related side effects at the maximum analgesic dose, and has no addictive potential. RPI-GLYT2-82 can be used for the research of neuropathic pain.
  • HY-172258
    5-HT2B antagonist-2
    Inhibitor
    5-HT2B antagonist-2 (Compound 19c) is a 5HT2B receptor antagonist with an IC50 of 1.09 nM. 5-HT2B antagonist-2 can downregulate the expression of fibrosis-related genes α-SMA, Timp1, Col1a1, and Col3a1, and significantly reduce the deposition of fibrosis, thereby reducing the fibrotic area and inhibiting the fibrotic process in CCl4-induced liver fibrosis mouse models. 5-HT2B antagonist-2 can be used in the study of immune inflammatory-related diseases, particularly in the research of pulmonary fibrosis diseases.
  • HY-175822
    5-HT2A inverse agonist-1
    Inhibitor
    5-HT2A inverse agonist-1 is a 5-HT2A receptor inverse agonist with a IC50 of 5.5 nM. 5-HT2A inverse agonist-1 shows minimal hERG inhibition. 5-HT2A inverse agonist-1 can be used for the research of neurological disease, such as Parkinson’s disease.
  • HY-N0775R
    Isocorynoxeine (Standard)
    Inhibitor
    Isocorynoxeine (Standard) is the analytical standard of Isocorynoxeine. This product is intended for research and analytical applications. Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
  • HY-175285
    5-HT2AR-IN-1
    Inhibitor
    5-HT2AR-IN-1 (Compound Ie) is an orally active 5-hydroxytryptamine 2A receptor (5-HT2AR) inhibitor with antidepressant efficacy. 5-HT2AR-IN-1 reduces 5-HT2AR expression and SERT protein levels. 5-HT2AR-IN-1 is promising for research of central nervous system (CNS), such as depression and addiction-related disorders.
  • HY-180584
    5-HT2A agonist 9
    Inhibitor
    5-HT2A agonist 9 (Compound I-53) is a 5-HT2A agonist with an EC₅₀ of 34 nM. 5-HT2A agonist 9 can be used for the study of mental disorders and central system disorders.