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

5-HT2 Receptor Inhibitors

5-HT1 Receptor

5-HT2 Receptor

5-HT3 Receptor

5-HT5 Receptor

5-HT6 Receptor

5-HT7 Receptor

5-HT Receptor

5-HT4 Receptor

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Sorry. There is currently no product that acts on isoform 5-HT2 Receptor together.

Please try each isoform separately.

5-HT2 Receptor Specific Inhibitors, Agonists, Antagonists & Modulators
Product Name 5-HT2 Receptor 5-HT1 Receptor 5-HT3 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT4 Receptor 5-HT2 Receptor Selectivity Purity
Chlorpromazine hydrochloride
5-HT2A Receptor, Ki: 8.9 nM
            Selective Antagonist 99.90%
SCH-23390 hydrochloride
5-HT2C Receptor, Ki: 9.3 nM
            Selective Agonist 99.31%
Harmine
5-HT2A Receptor, Ki: 397 nM
            Selective Inhibitor 99.78%
Risperidone
5-HT2A Receptor, Ki: 4.8 nM
            Selective Inhibitor 99.16%
Pimavanserin
5-HT2A Receptor, pIC50: 8.7
            Selective Inhibitor 99.99%
Asenapine maleate
5-HT2A Receptor, Ki: 0.06 nM
5-HT2C Receptor, Ki: 0.03 nM
       
5-HT7 Receptor, Ki: 0.13 nM
  Selective Antagonist 99.95%
Puerarin
5-HT2C Receptor
            Selective Antagonist 99.20%
Volinanserin
5-HT2 Receptor, Ki: 0.36 nM
            Selective Antagonist 99.71%
Perphenazine
5-HT2A Receptor, Ki: 5.6 nM
            Selective Inhibitor 99.90%
Pimavanserin tartrate
5-HT2A Receptor, pIC50: 8.73
5-HT2A Receptor, pKi: 9.3
            Selective Inhibitor 99.50%
Agomelatine
5-HT2C Receptor, pKi: 6.4 (native porcine)
5-HT2C Receptor, pKi: 6.2 (human)
            Selective Antagonist 99.88%
Pizotifen
5-HT2A Receptor
            Selective Antagonist 99.65%
Trimipramine maleate
5-HT2 Receptor, pKi: 8.10
            Selective Antagonist 99.84%
Vabicaserin hydrochloride
5-HT2C Receptor, EC50: 8 nM
            Selective Agonist 98.99%
Cyproheptadine hydrochloride
5-HT2 Receptor, IC50: 0.6 nM
            Selective Antagonist 98.96%
Ritanserin
5-HT2 Receptor, IC50: 0.9 nM
            Selective Antagonist >99.0%
Blonanserin
5-HT2 Receptor
            Selective Antagonist 99.77%
Cinanserin hydrochloride
5-HT2 Receptor, Ki: 41 nM
            Selective Antagonist 99.74%
Asenapine hydrochloride
5-HT2A Receptor, Ki: 0.06 nM
5-HT2C Receptor, Ki: 0.03 nM
       
5-HT7 Receptor, Ki: 0.13 nM
  Selective Antagonist 99.39%
Lidanserin
5-HT2A Receptor
            Selective Antagonist >98.0%
Roluperidone
5-HT2A Receptor, Ki: 7.53 nM
            Selective 98.08%
Agomelatine hydrochloride
5-HT2C Receptor, pKi: 6.4 (native porcine)
5-HT2C Receptor, pKi: 6.2 (human)
            Selective Antagonist 99.49%
Nelotanserin
5-HT2A Receptor, IC50: 1.7 nM
5-HT2C Receptor, IC50: 79 nM
5-HT2B Receptor, IC50: 791 nM
            Selective Antagonist 99.79%
Pimethixene maleate
5-HT2A Receptor, pKi: 10.22
5-HT2B Receptor, pKi: 10.44
5-HT2C Receptor, pKi: 8.42
5-HT1A Receptor, pKi: 7.63
          Selective Antagonist >98.0%
Cyproheptadine hydrochloride sesquihydrate
5-HT2 Receptor
            Selective Antagonist 99.20%
PRX-08066
5-HT2B Receptor, IC50: 3.4 nM
            Selective Antagonist 97.04%
Naftidrofuryl oxalate
5-HT2 Receptor
            Selective Antagonist 95.81%
Isocorynoxeine
5-HT2A Receptor, IC50: 72.4 μM
            Selective Inhibitor 99.97%
Risperidone hydrochloride
5-HT2 Receptor, Ki: 4.8 nM
            Selective Antagonist
Pimethixene
5-HT2A Receptor, pKi: 10.22
5-HT2B Receptor, pKi: 10.44
5-HT2C Receptor, pKi: 8.42
5-HT1A Receptor, pKi: 7.63
          Selective Antagonist
WAY 163909
5-HT2C Receptor, Ki: 10.5±1.1 nM
            Selective Agonist
Blonanserin D5
5-HT2 Receptor
            Selective Antagonist
cis-Urocanic acid
5-HT2A Receptor
            Selective Agonist 99.92%
SB-215505
5-HT2B Receptor, pKi: 8.3
5-HT2A Receptor, pKi: 6.77
5-HT2C Receptor, pKi: 7.66
            Selective Antagonist
3-Hydroxy agomelatine
5-HT2C Receptor, IC50: 3.2 μM
5-HT2C Receptor, Ki: 1.8 μM
            Selective Antagonist
Blonanserin D8
5-HT2 Receptor
            Selective Antagonist
SCH-23390 maleate
5-HT2C Receptor, Ki: 9.3 nM
            Selective Agonist
7-Desmethyl-3-hydroxyagomelatine
5-HT2C Receptor
            Selective Antagonist
Flumexadol
5-HT2C Receptor, Ki: 25 nM
            Selective Agonist 98.50%
Iferanserin
5-HT2A Receptor
            Selective Antagonist
3-Hydroxy agomelatine D3
5-HT2C Receptor, IC50: 3.2 μM
5-HT2C Receptor, Ki: 1.8 μM
            Selective Antagonist
Eplivanserin (mixture)
5-HT2A Receptor
            Selective Antagonist 99.95%
Org-12962
5-HT2C Receptor, pEC50: 7.01
5-HT2A Receptor, pEC50: 6.38
5-HT2B Receptor, pEC50: 6.28
            Selective Agonist >98.0%
Fananserin
5-HT2 Receptor, Ki: 0.37 nM
            Selective Antagonist 99.71%
(Rac)-WAY-161503
5-HT2C Receptor, Ki: 4 nM
5-HT2C Receptor, EC50: 12 nM
            Selective Agonist >99.0%
Clocapramine hydrochloride hydrate
5-HT2A Receptor
            Selective Antagonist
Opiranserin
5-HT2A Receptor, IC50: 1.3 μM
            Selective Antagonist
YM348
5-HT2A Receptor, Ki: 13 nM
5-HT2B Receptor, Ki: 2.5 nM
5-HT2C Receptor, Ki: 0.89 nM
5-HT2A Receptor, EC50: 93 nM
5-HT2B Receptor, EC50: 3.2 nM
5-HT2C Receptor, EC50: 1 nM
            Selective Agonist
(R)-Praziquantel D11
5-HT2B Receptor
            Selective Agonist
Harmine hydrochloride
5-HT2A Receptor, Ki: 397 nM
            Selective Inhibitor
Risperidone mesylate
5-HT2A Receptor, Ki: 4.8 nM
            Selective Inhibitor
Agomelatine (L(+)-Tartaric acid)
5-HT2C Receptor, pKi: 6.4 (native porcine)
5-HT2C Receptor, pKi: 6.2 (human)
            Selective Antagonist 99.82%
Pizotifen malate
5-HT2A Receptor
            Selective Antagonist
Clocapramine
5-HT2A Receptor
            Selective Antagonist
(4E)-SUN9221
5-HT2 Receptor
            Selective Antagonist
5-HT2 antagonist 1
5-HT2 Receptor
            Selective Antagonist
5-HT2A antagonist 1
5-HT2A Receptor
            Selective Antagonist
Perospirone
5-HT2A Receptor, Ki: 0.6 nM
5-HT1A Receptor, Ki: 2.9 nM
5-HT1 Receptor, Ki: 18 nM
          Pan Modulator 99.51%
Sertindole
5-HT2A Receptor
5-HT2C Receptor
            Pan Antagonist 99.76%
Olanzapine
5-HT2A Receptor, Ki: 4 nM
5-HT2C Receptor, Ki: 11 nM
5-HT1 Receptor, Ki: 7 nM
5-HT3 Receptor, Ki: 57 nM
 
5-HT6 Receptor, Ki: 5 nM
    Pan Antagonist 99.94%
Brexpiprazole
5-HT2A Receptor, Ki: 0.47 nM
5-HT1A Receptor, Ki: 0.12 nM
          Pan Modulator 99.40%
Lumateperone tosylate
5-HT2A Receptor, Ki: 0.54 nM
            Pan Antagonist 99.21%
Quetiapine
5-HT2A Receptor, pKi: 7.54
5-HT2C Receptor, pKi: 5.55
5-HT1A Receptor, pKi: 5.74
5-HT1A Receptor, pEC50: 4.77
          Pan Agonist 99.97%
Methiothepin mesylate
5-HT2A Receptor, pKi: 8.50
5-HT2B Receptor, pKi: 8.68
5-HT2C Receptor, pKi: 8.35
5-HT1A Receptor, pKd: 7.10
5-HT1B Receptor, pKd: 7.28
5-HT1C Receptor, pKd: 7.56
5-HT1D Receptor, pKd: 6.99
 
5-HT5A Receptor, pKd: 7.0
5-HT5B Receptor, pKd: 7.8
5-HT6 Receptor, pKd: 8.74
5-HT7 Receptor, pKd: 8.99
  Pan Antagonist 99.32%
Flibanserin
5-HT2A Receptor, Ki: 49 nM
5-HT1A Receptor, Ki: 1 nM
          Pan Modulator 99.31%
Mirtazapine
5-HT2 Receptor
 
5-HT3 Receptor
        Pan Antagonist 99.77%
RS 127445
5-HT2A Receptor, pKi: 6.3
5-HT2C Receptor, pKi: 6.4
5-HT2B Receptor, pKi: 9.5
 
5-HT3 Receptor, pKi: <6
5-HT5 Receptor, pKi: <6
5-HT6 Receptor, pKi: <6
    Pan Antagonist 99.68%
Nuciferine
5-HT2C Receptor, IC50: 131 nM
5-HT2A Receptor, IC50: 478 nM
5-HT2B Receptor, IC50: 1 μM
5-HT1A Receptor, EC50: 3.2 μM
   
5-HT6 Receptor, EC50: 700 nM
5-HT7 Receptor, IC50: 150 nM
  Pan Modulator 99.66%
Temanogrel
5-HT2A Receptor, Ki: 4.9 nM
            Pan Antagonist 98.94%
Sarpogrelate hydrochloride
5-HT2 Receptor
            Pan Antagonist >98.0%
Eltoprazine hydrochloride
5-HT2C Receptor
5-HT1A Receptor
5-HT1B Receptor
          Pan Modulator 99.35%
Setiptiline
5-HT2A Receptor
5-HT2C Receptor
 
5-HT3 Receptor
        Pan Modulator 96.54%
Pipamperone
5-HT2A Receptor, pKi: 8.2
5-HT2C Receptor, pKi: 6.9
5-HT1 Receptor, pKi: 5.7
          Pan Antagonist 99.89%
Asenapine
5-HT2A Receptor, pKi: 10.2
5-HT2B Receptor, pKi: 9.8
5-HT2C Receptor, pKi: 10.5
5-HT1A Receptor, pKi: 8.6
5-HT1B Receptor, pKi: 8.4
 
5-HT5 Receptor, pKi: 8.8
5-HT6 Receptor, pKi: 9.6
5-HT7 Receptor, pKi: 9.9
  Pan Antagonist 98.81%
BRL 54443
5-HT2A Receptor, Ki: 1259 nM
5-HT2B Receptor, Ki: 100 nM
5-HT2C Receptor, Ki: 316 nM
5-HT1E Receptor, Ki: 1.1 nM
5-HT1F Receptor, Ki: 0.7 nM
5-HT1A Receptor, Ki: 63 nM
5-HT1B Receptor, Ki: 126 nM
5-HT1D Receptor, Ki: 63 nM
   
5-HT6 Receptor, Ki: >10,000 nM
5-HT7 Receptor, Ki: >10,000 nM
  Pan Agonist 99.39%
Ocaperidone
5-HT2 Receptor, Ki: 0.14 nM
5-HT1A Receptor, pEC50: 7.6 (h5-HT1A)
5-HT1A Receptor, pKi: 8.08 (h5-HT1A)
          Pan Modulator 98.55%
SB-200646A
5-HT2B Receptor, pKi: 7.5
5-HT2C Receptor, pKi: 6.9
5-HT2A Receptor, pKi: 5.2
            Pan Antagonist 99.47%
Arotinolol
5-HT2A Receptor
            Pan Antagonist 98.18%
(Rac)-Rotigotine hydrochloride
5-HT2B Receptor, Ki: 27 nM
5-HT1A Receptor, Ki: 30 nM
          Pan Agonist 97.76%
Quetiapine hemifumarate
5-HT2A Receptor, pKi: 7.54
5-HT2C Receptor, pKi: 5.55
5-HT1A Receptor, pKi: 5.74
5-HT1A Receptor, pEC50: 4.77
          Pan Agonist 98.24%
Iloperidone
Rat 5-HT2 Receptor, Ki: 3.1 nM
Human 5-HT2A Receptor, Ki: 5.6 nM
Human 5-HT2C Receptor, Ki: 42.8 nM
Rat 5-HT1A, Ki: 168 nM
   
Rat 5-HT6 Receptor, Ki: 42.7 μM
Rat 5-HT7 Receptor, Ki: 21.6 nM
  Pan Antagonist 99.64%
SEP-363856 hydrochloride
5-HT2A Receptor, EC50: >10 μM
5-HT2C Receptor, EC50: 30 μM
5-HT1A Receptor, EC50: 2.3 μM
5-HT1B Receptor, EC50: 15.6 μM
5-HT1D Receptor, EC50: 0.262 μM
     
5-HT7 Receptor, EC50: 6.7 μM
  Pan Agonist 99.78%
SB 243213 dihydrochloride
5-HT2C Receptor, pKi: 9.37
            Pan Antagonist >99.0%
SB 243213 hydrochloride
5-HT2C Receptor, pKi: 9.37
            Pan Antagonist
Eltoprazine
5-HT2C Receptor
5-HT1A Receptor
5-HT1B Receptor
          Pan Modulator >95.0%
5-HT6/7 antagonist 1
5-HT2A Receptor
     
5-HT6 Receptor
5-HT7 Receptor
  Pan Antagonist
Tedatioxetine hydrobromide
5-HT2A Receptor
5-HT2C Receptor
 
5-HT3 Receptor
        Pan Antagonist 98.44%
SEP-363856
5-HT2A Receptor, EC50: >10 μM
5-HT2C Receptor, EC50: 30 μM
5-HT1A Receptor, EC50: 2.3 μM
5-HT1B Receptor, EC50: 15.6 μM
5-HT1D Receptor, EC50: 0.262 μM
     
5-HT7 Receptor, EC50: 6.7 μM
  Pan Agonist
PRX933 hydrochloride
5-HT2C Receptor
            Pan Agonist
Mirtazapine D3
5-HT2 Receptor
 
5-HT3 Receptor
        Pan Inhibitor
Isopteropodine
5-HT2 Receptor
            Pan Agonist
Brexpiprazole S-oxide D8
5-HT2A Receptor, Ki: 0.47 nM
5-HT1A Receptor, Ki: 0.12 nM
          Pan Modulator
Cyamemazine
5-HT2A Receptor, Ki: 1.5 nM
5-HT2C Receptor, Ki: 12 nM
 
5-HT3 Receptor, Ki: 75 nM
        Pan Antagonist >99.0%
PRX-07034 hydrochloride
5-HT2A Receptor, IC50: 2.5 μM
5-HT2B Receptor, IC50: 2.5 μM
5-HT2C Receptor, IC50: 3.7 μM
5-HT1A Receptor, Ki: 420 nM
5-HT1B Receptor, Ki: 260 nM
5-HT1D Receptor, Ki: 2.8 μM
   
5-HT6 Receptor, Ki: 4-8 nM
5-HT6 Receptor, IC50: 19 nM
    Pan Antagonist
5-HT1A modulator 1
5-HT2A Receptor, IC50: 500 nM
5-HT2C Receptor, IC50: 4000 nM
            Pan Modulator
Piromelatine
5-HT2B Receptor (Antagonist)
5-HT1A Receptor (Agonist)
5-HT1D Receptor (Agonist)
          Pan Modulator 99.21%
Eplivanserin
5-HT2 Receptor, IC50: 5.8 nM (in rat cortical membrane)
5-HT2 Receptor, Ki: 1.14 nM
            Pan Antagonist
ST1936 oxalate
5-HT2B Receptor, Ki: 245 nM
     
5-HT6 Receptor, Ki: 13 nM
Human 5-HT7 Receptor , Ki: 168 nM
  Pan Agonist
AR-A 2
5-HT2A Receptor, Ki: 339 nM
5-HT1A Receptor, Ki: 3070 nM
5-HT1B/D Receptor, Ki: 20 nM
          Pan Antagonist
TIK-301
5-HT2C Receptor
5-HT2B Receptor
            Pan Antagonist
SB228357
5-HT2A Receptor, pKi: 6.9
5-HT2C Receptor, pKi: 9
5-HT2B Receptor, pKi: 8
            Pan Antagonist >99.0%
Brilaroxazine
5-HT2A Receptor, Ki: 2.5 nM
5-HT2B Receptor, Ki: 0.19 nM
5-HT1A Receptor, Ki: 1.5 nM
     
5-HT7 Receptor, Ki: 2.7 nM
  Pan Modulator
GR 113808
5-HT2A Receptor
5-HT2C Receptor
5-HT1A Receptor
5-HT3 Receptor
     
5-HT4 Receptor
Pan Antagonist
Sarizotan
5-HT2A Receptor, IC50: 960 nM (rat, agonist site)
5-HT2A Receptor, IC50: 587 nM (human, antagonist site)
5-HT2C Receptor, IC50: 800 nM (pig)
5-HT2B Receptor, IC50: 108 nM (human)
5-HT1D Receptor, IC50: 500 nM (calf)
5-HT1A Receptor, IC50: 6.5 nM (rat)
5-HT1A Receptor, IC50: 0.1 nM (human)
5-HT1B Receptor, IC50: 600 nM (rat)
5-HT3 Receptor, IC50: 3500 nM (NG 108 cells)
5-HT5A Receptor, IC50: 313 nM (human)
5-HT6 Receptor, IC50: 3300 nM (human)
5-HT7 Receptor, IC50: 10 nM (human)
  Pan Agonist
(S)-Mirtazapine
5-HT2 Receptor
 
5-HT3 Receptor
        Pan Antagonist
SB-200646
5-HT2B Receptor, pKi: 7.5
5-HT2C Receptor, pKi: 6.9
5-HT2A Receptor, pKi: 5.2
            Pan Antagonist
cis-(Z)-Flupentixol dihydrochloride
5-HT2A Receptor, Ki: 7 nM
            Pan Antagonist
Brexpiprazole S-oxide
5-HT2A Receptor, Ki: 0.47 nM
5-HT1A Receptor, Ki: 0.12 nM
          Pan Modulator
Iloperidone hydrochloride
Rat 5-HT2 Receptor, Ki: 3.1 nM
Human 5-HT2A Receptor, Ki: 5.6 nM
Human 5-HT2C Receptor, Ki: 42.8 nM
Rat 5-HT1A, Ki: 168 nM
   
Rat 5-HT6 Receptor, Ki: 42.7 nM
Rat 5-HT7 Receptor, Ki: 21.6 nM
  Pan Antagonist
Nexopamil racemate
5-HT2 Receptor
            Pan
Deramciclane
5-HT2A Receptor
5-HT2C Receptor
            Pan Antagonist
Irindalone
5-HT2 Receptor
            Pan Antagonist
Wf-516
5-HT2A Receptor, Ki: 40 nM
5-HT1A Receptor, Ki: 5 nM
          Pan Antagonist
CP-809101
5-HT2C Receptor, pEC50: 9.96
5-HT2B Receptor, pEC50: 7.19
5-HT2A Receptor, pEC50: 6.81
            Pan Agonist
Paliperidone
5-HT2A Receptor
            default Antagonist 99.87%
Paliperidone palmitate
5-HT2A Receptor
            default Antagonist