1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT6 Receptor Inhibitors

5-HT6 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-HT6 Receptor together.

Please try each isoform separately.

5-HT6 Receptor Specific Agonists, Antagonists & Modulators
Product Name 5-HT6 Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT5 Receptor 5-HT7 Receptor 5-HT4 Receptor 5-HT6 Receptor Selectivity Purity
WAY-181187
5-HT6 Receptor, Ki: 2.2 nM
5-HT6 Receptor, EC50: 6.6 nM
            Selective Agonist 98.05%
Idalopirdine Hydrochloride
5-HT6 Receptor, Ki: 0.83 nM
            Selective Antagonist 99.83%
Intepirdine
5-HT6 Receptor, pKi: 9.63
            Selective Antagonist 98.92%
SB 271046 Hydrochloride
5-HT6 Receptor, pKi: 8.92-9.02
5-HT1D Receptor, pKi: 6.55
5-HT1A Receptor, pKi: 6.35
5-HT1B Receptor, pKi: 6.05
5-HT1F Receptor, pKi: 5.95
5-HT1E Receptor, pKi: <4.99
5-HT2A Receptor, pKi: 5.62
5-HT2B Receptor, pKi: 5.41
Human 5-HT2C Receptor, pKi: 5.73
   
5-HT7 Receptor, pKi: 5.39
5-HT4 Receptor, pKi: 5.27
Selective Antagonist 98.64%
NPS ALX Compound 4a
5-HT6 Receptor, IC50: 7.2 nM
5-HT6 Receptor, Ki: 0.2 nM
            Selective Antagonist ≥99.0%
Masupirdine mesylate
5-HT6 Receptor, Ki: 2.04 nM
            Selective Antagonist
PRX-07034 hydrochloride
5-HT6 Receptor, Ki: 4-8 nM
5-HT6 Receptor, IC50: 19 nM
5-HT1A Receptor, Ki: 420 nM
5-HT1B Receptor, Ki: 260 nM
5-HT1D Receptor, Ki: 2.8 μM
5-HT2A Receptor, IC50: 2.5 μM
5-HT2B Receptor, IC50: 2.5 μM
5-HT2C Receptor, IC50: 3.7 μM
        Selective Antagonist
ST1936 oxalate
5-HT6 Receptor, Ki: 13 nM
 
5-HT2B Receptor, Ki: 245 nM
   
Human 5-HT7 Receptor , Ki: 168 nM
  Selective Agonist
EMDT oxalate
5-HT6 Receptor
            Selective Agonist
SGS518 oxalate
5-HT6 Receptor
            Selective Antagonist
NPS ALX Compound 4a dihydrochloride
5-HT6 Receptor, IC50: 7.2 nM
5-HT6 Receptor, Ki: 0.2 nM
            Selective Antagonist
Masupirdine free base
5-HT6 Receptor, Ki: 2.04 nM
            Selective Antagonist
Idalopirdine
5-HT6 Receptor, Ki: 0.83 nM
            Selective Antagonist
5HT6-ligand-1
5-HT6 Receptor, Ki: 1.43 nM
            Selective
Olanzapine
5-HT6 Receptor, Ki: 5 nM
5-HT1 Receptor, Ki: 7 nM
5-HT2A Receptor, Ki: 4 nM
5-HT2C Receptor, Ki: 11 nM
5-HT3 Receptor, Ki: 57 nM
      Pan Antagonist 99.89%
AVN-492
5-HT6 Receptor, Ki: 91 pM
            Pan Antagonist 99.49%
Methiothepin mesylate
5-HT6 Receptor, pKd: 8.74
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-HT2A Receptor, pKi: 8.50
5-HT2B Receptor, pKi: 8.68
5-HT2C Receptor, pKi: 8.35
 
5-HT5A Receptor, pKd: 7.0
5-HT5B Receptor, pKd: 7.8
5-HT7 Receptor, pKd: 8.99
  Pan Antagonist ≥98.0%
Iloperidone
Rat 5-HT6 Receptor, Ki: 42.7 μM
Rat 5-HT1A Receptor, Ki: 168 nM
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-HT7 Receptor, Ki: 21.6 nM
  Pan Antagonist 99.64%
Asenapine
5-HT6 Receptor, pKi: 9.6
5-HT1A Receptor, pKi: 8.6
5-HT1B Receptor, pKi: 8.4
5-HT2A Receptor, pKi: 10.2
5-HT2C Receptor, pKi: 10.5
5-HT2B Receptor, pKi: 9.8
 
5-HT5 Receptor, pKi: 8.8
5-HT7 Receptor, pKi: 9.9
  Pan Antagonist 98.81%
Blonanserin
5-HT6 Receptor, Ki: 11.7 nM
 
5-HT2A Receptor, Ki: 0.812 nM
5-HT2C Receptor, Ki: 26.4 nM
        Pan Antagonist 99.77%
BRL 54443
5-HT6 Receptor, Ki: >10,000 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-HT2A Receptor, Ki: 1259 nM
5-HT2B Receptor, Ki: 100 nM
5-HT2C Receptor, Ki: 316 nM
   
5-HT7 Receptor, Ki: >10,000 nM
  Pan Agonist 99.39%
Nuciferine
5-HT6 Receptor, EC50: 700 nM
5-HT1A Receptor, EC50: 3.2 μM
5-HT2C Receptor, IC50: 131 nM
5-HT2A Receptor, IC50: 478 nM
5-HT2B Receptor, IC50: 1 μM
   
5-HT7 Receptor, IC50: 150 nM
  Pan Modulator 99.66%
RS-127445 hydrochloride
5-HT6 Receptor, pKi: <6
 
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
    Pan Antagonist 99.68%
GSK163090
Human 5-HT6 Receptor, pKi: <5.3
5-HT1A Receptor, pKi: 9.4
5-HT1B Receptor, pKi: 8.5
5-HT1D Receptor, pKi: 9.7
5-HT2A Receptor, pKi: 6
5-HT2B Receptor, pKi: 6.3
5-HT2C Receptor, pKi: 5.8
   
Human 5-HT7 Receptor , pKi: 6.8
  Pan Antagonist 99.95%
SB-399885 hydrochloride
5-HT6 Receptor
            Pan Antagonist 99.54%
SB 243213 dihydrochloride
Human 5-HT6 Receptor, pKi: 6.5
human 5-HT1A Receptor, pKi: <5.3
human 5-HT1B Receptor, pKi: 5.5
human 5-HT1D Receptor, pKi: 6.32
human 5-HT1E Receptor, pKi: <5.4
human 5-HT1F Receptor, pKi: 5.35
Human 5-HT2C Receptor, pKi: 9.37
Human 5-HT2A Receptor, pKi: 7.01
human 5-HT2B Receptor, pKi: 7.2
   
Human 5-HT7 Receptor , pKi: 5.64
  Pan Antagonist ≥99.0%
SB 243213 hydrochloride
Human 5-HT6 Receptor, pKi: 6.5
human 5-HT1A Receptor, pKi: <5.3
human 5-HT1B Receptor, pKi: 5.5
human 5-HT1D Receptor, pKi: 6.32
human 5-HT1E Receptor, pKi: <5.4
human 5-HT1F Receptor, pKi: 5.35
Human 5-HT2C Receptor, pKi: 9.37
Human 5-HT2A Receptor, pKi: 7.01
human 5-HT2B Receptor, pKi: 7.2
   
Human 5-HT7 Receptor , pKi: 5.64
  Pan Antagonist
5-HT6/7 antagonist 1
5-HT6 Receptor
 
5-HT2A Receptor
   
5-HT7 Receptor
  Pan Antagonist
SB 243213
Human 5-HT6 Receptor, pKi: 6.5
human 5-HT1A Receptor, pKi: <5.3
human 5-HT1B Receptor, pKi: 5.5
human 5-HT1D Receptor, pKi: 6.32
human 5-HT1E Receptor, pKi: <5.4
human 5-HT1F Receptor, pKi: 5.35
Human 5-HT2C Receptor, pKi: 9.37
Human 5-HT2A Receptor, pKi: 7.01
human 5-HT2B Receptor, pKi: 7.2
   
Human 5-HT7 Receptor , pKi: 5.64
  Pan Antagonist 98.62%
Ro 04-6790
Rat 5-HT6 Receptor, pKi: 7.26
Human 5-HT6 Receptor, pKi: 7.35
            Pan Antagonist
BGC20-761
Human 5-HT6 Receptor, Ki: 20 nM
 
Human 5-HT2A Receptor, Ki: 69 nM
        Pan Antagonist
Sarizotan
5-HT6 Receptor, IC50: 3300 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-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-HT3 Receptor, IC50: 3500 nM (NG 108 cells)
5-HT5A Receptor, IC50: 313 nM (human)
5-HT7 Receptor, IC50: 10 nM (human)
  Pan Agonist
Iloperidone hydrochloride
Rat 5-HT6 Receptor, Ki: 42.7 nM
Rat 5-HT1A Receptor, Ki: 168 nM
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-HT7 Receptor, Ki: 21.6 nM
  Pan Antagonist