1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor
  4. 5-HT1 Receptor Inhibitors

5-HT1 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-HT1 Receptor together.

Please try each isoform separately.

5-HT1 Receptor Specific Inhibitors, Agonists, Antagonists & Modulators
Product Name 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT4 Receptor 5-HT1 Receptor Selectivity Purity
Rizatriptan benzoate
5-HT1 Receptor
            Selective Agonist 99.96%
Pindolol
5-HT1A Receptor
            Selective Modulator 99.91%
Flibanserin
5-HT1A Receptor, Ki: 1 nM
5-HT2A Receptor, Ki: 49 nM
          Selective Modulator 99.31%
Vilazodone
5-HT1A Receptor
            Selective Agonist 99.91%
Tandospirone
5-HT1A Receptor, Ki: 27 nM
            Selective Agonist 96.81%
NAN-190 hydrobromide
5-HT1 Receptor
            Selective Antagonist 99.02%
Sumatriptan succinate
5-HT1D Receptor
            Selective Agonist 99.73%
Befiradol hydrochloride
5-HT1A Receptor
            Selective Agonist 99.22%
Rotundine
5-HT1A Receptor, IC50: 370 nM
            Selective Antagonist 99.88%
YL0919
5-HT1A Receptor
            Selective Agonist 99.77%
LY310762
5-HT1D Receptor, Ki: 249 nM
            Selective Antagonist 99.84%
Adoprazine
5-HT1A Receptor
            Selective Agonist 98.10%
Alverine citrate
5-HT1A Receptor, IC50: 101 nM
            Selective Antagonist 98.71%
LY 344864
5-HT1F Receptor, Ki: 6 nM
            Selective Agonist 99.16%
Donitriptan
5-HT1B Receptor, pKi: 9.4
5-HT1D Receptor, pKi: 9.3
            Selective Agonist
EMD 56551
5-HT1A Receptor
            Selective Agonist
Eptapirone
5-HT1A Receptor
            Selective Agonist 99.91%
Flesinoxan
5-HT1A Receptor, EC50: 24 nM
            Selective Agonist 99.07%
OPC-14523 free base
5-HT1A Receptor, IC50: 2.3 nM
            Selective Agonist
Frovatriptan succinate hydrate
5-HT1B Receptor, pKi: 8.6
5-HT1D Receptor, pKi: 8.4
       
Human 5-HT7 Receptor , pKi: 6.7
  Selective Agonist >99.0%
OPC-14523 hydrochloride
5-HT1A Receptor, IC50: 2.3 nM
            Selective Agonist 99.90%
Pardoprunox hydrochloride
5-HT1A Receptor, pEC50: 6.3
            Selective Agonist 98.24%
Naratriptan
5-HT1 Receptor
            Selective Agonist
SB-616234A
5-HT1B Receptor
            Selective Antagonist
F-15599
5-HT1A Receptor, Ki: 3.4 nM
            Selective Agonist 99.61%
BRL-15572 dihydrochloride
5-HT1D Receptor
            Selective Antagonist 99.78%
WAY-100635
5-HT1A Receptor, pIC50: 8.87
5-HT1A Receptor, pA2: 9.71
            Selective Antagonist
Cariprazine D6
5-HT1A Receptor, Ki: 2.6 nM
            Selective Modulator
Befiradol
5-HT1A Receptor
            Selective Agonist
Xaliproden hydrochloride
5-HT1A Receptor, IC50: 3 nM
            Selective Agonist
PNU-142633
5-HT1D Receptor, Ki: 6 nM
            Selective Agonist >98.0%
BRL-15572 hydrochloride
5-HT1D Receptor
            Selective Antagonist
8-Hydroxy-DPAT hydrobromide
5-HT1A Receptor, pIC50: 8.19
            Selective Agonist
Geissoschizine methyl ether
5-HT1A Receptor
            Selective Agonist
Urapidil
5-HT1A Receptor
            Selective Agonist 99.89%
Bifeprunox
5-HT1A Receptor, pKi: 7.19 (cortex)
5-HT1A Receptor, pEC50: 6.37 (hippocampus)
            Selective Agonist
Desmethyl cariprazine
5-HT1A Receptor, Ki: 2.6 nM
            Selective Modulator
Urapidil D6
5-HT1A Receptor
            Selective Agonist
Dehydroaripiprazole
5-HT1A Receptor, Ki: 4.2 nM
            Selective Agonist
p-MPPI hydrochloride
5-HT1A Receptor
            Selective Antagonist 99.19%
LY 344864 racemate
5-HT1F Receptor
            Selective Agonist 98.88%
Pardoprunox
5-HT1A Receptor, pEC50: 6.3
            Selective Agonist
Lesopitron dihydrochloride
5-HT1A Receptor, IC50: 125 nM (in rat hippocampal membranes)
            Selective Agonist
Naluzotan
5-HT1A Receptor, IC50: 20 nM
5-HT1A Receptor, Ki: 5.1 nM
            Selective Agonist
Urapidil hydrochloride
5-HT1A Receptor
            Selective Agonist >99.0%
Perospirone
5-HT1A Receptor, Ki: 2.9 nM
5-HT1 Receptor, Ki: 18 nM
5-HT2A Receptor, Ki: 0.6 nM
          Pan Modulator 99.51%
Aripiprazole
5-HT1A Receptor, Ki: 4.2 nM
            Pan Agonist 99.98%
Olanzapine
5-HT1 Receptor, Ki: 7 nM
5-HT2A Receptor, Ki: 4 nM
5-HT2C Receptor, Ki: 11 nM
5-HT3 Receptor, Ki: 57 nM
 
5-HT6 Receptor, Ki: 5 nM
    Pan Antagonist 99.94%
Brexpiprazole
5-HT1A Receptor, Ki: 0.12 nM
5-HT2A Receptor, Ki: 0.47 nM
          Pan Modulator 99.40%
RU 24969
5-HT1B Receptor, Ki: 0.38 nM
5-HT1A Receptor, Ki: 2.5 nM
            Pan Agonist 99.77%
Alprenolol hydrochloride
5-HT1A Receptor
            Pan Antagonist 99.58%
Lurasidone
5-HT1A Receptor, IC50: 6.75 nM
       
5-HT7 Receptor, IC50: 0.495 nM
  Pan Modulator 99.33%
SB-224289 hydrochloride
5-HT1B Receptor
            Pan Antagonist >98.0%
Cariprazine hydrochloride
5-HT1A Receptor, Ki: 2.6 nM
            Pan Modulator 99.89%
Quetiapine
5-HT1A Receptor, pKi: 5.74
5-HT1A Receptor, pEC50: 4.77
5-HT2A Receptor, pKi: 7.54
5-HT2C Receptor, pKi: 5.55
          Pan Agonist 99.97%
Alprenolol
5-HT1A Receptor
            Pan Antagonist 99.87%
Methiothepin mesylate
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-HT6 Receptor, pKd: 8.74
5-HT7 Receptor, pKd: 8.99
  Pan Antagonist 99.32%
8-OH-DPAT
5-HT1A Receptor, pIC50: 8.19
       
5-HT7 Receptor, Ki: 466 nM
  Pan Agonist >98.0%
Lurasidone Hydrochloride
5-HT1A Receptor, IC50: 6.75 nM
       
5-HT7 Receptor, IC50: 0.495 nM
  Pan Modulator 99.87%
Cariprazine
5-HT1A Receptor, Ki: 2.6 nM
            Pan Modulator 99.35%
Rotigotine
5-HT1A Receptor, Ki: 30 nM
       
5-HT7 Receptor, Ki: 86 nM
  Pan Agonist 99.98%
Eletriptan hydrobromide
5-HT1B Receptor, Ki: 0.92 nM
5-HT1D Receptor, Ki: 3.14 nM
            Pan Agonist 95.13%
LP-211
5-HT1A Receptor, Ki: 188 nM
       
5-HT7 Receptor, Ki: 0.58 nM
  Pan Agonist 99.66%
Vilazodone Hydrochloride
5-HT1A Receptor
            Pan Agonist 99.95%
Nuciferine
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-HT6 Receptor, EC50: 700 nM
5-HT7 Receptor, IC50: 150 nM
  Pan Modulator 99.66%
Flopropione
5-HT1A Receptor
            Pan Antagonist 98.37%
Eltoprazine hydrochloride
5-HT1A Receptor
5-HT1B Receptor
5-HT2C Receptor
          Pan Modulator 99.35%
GSK163090
5-HT1A Receptor, pKi: 9.4
5-HT1B Receptor, pKi: 8.5
5-HT1D Receptor, pKi: 9.7
            Pan Antagonist 99.95%
Pipamperone
5-HT1 Receptor, pKi: 5.7
5-HT2A Receptor, pKi: 8.2
5-HT2C Receptor, pKi: 6.9
          Pan Antagonist 99.89%
Pimethixene maleate
5-HT1A Receptor, pKi: 7.63
5-HT2A Receptor, pKi: 10.22
5-HT2B Receptor, pKi: 10.44
5-HT2C Receptor, pKi: 8.42
          Pan Antagonist >98.0%
Asenapine
5-HT1A Receptor, pKi: 8.6
5-HT1B Receptor, pKi: 8.4
5-HT2A Receptor, pKi: 10.2
5-HT2B Receptor, pKi: 9.8
5-HT2C Receptor, pKi: 10.5
 
5-HT5 Receptor, pKi: 8.8
5-HT6 Receptor, pKi: 9.6
5-HT7 Receptor, pKi: 9.9
  Pan Antagonist 98.81%
Rotigotine Hydrochloride
5-HT1A Receptor, Ki: 30 nM
       
5-HT7 Receptor, Ki: 86 nM
  Pan Agonist 99.39%
BRL 54443
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-HT6 Receptor, Ki: >10,000 nM
5-HT7 Receptor, Ki: >10,000 nM
  Pan Agonist 99.39%
LY334370
5-HT1F Receptor, Ki: 1.6 nM
            Pan Agonist 99.70%
Ocaperidone
5-HT1A Receptor, pEC50: 7.6 (h5-HT1A)
5-HT1A Receptor, pKi: 8.08 (h5-HT1A)
5-HT2 Receptor, Ki: 0.14 nM
          Pan Modulator 98.55%
(Rac)-Rotigotine hydrochloride
5-HT1A Receptor, Ki: 30 nM
5-HT2B Receptor, Ki: 27 nM
          Pan Agonist 97.76%
Quetiapine hemifumarate
5-HT1A Receptor, pKi: 5.74
5-HT1A Receptor, pEC50: 4.77
5-HT2A Receptor, pKi: 7.54
5-HT2C Receptor, pKi: 5.55
          Pan Agonist 98.24%
Iloperidone
Rat 5-HT1A, 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-HT6 Receptor, Ki: 42.7 μM
Rat 5-HT7 Receptor, Ki: 21.6 nM
  Pan Antagonist 99.64%
SEP-363856 hydrochloride
5-HT1A Receptor, EC50: 2.3 μM
5-HT1B Receptor, EC50: 15.6 μM
5-HT1D Receptor, EC50: 0.262 μM
5-HT2A Receptor, EC50: >10 μM
5-HT2C Receptor, EC50: 30 μM
     
5-HT7 Receptor, EC50: 6.7 μM
  Pan Agonist 99.78%
Almotriptan
5-HT1B Receptor
5-HT1D Receptor
            Pan Agonist
Almotriptan malate
5-HT1B Receptor
5-HT1D Receptor
            Pan Agonist 99.49%
Eltoprazine
5-HT1A Receptor
5-HT1B Receptor
5-HT2C Receptor
          Pan Modulator >95.0%
Pimethixene
5-HT1A Receptor, pKi: 7.63
5-HT2A Receptor, pKi: 10.22
5-HT2B Receptor, pKi: 10.44
5-HT2C Receptor, pKi: 8.42
          Pan Antagonist
Rodatristat ethyl
5-HT1 Receptor
            Pan Inhibitor
SEP-363856
5-HT1A Receptor, EC50: 2.3 μM
5-HT1B Receptor, EC50: 15.6 μM
5-HT1D Receptor, EC50: 0.262 μM
5-HT2A Receptor, EC50: >10 μM
5-HT2C Receptor, EC50: 30 μM
     
5-HT7 Receptor, EC50: 6.7 μM
  Pan Agonist
RU 24969 hemisuccinate
5-HT1A Receptor, Ki: 2.5 nM
5-HT1B Receptor, Ki: 0.38 nM
            Pan Agonist
AS19
5-HT1A Receptor, Ki: 89.7 nM
5-HT1B Receptor, Ki: 490 nM
5-HT1D Receptor, Ki: 6.6 nM
   
5-HT5 Receptor, Ki: 98.5 nM
 
Human 5-HT7 Receptor , IC50: 0.83 nM
Human 5-HT7 Receptor , Ki: 0.6 nM
  Pan Agonist >99.0%
Brexpiprazole S-oxide D8
5-HT1A Receptor, Ki: 0.12 nM
5-HT2A Receptor, Ki: 0.47 nM
          Pan Modulator
PRX-07034 hydrochloride
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
   
5-HT6 Receptor, Ki: 4-8 nM
5-HT6 Receptor, IC50: 19 nM
    Pan Antagonist
Piromelatine
5-HT1A Receptor (Agonist)
5-HT1D Receptor (Agonist)
5-HT2B Receptor (Antagonist)
          Pan Modulator 99.21%
Perospirone hydrochloride
5-HT1A Receptor, Ki: 2.9 nM
5-HT1 Receptor, Ki: 18 nM
5-HT2A Receptor, Ki: 0.6 nM
          Pan Modulator
SB-277011 hydrochloride
5-HT1D Receptor
5-HT1B Receptor
            Pan Antagonist 98.22%
AR-A 2
5-HT1A Receptor, Ki: 3070 nM
5-HT1B/D Receptor, Ki: 20 nM
5-HT2A Receptor, Ki: 339 nM
          Pan Antagonist
5-Carboxamidotryptamine maleate
5-HT1A Receptor
5-HT1B Receptor
5-HT1D Receptor
   
5-HT5 Receptor
 
5-HT7 Receptor
  Pan Agonist
AP521
5-HT1A Receptor, IC50: 94 nM (in human)
5-HT1A Receptor, IC50: 135 nM (in rat)
5-HT1B Receptor, IC50: 254 nM (in rat)
5-HT1B Receptor, IC50: 5530 nM (in human)
5-HT1D Receptor, IC50: 418 nM (in human)
   
5-HT5A Receptor, IC50: 422 nM (in human)
 
5-HT7 Receptor, IC50: 198 nM (in rat)
  Pan Agonist
Didesmethyl cariprazine
5-HT1A Receptor
            Pan Modulator
Brilaroxazine
5-HT1A Receptor, Ki: 1.5 nM
5-HT2A Receptor, Ki: 2.5 nM
5-HT2B Receptor, Ki: 0.19 nM
     
5-HT7 Receptor, Ki: 2.7 nM
  Pan Modulator
GR 113808
5-HT1A Receptor
5-HT2A Receptor
5-HT2C Receptor
5-HT3 Receptor
     
5-HT4 Receptor
Pan Antagonist
Sarizotan
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-HT6 Receptor, IC50: 3300 nM (human)
5-HT7 Receptor, IC50: 10 nM (human)
  Pan Agonist
Brexpiprazole S-oxide
5-HT1A Receptor, Ki: 0.12 nM
5-HT2A Receptor, Ki: 0.47 nM
          Pan Modulator
Iloperidone hydrochloride
Rat 5-HT1A, 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-HT6 Receptor, Ki: 42.7 nM
Rat 5-HT7 Receptor, Ki: 21.6 nM
  Pan Antagonist
Alniditan
5-HT1B Receptor, IC50: 1.7 nM (in HEK 293 cell)
5-HT1D Receptor, IC50: 1.3 nM (in HEK 293 cell)
            Pan Agonist
NEO 376
5-HT1 Receptor
            Pan Modulator
Wf-516
5-HT1A Receptor, Ki: 5 nM
5-HT2A Receptor, Ki: 40 nM
          Pan Antagonist