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

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-HT_2A Receptor, Ki: 8.9 nM							Selective Antagonist	99.90%
Harmine	5-HT_2A Receptor, Ki: 397 nM							Selective Inhibitor	99.93%
SCH-23390 hydrochloride	5-HT_2C Receptor, Ki: 9.3 nM							Selective Agonist	99.31%
SKF-83566	5-HT₂ Receptor, Ki: 11 nM							Selective Antagonist	99.86%
Risperidone	5-HT_2A Receptor, Ki: 4.8 nM							Selective Inhibitor	98.01%
Puerarin	5-HT_2C Receptor							Selective Antagonist	99.20%
Ketanserin	5-HT₂ Receptor							Selective Antagonist	98.57%
Pimavanserin	5-HT_2A Receptor, pIC₅₀: 8.7							Selective Inhibitor	99.99%
Perphenazine	5-HT_2A Receptor, Ki: 5.6 nM							Selective Inhibitor	99.72%
Asenapine maleate	5-HT_2A Receptor, Ki: 0.06 nM 5-HT_2C Receptor, Ki: 0.03 nM					5-HT₇ Receptor, Ki: 0.13 nM		Selective Antagonist	99.95%
Volinanserin	5-HT₂ Receptor, Ki: 0.36 nM							Selective Antagonist	99.71%
Agomelatine	5-HT_2C Receptor, pKi: 6.4 (native porcine) 5-HT_2C Receptor, pKi: 6.2 (human)							Selective Antagonist	98.77%
Cyproheptadine hydrochloride	5-HT₂ Receptor							Selective Antagonist	99.98%
Nefazodone hydrochloride	5-HT_2A Receptor, Ki: 5.8 nM							Selective Antagonist	99.71%
Pimavanserin tartrate	5-HT_2A Receptor, pIC₅₀: 8.73 5-HT_2A Receptor, pKi: 9.3							Selective Inhibitor	99.50%
Pizotifen	5-HT_2A Receptor							Selective Antagonist	99.73%
SB 242084	5-HT_2C Receptor, pKi: 9.0							Selective Antagonist	99.47%
Ketanserin tartrate	5-HT₂ Receptor							Selective Antagonist	99.97%
Ritanserin	5-HT₂ Receptor, IC₅₀: 0.9 nM							Selective Antagonist	>99.0%
Trimipramine maleate	5-HT₂ Receptor, pKi: 8.10							Selective Antagonist	99.84%
Cinanserin hydrochloride	5-HT₂ Receptor, Ki: 41 nM							Selective Antagonist	99.74%
Vabicaserin hydrochloride	5-HT_2C Receptor, EC₅₀: 8 nM							Selective Agonist	98.99%
Sarpogrelate hydrochloride	5-HT_2A Receptor, pKi: 8.52 5-HT_2B Receptor, pKi: 6.57 5-HT_2C Receptor, pKi: 7.43							Selective Antagonist	>98.0%
Blonanserin	5-HT_2A Receptor, Ki: 0.812 nM 5-HT_2C Receptor, Ki: 26.4 nM				5-HT₆ Receptor, Ki: 11.7 nM			Selective Antagonist	99.77%
Asenapine hydrochloride	5-HT_2A Receptor, Ki: 0.06 nM 5-HT_2C Receptor, Ki: 0.03 nM					5-HT₇ Receptor, Ki: 0.13 nM		Selective Antagonist	99.39%
Lidanserin	5-HT_2A Receptor							Selective Antagonist	>98.0%
Nelotanserin	5-HT_2A Receptor, IC₅₀: 1.7 nM 5-HT_2C Receptor, IC₅₀: 79 nM 5-HT_2B Receptor, IC₅₀: 791 nM							Selective Antagonist	99.79%
Pimethixene maleate	5-HT_2A Receptor, pKi: 10.22 5-HT_2B Receptor, pKi: 10.44 5-HT_2C Receptor, pKi: 8.42	5-HT_1A Receptor, pKi: 7.63						Selective Antagonist	>98.0%
PRX-08066	5-HT_2B Receptor, IC₅₀: 3.4 nM							Selective Antagonist	97.04%
Roluperidone	5-HT_2A Receptor, Ki: 7.53 nM							Selective	98.08%
Agomelatine hydrochloride	5-HT_2C Receptor, pKi: 6.4 (native porcine) 5-HT_2C Receptor, pKi: 6.2 (human)							Selective Antagonist	99.49%
Cyproheptadine hydrochloride sesquihydrate	5-HT₂ Receptor							Selective Antagonist	99.20%
Naftidrofuryl oxalate	5-HT₂ Receptor							Selective Antagonist	95.81%
Isocorynoxeine	5-HT_2A Receptor, IC₅₀: 72.4 μM							Selective Inhibitor	99.97%
SKF-83566 hydrobromide	5-HT₂ Receptor, Ki: 11 nM							Selective Antagonist
Fananserin	5-HT₂ Receptor, Ki: 0.37 nM							Selective Antagonist	99.71%
Spiramide	5-HT₂ Receptor, Ki: 2 nM	5-HT_1A Receptor, Ki: 50 nM 5-HT_1C Receptor, Ki: 4300 nM						Selective Antagonist	98.81%
Risperidone hydrochloride	5-HT₂ Receptor, Ki: 4.8 nM							Selective Antagonist
Pimethixene	5-HT_2A Receptor, pKi: 10.22 5-HT_2B Receptor, pKi: 10.44 5-HT_2C Receptor, pKi: 8.42	5-HT_1A Receptor, pKi: 7.63						Selective Antagonist
Blonanserin D5	5-HT₂ Receptor							Selective Antagonist
cis-Urocanic acid	5-HT_2A Receptor							Selective Agonist	99.92%
SB-215505	5-HT_2B Receptor, pKi: 8.3 5-HT_2A Receptor, pKi: 6.77 5-HT_2C Receptor, pKi: 7.66							Selective Antagonist
SB 243213	Human 5-HT_2C Receptor, pKi: 9.37 Human 5-HT_2A Receptor, pKi: 7.01 human 5-HT_2B Receptor, pKi: 7.2	human 5-HT_1A Receptor, pKi: <5.3 human 5-HT_1B Receptor, pKi: 5.5 human 5-HT_1D Receptor, pKi: 6.32 human 5-HT_1E Receptor, pKi: <5.4 human 5-HT_1F Receptor, pKi: 5.35			Human 5-HT₆ Receptor, pKi: 6.5	Human 5-HT₇ Receptor , pKi: 5.64		Selective Antagonist	98.62%
3-Hydroxy agomelatine	5-HT_2C Receptor, IC₅₀: 3.2 μM 5-HT_2C Receptor, Ki: 1.8 μM							Selective Antagonist
Blonanserin D8	5-HT₂ Receptor							Selective Antagonist
SCH-23390 maleate	5-HT_2C Receptor, Ki: 9.3 nM							Selective Agonist
7-Desmethyl-3-hydroxyagomelatine	5-HT_2C Receptor							Selective Antagonist
Flumexadol	5-HT_2C Receptor, Ki: 25 nM							Selective Agonist	98.50%
Iferanserin	5-HT_2A Receptor							Selective Antagonist
Eplivanserin (mixture)	5-HT_2A Receptor							Selective Antagonist	99.95%
Org-12962	5-HT_2C Receptor, pEC₅₀: 7.01 5-HT_2A Receptor, pEC₅₀: 6.38 5-HT_2B Receptor, pEC₅₀: 6.28							Selective Agonist	>98.0%
(Rac)-WAY-161503	5-HT_2C Receptor, Ki: 4 nM 5-HT_2C Receptor, EC₅₀: 12 nM							Selective Agonist	>99.0%
Clocapramine hydrochloride hydrate	5-HT_2A Receptor							Selective Antagonist
Opiranserin	5-HT_2A Receptor, IC₅₀: 1.3 μM							Selective Antagonist
RS-127445	5-HT_2B Receptor, pKi: 9.5 nM							Selective Antagonist
Org-12962 hydrochloride	5-HT_2C Receptor, pEC₅₀: 7.01 5-HT_2A Receptor, pEC₅₀: 6.38 5-HT_2B Receptor, pEC₅₀: 6.28							Selective Agonist
(R)-Praziquantel D11	5-HT_2B Receptor							Selective Agonist
Harmine hydrochloride	5-HT_2A Receptor, Ki: 397 nM							Selective Inhibitor
Risperidone mesylate	5-HT_2A Receptor, Ki: 4.8 nM							Selective Inhibitor
Agomelatine (L(+)-Tartaric acid)	5-HT_2C Receptor, pKi: 6.4 (native porcine) 5-HT_2C Receptor, pKi: 6.2 (human)							Selective Antagonist	99.82%
Pizotifen malate	5-HT_2A Receptor							Selective Antagonist
Clocapramine	5-HT_2A Receptor							Selective Antagonist
(4E)-SUN9221	5-HT₂ Receptor							Selective Antagonist
5-HT2 antagonist 1	5-HT₂ Receptor							Selective Antagonist
5-HT2A antagonist 1	5-HT_2A Receptor							Selective Antagonist
Olanzapine	5-HT_2A Receptor, Ki: 4 nM 5-HT_2C Receptor, Ki: 11 nM	5-HT₁ Receptor, Ki: 7 nM	5-HT₃ Receptor, Ki: 57 nM		5-HT₆ Receptor, Ki: 5 nM			Pan Antagonist	99.89%
Sertindole	5-HT_2A Receptor 5-HT_2C Receptor							Pan Antagonist	99.76%
Brexpiprazole	5-HT_2A Receptor, Ki: 0.47 nM	5-HT_1A Receptor, Ki: 0.12 nM						Pan Modulator	99.40%
Amitriptyline hydrochloride	5-HT_2A Receptor, IC₅₀: 4 nM 5-HT_2B Receptor, IC₅₀: 40 nM 5-HT_2C Receptor, IC₅₀: 6 nM	5-HT_1A Receptor, IC₅₀: 450 nM 5-HT_1B Receptor, IC₅₀: 40 nM						Pan Inhibitor	99.56%
Lumateperone tosylate	5-HT_2A Receptor, Ki: 0.54 nM							Pan Antagonist	99.21%
Methiothepin mesylate	5-HT_2A Receptor, pKi: 8.50 5-HT_2B Receptor, pKi: 8.68 5-HT_2C Receptor, pKi: 8.35	5-HT_1A Receptor, pKd: 7.10 5-HT_1B Receptor, pKd: 7.28 5-HT_1C Receptor, pKd: 7.56 5-HT_1D Receptor, pKd: 6.99		5-HT_5A Receptor, pKd: 7.0 5-HT_5B Receptor, pKd: 7.8	5-HT₆ Receptor, pKd: 8.74	5-HT₇ Receptor, pKd: 8.99		Pan Antagonist	99.32%
Ziprasidone	Rat 5-HT_2A, Ki: 0.42 nM	Rat 5-HT_1A Receptor, Ki: 3.4 nM human 5-HT_1A Receptor, Ki: 2.5 nM						Pan Antagonist	98.69%
Quetiapine	5-HT_2A Receptor, pKi: 7.54 5-HT_2C Receptor, pKi: 5.55	5-HT_1A Receptor, pKi: 5.74 5-HT_1A Receptor, pEC₅₀: 4.77						Pan Agonist	99.96%
Mirtazapine	5-HT₂ Receptor, pKi: 8.05		5-HT₃ Receptor, pKi: 8.1					Pan Antagonist	99.97%
Tegaserod maleate	5-HT_2B Receptor (Antagonist)						5-HT₄ Receptor (Agonist)	Pan Modulator	99.75%
Flibanserin	5-HT_2A Receptor, Ki: 49 nM	5-HT_1A Receptor, Ki: 1 nM						Pan Modulator	99.10%
Quetiapine hemifumarate	5-HT_2A Receptor, pKi: 7.54 5-HT_2C Receptor, pKi: 5.55	5-HT_1A Receptor, pKi: 5.74 5-HT_1A Receptor, pEC₅₀: 4.77						Pan Agonist	98.24%
GSK163090	5-HT_2A Receptor, pKi: 6 5-HT_2B Receptor, pKi: 6.3 5-HT_2C Receptor, pKi: 5.8	5-HT_1A Receptor, pKi: 9.4 5-HT_1B Receptor, pKi: 8.5 5-HT_1D Receptor, pKi: 9.7			Human 5-HT₆ Receptor, pKi: <5.3	Human 5-HT₇ Receptor , pKi: 6.8		Pan Antagonist	99.95%
RS-127445 hydrochloride	5-HT_2A Receptor, pKi: 6.3 5-HT_2C Receptor, pKi: 6.4 5-HT_2B Receptor, pKi: 9.5		5-HT₃ Receptor, pKi: <6	5-HT₅ Receptor, pKi: <6	5-HT₆ Receptor, pKi: <6			Pan Antagonist	99.68%
Asenapine	5-HT_2A Receptor, pKi: 10.2 5-HT_2C Receptor, pKi: 10.5 5-HT_2B Receptor, pKi: 9.8	5-HT_1A Receptor, pKi: 8.6 5-HT_1B 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-HT_2A Receptor, Ki: 1259 nM 5-HT_2B Receptor, Ki: 100 nM 5-HT_2C Receptor, Ki: 316 nM	5-HT_1E Receptor, Ki: 1.1 nM 5-HT_1F Receptor, Ki: 0.7 nM 5-HT_1A Receptor, Ki: 63 nM 5-HT_1B Receptor, Ki: 126 nM 5-HT_1D Receptor, Ki: 63 nM			5-HT₆ Receptor, Ki: >10,000 nM	5-HT₇ Receptor, Ki: >10,000 nM		Pan Agonist	99.39%
Iloperidone	Rat 5-HT₂ Receptor, Ki: 3.1 nM Human 5-HT_2A Receptor, Ki: 5.6 nM Human 5-HT_2C Receptor, Ki: 42.8 nM	Rat 5-HT_1A Receptor, Ki: 168 nM			Rat 5-HT₆ Receptor, Ki: 42.7 μM	Rat 5-HT₇ Receptor, Ki: 21.6 nM		Pan Antagonist	99.64%
Nuciferine	5-HT_2C Receptor, IC₅₀: 131 nM 5-HT_2A Receptor, IC₅₀: 478 nM 5-HT_2B Receptor, IC₅₀: 1 μM	5-HT_1A Receptor, EC₅₀: 3.2 μM			5-HT₆ Receptor, EC₅₀: 700 nM	5-HT₇ Receptor, IC₅₀: 150 nM		Pan Modulator	99.66%
SEP-363856 hydrochloride	5-HT_2A Receptor, EC₅₀: >10 μM 5-HT_2C Receptor, EC₅₀: 30 μM	5-HT_1A Receptor, EC₅₀: 2.3 μM 5-HT_1B Receptor, EC₅₀: 15.6 μM 5-HT_1D Receptor, EC₅₀: 0.262 μM				5-HT₇ Receptor, EC₅₀: 6.7 μM		Pan Agonist	99.78%
Temanogrel	5-HT_2A Receptor, Ki: 4.9 nM							Pan Antagonist	98.94%
SB-200646A	5-HT_2B Receptor, pKi: 7.5 5-HT_2C Receptor, pKi: 6.9 5-HT_2A Receptor, pKi: 5.2							Pan Antagonist	99.47%
Arotinolol	5-HT_2A Receptor							Pan Antagonist	98.18%
Eltoprazine hydrochloride	5-HT_2C Receptor	5-HT_1A Receptor 5-HT_1B Receptor						Pan Modulator	99.85%
Perospirone	5-HT_2A Receptor, Ki: 0.6 nM	5-HT_1A Receptor, Ki: 2.9 nM 5-HT₁ Receptor, Ki: 18 nM						Pan Modulator	99.51%
Pipamperone	5-HT_2A Receptor, pKi: 8.2 5-HT_2C Receptor, pKi: 6.9	5-HT₁ Receptor, pKi: 5.7						Pan Antagonist	99.89%
(Rac)-Rotigotine hydrochloride	5-HT_2B Receptor, Ki: 27 nM	5-HT_1A Receptor, Ki: 30 nM						Pan Agonist	97.76%
Ziprasidone hydrochloride monohydrate	Rat 5-HT_2A, : 0.42 nM	Rat 5-HT_1A Receptor, : 3.4 nM human 5-HT_1A Receptor, : 2.5 nM						Pan Antagonist	99.83%
Ocaperidone	5-HT₂ Receptor, Ki: 0.14 nM	5-HT_1A Receptor, pEC₅₀: 7.6 (h5-HT_1A) 5-HT_1A Receptor, pKi: 8.08 (h5-HT_1A)						Pan Modulator	98.55%
SB 271046 Hydrochloride	5-HT_2A Receptor, pKi: 5.62 5-HT_2B Receptor, pKi: 5.41 Human 5-HT_2C Receptor, pKi: 5.73	5-HT_1D Receptor, pKi: 6.55 5-HT_1A Receptor, pKi: 6.35 5-HT_1B Receptor, pKi: 6.05 5-HT_1F Receptor, pKi: 5.95 5-HT_1E Receptor, pKi: <4.99			5-HT₆ Receptor, pKi: 8.92-9.02	5-HT₇ Receptor, pKi: 5.39	5-HT₄ Receptor, pKi: 5.27	Pan Antagonist	99.06%
Setiptiline	5-HT_2A Receptor 5-HT_2C Receptor		5-HT₃ Receptor					Pan Modulator	96.54%
SB 243213 dihydrochloride	Human 5-HT_2C Receptor, pKi: 9.37 Human 5-HT_2A Receptor, pKi: 7.01 human 5-HT_2B Receptor, pKi: 7.2	human 5-HT_1A Receptor, pKi: <5.3 human 5-HT_1B Receptor, pKi: 5.5 human 5-HT_1D Receptor, pKi: 6.32 human 5-HT_1E Receptor, pKi: <5.4 human 5-HT_1F Receptor, pKi: 5.35			Human 5-HT₆ Receptor, pKi: 6.5	Human 5-HT₇ Receptor , pKi: 5.64		Pan Antagonist	>99.0%
Piromelatine	5-HT_2B Receptor (Antagonist)	5-HT_1A Receptor (Agonist) 5-HT_1D Receptor (Agonist)						Pan Modulator	99.21%
SB 243213 hydrochloride	Human 5-HT_2C Receptor, pKi: 9.37 Human 5-HT_2A Receptor, pKi: 7.01 human 5-HT_2B Receptor, pKi: 7.2	human 5-HT_1A Receptor, pKi: <5.3 human 5-HT_1B Receptor, pKi: 5.5 human 5-HT_1D Receptor, pKi: 6.32 human 5-HT_1E Receptor, pKi: <5.4 human 5-HT_1F Receptor, pKi: 5.35			Human 5-HT₆ Receptor, pKi: 6.5	Human 5-HT₇ Receptor , pKi: 5.64		Pan Antagonist
Eltoprazine	5-HT_2C Receptor	5-HT_1A Receptor 5-HT_1B Receptor						Pan Modulator	>95.0%
5-HT6/7 antagonist 1	5-HT_2A Receptor				5-HT₆ Receptor	5-HT₇ Receptor		Pan Antagonist
Spiperone hydrochloride	5-HT_2A Receptor, Ki: 1 nM	5-HT_1A Receptor, Ki: 49 nM						Pan Antagonist
LY320135	5-HT₂ Receptor, Ki: 6.4 μM							Pan Modulator
Mirtazapine D3	5-HT₂ Receptor		5-HT₃ Receptor					Pan Inhibitor
Isopteropodine	5-HT₂ Receptor							Pan Agonist
Brexpiprazole S-oxide D8	5-HT_2A Receptor, Ki: 0.47 nM	5-HT_1A Receptor, Ki: 0.12 nM						Pan Modulator
Cyamemazine	5-HT_2A Receptor, Ki: 1.5 nM 5-HT_2C Receptor, Ki: 12 nM		5-HT₃ Receptor, Ki: 75 nM					Pan Antagonist	>99.0%
5-HT1A modulator 1	5-HT_2A Receptor, IC₅₀: 500 nM 5-HT_2C Receptor, IC₅₀: 4000 nM							Pan Modulator
Perospirone hydrochloride	5-HT_2A Receptor, Ki: 0.6 nM	5-HT_1A Receptor, Ki: 2.9 nM 5-HT₁ Receptor, Ki: 18 nM						Pan Modulator
Eplivanserin	5-HT₂ Receptor, IC₅₀: 5.8 nM (in rat cortical membrane) 5-HT₂ Receptor, Ki: 1.14 nM							Pan Antagonist
AR-A 2	5-HT_2A Receptor, Ki: 339 nM	5-HT_1A Receptor, Ki: 3070 nM 5-HT_1B/D Receptor, Ki: 20 nM						Pan Antagonist
TIK-301	5-HT_2C Receptor 5-HT_2B Receptor							Pan Antagonist
BGC20-761	Human 5-HT_2A Receptor, Ki: 69 nM				Human 5-HT₆ Receptor, Ki: 20 nM			Pan Antagonist
SB228357	5-HT_2A Receptor, pKi: 6.9 5-HT_2C Receptor, pKi: 9 5-HT_2B Receptor, pKi: 8							Pan Antagonist	>99.0%
Brilaroxazine	5-HT_2A Receptor, Ki: 2.5 nM 5-HT_2B Receptor, Ki: 0.19 nM	5-HT_1A Receptor, Ki: 1.5 nM				5-HT₇ Receptor, Ki: 2.7 nM		Pan Modulator
GR 113808	5-HT_2A Receptor 5-HT_2C Receptor	5-HT_1A Receptor	5-HT₃ Receptor				5-HT₄ Receptor	Pan Antagonist
(S)-Mirtazapine	5-HT₂ Receptor		5-HT₃ Receptor					Pan Antagonist
SB-200646	5-HT_2B Receptor, pKi: 7.5 5-HT_2C Receptor, pKi: 6.9 5-HT_2A Receptor, pKi: 5.2							Pan Antagonist
cis-(Z)-Flupentixol dihydrochloride	5-HT_2A Receptor, Ki: 7 nM							Pan Antagonist
Brexpiprazole S-oxide	5-HT_2A Receptor, Ki: 0.47 nM	5-HT_1A Receptor, Ki: 0.12 nM						Pan Modulator
Iloperidone hydrochloride	Rat 5-HT₂ Receptor, Ki: 3.1 nM Human 5-HT_2A Receptor, Ki: 5.6 nM Human 5-HT_2C Receptor, Ki: 42.8 nM	Rat 5-HT_1A Receptor, Ki: 168 nM			Rat 5-HT₆ Receptor, Ki: 42.7 nM	Rat 5-HT₇ Receptor, Ki: 21.6 nM		Pan Antagonist
Ziprasidone hydrochloride	Rat 5-HT_2A, Ki: 0.42 nM	Rat 5-HT_1A Receptor, Ki: 3.4 nM human 5-HT_1A Receptor, Ki: 2.5 nM						Pan Antagonist
Nexopamil racemate	5-HT₂ Receptor							Pan
Deramciclane	5-HT_2A Receptor 5-HT_2C Receptor							Pan Antagonist
Irindalone	5-HT₂ Receptor							Pan Antagonist
Paliperidone	5-HT_2A Receptor							Antagonist	99.87%
Setiptiline maleate	5-HT_2A Receptor 5-HT_2C Receptor		5-HT₃ Receptor					Antagonist	98.18%
Paliperidone palmitate	5-HT_2A Receptor							Antagonist	98.16%

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5-HT2 Receptor Inhibitors

5-HT₂ Receptor Inhibitors