5-HT2 Selective Inhibitors | Agonists | Antagonists | Modulators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S4283 Cyclobenzaprine HCl

Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist.

Selective
S5472 Nafronyl oxalate salt

Nafronyl oxalate salt is the oxalate salt form of nafronyl, which is a selective antagonist of 5-HT2 receptors and a vasodilator used in the management of peripheral and cerebral vascular disorders.

Selective
S2698 RS-127445

RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.

Selective 5-HT2B, pIC50: 10.4; 5-HT2B, pKi: 9.5
S3706 Sarpogrelate hydrochloride

Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively.

Selective 5-HT2B, Kd: 2.1 nM; 5-HT2C, Kd: 1.1 nM; 5-HT2B, Ki: 2.1 nM; 5-HT2A, Kd: 0.2 nM
S0313 Volinanserin

Volinanserin (Volinanserin Hydrochloride Salt, MDL100907, M 100907, MDL-100,907) is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity.

Selective 5-HT2 receptor, Ki: 0.36 nM
S4635 Cyproheptadine hydrochloride sesquihydrate

Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.

Selective 5-HT2, IC50: 0.6 nM
S8183 Pimavanserin

Pimavanserin (ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease.

Selective 5-HT2A, pIC50: 8.7
S2232 Ketanserin

Ketanserin (R41468) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug.

Selective 5-HT2C (Human), Ki: 100 nM; 5-HT2C (Rat), Ki: 50 nM; 5-HT2A, Ki: 2.5 nM
S8010 PRX-08066 Maleic acid

PRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2.

Selective 5-HT2B, IC50: 3.4 nM
S2112 Blonanserin

Blonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.

Selective 5-HT2, Ki: 3.98 nM
S4086 Loxapine Succinate

Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

Selective 5-HT2 (bovine), Ki: 6.6 nM; 5-HT2 (bovine), Ki: 6.8 nM; 5-HT2 (human), Ki: 6.2 nM
S0476 SCH-23390 hydrochloride

SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.

Selective h5-HT2C receptor, Ki: 9.3 nM
S2649 SB 200646

SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo.

Selective 5-HT2A (rat), pKi: 5.2; 5-HT2B (rat), pKi: 7.5; 5-HT2C (Rat), pKi: 6.9
S3183 Amitriptyline HCl

Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA).

Selective 5-HT2, Ki: 235 nM
S2459 Clozapine

Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.

Selective
S2493 Olanzapine

Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

Selective
S1243 Agomelatine (S20098)

Agomelatine (S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.

Selective
S5770 Pizotifen

Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site.

Selective
S1283 Asenapine maleate

Asenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.

Pan 5-HT2A, pKi: 10.15; 5-HT2B, pKi: 9.75; 5-HT2C, pKi: 10.46
S3913 Pimethixene maleate

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.

Pan 5-HT2C, pKi: 8.42; 5-HT2B, pKi: 10.44; 5-HT2A, pKi: 10.22
S1615 Risperidone

Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.

Pan 5-HT2C, Ki: 12 nM; 5-HT2B, Ki: 61.9 nM; 5-HT2A, Ki: 0.17 nM
S4639 Brexpiprazole

Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.

Pan 5-HT2A receptors, Ki: 0.47 nM
S5714 lurasidone

Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.

Pan 5-HT2A, Ki: 0.5 nM
S5185 Perospirone

Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.

Pan 5-HT2 receptor, Ki: 0.6 nM
S4889 Perospirone hydrochloride

Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.

Pan 5-HT2 receptor, Ki: 0.61 nM
S2677 BRL-15572 Dihydrochloride

BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

Pan 5-HT2C, pKi: 6.2; 5-HT2B, pKi: 7.4; 5-HT2A, pKi: 6.6
S3716 Flibanserin

Flibanserin (BIMT-17, BIMT-17-BS) is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.

Pan 5-HT2A, Ki: 49 nM
S2691 BMY 7378 Dihydrochloride

BMY 7378 is a multi-targeted inhibitor of α2C-adrenoceptor and α1D-adrenoceptor with pKi of 6.54 and 8.2, respectively, and acts as a mixed agonist and antagonist for 5-HT1A receptor with pKi of 8.3.

Pan 5-HT2, pIC50: 5.5
S5843 Cinitapride Hydrogen Tartrate

Cinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors

Pan