5-HT2 Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S2698 RS-127445

RS-127445 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
S2232 Ketanserin

Ketanserin 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 is a novel atypical antipsychotic agent with potent dopamine D2 (Ki, 14.8 nM) and serotonin 5-HT2(Ki, 3.98 nM) receptors antagonist properties.

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
S2459 Clozapine

Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.

S2493 Olanzapine

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

S1243 Agomelatine

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

S1283 Asenapine

Asenapine 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-HT2C, pKi: 10.46; 5-HT2B, pKi: 9.75; 5-HT2A, pKi: 10.15
S1615 Risperidone

Risperidone 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
S4064 Escitalopram Oxalate

Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.

Pan 5-HT, Ki: 0.89 nM
S2663 WAY-100635 Maleate

WAY-100635 Maleate is a potent and selective 5-HT1A receptor agonist with pIC50 of 8.87, exhibits >100-fold selectivity against other 5-HT receptor subtypes and major neurotransmitter receptors.

Pan 5-HT, IC50: 0.95 nM
S4053 Sertraline HCl

Sertraline HCl is a 5-HT antagonist with Ki of 13 nM.

Pan 5-HT, Ki: 13 nM
S2677 BRL-15572

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-HT2B, pKi: 7.4; 5-HT2C, pKi: 6.2; 5-HT2A, pKi: 6.6
S4113 Desvenlafaxine

Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.

Pan 5-HT, Ki: 40.2 nM
S4112 Desvenlafaxine Succinate

Desvenlafaxine Succinate is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.

Pan 5-HT, Ki: 40.2 nM
S3175 Atomoxetine HCl

Atomoxetine is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters.

Pan 5-HT, Ki: 77 nM
S3183 Amitriptyline HCl

Amitriptyline inhibits serotonin receptor, norepinephrine receptor, 5-HT4, 5-HT2 and sigma 1 receptor with IC50 of 3.45 nM, 13.3 nM, 7.31 nM, 235 nM and 287 nM, respectively.

Pan 5-HT2, IC50: 235 nM
S2691 BMY 7378

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
S1333 Fluoxetine HCl

Fluoxetine is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.

S1336 Fluvoxamine maleate

Fluvoxamine maleate is a selective serotonin (5-HT) reuptake inhibitor (SSRI).

S1869 Dapoxetine HCl

Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor.

S1432 Sumatriptan Succinate

Sumatriptan Succinate is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.

S2084 Duloxetine HCl

Duloxetine HCl is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).

S1245 Latrepirdine

Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.

S1436 Tianeptine sodium

Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.

S2016 Mirtazapine

Mirtazapine is a potent tetracyclic antidepressant.

S3005 Paroxetine HCl

Paroxetine HCl is an antidepressant drug of the SSRI type.

S2582 Trazodone HCl

Trazodone HCl is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.

S1441 Venlafaxine

Venlafaxine is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.

S1483 Iloperidone

Iloperidone is an atypical antipsychotic for the treatment of schizophrenia.

S4244 Serotonin HCl

Serotonin HCl is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.

S1649 Zolmitriptan

Zolmitriptan is a selective serotonin receptor agonist.

S1488 Naratriptan

Naratriptan is a triptan agent that is used for the treatment of migraine headaches.

S2541 Clomipramine HCl

Clomipramine HCl is a hydrochloride salt of clomipramine which is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively.