5-HT Receptor

Sigaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S2459 Clozapine <1 mg/mL 65 mg/mL 32 mg/mL
S2493 Olanzapine <1 mg/mL 62 mg/mL 9 mg/mL
S2232 Ketanserin <1 mg/mL 2 mg/mL <1 mg/mL
S1333 Fluoxetine HCl 4 mg/mL 69 mg/mL 69 mg/mL
S1245 Latrepirdine 2HCl <1 mg/mL 24 mg/mL 13 mg/mL
S4749 Citalopram HBr 81 mg/mL 81 mg/mL 81 mg/mL
S4751 Cisapride hydrate <1 mg/mL 96 mg/mL <1 mg/mL
S4748 Ondansetron Hydrochloride Dihydrate 73 mg/mL 73 mg/mL 40 mg/mL
S4694 Alosetron Hydrochloride 1 mg/mL <1 mg/mL <1 mg/mL
S4635 Cyproheptadine hydrochloride <1 mg/mL 70 mg/mL 13 mg/mL
S1436 Tianeptine sodium 91 mg/mL 91 mg/mL 91 mg/mL
S2698 RS-127445 <1 mg/mL 56 mg/mL 8 mg/mL
S1243 Agomelatine <1 mg/mL 48 mg/mL 48 mg/mL
S1283 Asenapine maleate <1 mg/mL 80 mg/mL <1 mg/mL
S1432 Sumatriptan Succinate 83 mg/mL 83 mg/mL <1 mg/mL
S1441 Venlafaxine HCl 55.5 mg/mL 55.5 mg/mL 55.5 mg/mL
S2875 Prucalopride <1 mg/mL 60 mg/mL 38 mg/mL
S3005 Paroxetine HCl 10 mg/mL 73 mg/mL 35 mg/mL
S1869 Dapoxetine HCl 68 mg/mL 68 mg/mL 68 mg/mL
S1615 Risperidone <1 mg/mL 4 mg/mL 4 mg/mL
S1444 Ziprasidone HCl <1 mg/mL 90 mg/mL <1 mg/mL
S2663 WAY-100635 Maleate <1 mg/mL 85 mg/mL 85 mg/mL
S1483 Iloperidone <1 mg/mL 27 mg/mL 4 mg/mL
S1975 Aripiprazole <1 mg/mL 90 mg/mL <1 mg/mL
S1488 Naratriptan HCl 22 mg/mL 74 mg/mL <1 mg/mL
S2691 BMY 7378 Dihydrochloride 92 mg/mL 92 mg/mL 20 mg/mL
S2112 Blonanserin <1 mg/mL <1 mg/mL <1 mg/mL
S8021 Vortioxetine (Lu AA21004) HBr <1 mg/mL 76 mg/mL 17 mg/mL
S1607 Rizatriptan Benzoate 46 mg/mL 20 mg/mL <1 mg/mL
S1649 Zolmitriptan <1 mg/mL 58 mg/mL 58 mg/mL
S2849 SB269970 HCl <1 mg/mL 11 mg/mL <1 mg/mL
S1336 Fluvoxamine maleate <1 mg/mL 87 mg/mL 87 mg/mL
S1345 Granisetron HCl 69 mg/mL 1 mg/mL 1 mg/mL
S1385 Mosapride Citrate <1 mg/mL 90 mg/mL <1 mg/mL
S4109 Lorcaserin HCl 46 mg/mL 46 mg/mL 46 mg/mL
S2016 Mirtazapine <1 mg/mL 53 mg/mL 53 mg/mL
S2894 SB742457 <1 mg/mL 78 mg/mL 2 mg/mL
S2677 BRL-15572(dihydrochloride) <1 mg/mL 96 mg/mL 40 mg/mL
S8010 PRX-08066 Maleic acid 104 mg/mL 104 mg/mL 98 mg/mL
S1390 Ondansetron HCl 24 mg/mL 66 mg/mL 10 mg/mL
S4053 Sertraline HCl <1 mg/mL 69 mg/mL 15 mg/mL
S3024 Lamotrigine <1 mg/mL 10 mg/mL 3 mg/mL
S2541 Clomipramine HCl 70 mg/mL 70 mg/mL 70 mg/mL
S4113 Desvenlafaxine <1 mg/mL 37 mg/mL 3 mg/mL
S1898 Tropisetron HCl 46 mg/mL 35 mg/mL <1 mg/mL
S3180 Eletriptan HBr <1 mg/mL 93 mg/mL <1 mg/mL
S3196 Azacyclonol 2 mg/mL 53 mg/mL 53 mg/mL
S1394 Pizotifen Malate <1 mg/mL 21 mg/mL <1 mg/mL
S4064 Escitalopram Oxalate 25 mg/mL 83 mg/mL <1 mg/mL
S2084 Duloxetine HCl <1 mg/mL 67 mg/mL <1 mg/mL
S2106 Azasetron HCl 3 mg/mL <1 mg/mL <1 mg/mL
S4247 Prucalopride Succinate 97 mg/mL 97 mg/mL <1 mg/mL
S4249 Flopropione <1 mg/mL 36 mg/mL 36 mg/mL
S4259 Vilazodone HCl <1 mg/mL 96 mg/mL <1 mg/mL
S4086 Loxapine Succinate <1 mg/mL 89 mg/mL 2 mg/mL
S1996 Ondansetron <1 mg/mL 0.1 mg/mL <1 mg/mL
S2856 SB 271046 hydrochloride <1 mg/mL 40 mg/mL <1 mg/mL
S3140 Milnacipran HCl 57 mg/mL 57 mg/mL 57 mg/mL
S2096 Almotriptan Malate <1 mg/mL 94 mg/mL 53 mg/mL
S3183 Amitriptyline HCl 15 mg/mL 63 mg/mL 63 mg/mL
S2852 BRL-54443 <1 mg/mL 46 mg/mL 2 mg/mL
S3050 Palonosetron HCl 67 mg/mL <1 mg/mL <1 mg/mL
S2865 VUF 10166 <1 mg/mL 21 mg/mL 61 mg/mL
S1642 Methyldopa <1 mg/mL 2 mg/mL <1 mg/mL
S4256 Buspirone HCl 84 mg/mL 84 mg/mL 36 mg/mL
S8183 Pimavanserin 100 mg/mL 100 mg/mL 100 mg/mL
S4112 Desvenlafaxine Succinate <1 mg/mL 80 mg/mL <1 mg/mL
S2346 Puerarin <1 mg/mL 86 mg/mL <1 mg/mL
S2582 Trazodone HCl <1 mg/mL 4 mg/mL <1 mg/mL
S2025 Urapidil HCl 85 mg/mL 24 mg/mL 1 mg/mL
S4244 Serotonin HCl 42 mg/mL 42 mg/mL 2 mg/mL
S4283 Cyclobenzaprine HCl 62 mg/mL 62 mg/mL 62 mg/mL
S2669 LY310762 HCl <1 mg/mL 0.4 mg/mL <1 mg/mL
S3175 Atomoxetine HCl 2 mg/mL 58 mg/mL 37 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1333

Fluoxetine HCl

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

S1245

Latrepirdine 2HCl

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.

S4749New

Citalopram HBr

Citalopram HBr, an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.

S4751New

Cisapride hydrate

Cisapride acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

S4748New

Ondansetron Hydrochloride Dihydrate

Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.

S4635New

Cyproheptadine hydrochloride

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

S1441

Venlafaxine HCl

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

S8021

Vortioxetine (Lu AA21004) HBr

Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

S1336

Fluvoxamine maleate

Fluvoxamine Maleate is a selective serotonin (5-HT) reuptake inhibitor (SSRI), used in the treatment of obsessive-compulsive disorder.

S4113

Desvenlafaxine

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

S4064

Escitalopram Oxalate

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

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).

S3140

Milnacipran HCl

Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively.

S1642

Methyldopa

Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.

S8183

Pimavanserin

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

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.

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.

S1283

Asenapine maleate

Asenapine maleate 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.

S4259

Vilazodone HCl

Vilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.

S3196

Azacyclonol

Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

S1436

Tianeptine sodium

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

S1432

Sumatriptan Succinate

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

S2875

Prucalopride

Prucalopride is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.

S1975

Aripiprazole

Aripiprazole is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.

S1488

Naratriptan HCl

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

S1607

Rizatriptan Benzoate

Rizatriptan Benzoate is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.

S1649

Zolmitriptan

Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.

S1385

Mosapride Citrate

Mosapride Citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

S4109

Lorcaserin HCl

Lorcaserin HCl is a selective full agonist of human 5-HT2C receptor with Ki of 15 nM.

S3180

Eletriptan HBr

Eletriptan is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.

S4247

Prucalopride Succinate

Prucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.

S2096

Almotriptan Malate

Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.

S2852

BRL-54443

BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.

S4256

Buspirone HCl

Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.

S2025

Urapidil HCl

Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively.

S4244

Serotonin HCl

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

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.

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.

S4694New

Alosetron Hydrochloride

Alosetron Hydrochloride is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.

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.

S1243

Agomelatine

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

S3005

Paroxetine HCl

Paroxetine HCl is an antidepressant drug of the SSRI type.

S1869

Dapoxetine HCl

Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.

S1615

Risperidone

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

S1444

Ziprasidone HCl

Ziprasidone HCl is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.

S2663

WAY-100635 Maleate

WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.

S1483

Iloperidone

Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.

S2112

Blonanserin

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

S2849

SB269970 HCl

SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.

S1345

Granisetron HCl

Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.

S2016

Mirtazapine

Mirtazapine is an adrenergic and seroton receptor antagonist, used to treat depression.

S2894

SB742457

SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.

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.

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.

S1390

Ondansetron HCl

Ondansetron is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.

S4053

Sertraline HCl

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

S3024

Lamotrigine

Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.

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.

S1898

Tropisetron HCl

Tropisetron HCl is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

S1394

Pizotifen Malate

Pizotifen Malate is a benzocycloheptane based agent used for recurrent migraine headaches.

S2106

Azasetron HCl

Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.

S4249

Flopropione

Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.

S4086

Loxapine Succinate

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

S1996

Ondansetron

Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.

S2856

SB 271046 hydrochloride

SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.

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.

S3050

Palonosetron HCl

Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.

S2865

VUF 10166

VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.

S2346

Puerarin

Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.

S2582

Trazodone HCl

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

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.

S2669

LY310762 HCl

LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.

Catalog No. Information Product Use Citations Product Validations
S1333

Fluoxetine HCl

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

S1245

Latrepirdine 2HCl

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.

S4749New

Citalopram HBr

Citalopram HBr, an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.

S4751New

Cisapride hydrate

Cisapride acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

S4748New

Ondansetron Hydrochloride Dihydrate

Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.

S4635New

Cyproheptadine hydrochloride

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

S1441

Venlafaxine HCl

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

S8021

Vortioxetine (Lu AA21004) HBr

Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

S1336

Fluvoxamine maleate

Fluvoxamine Maleate is a selective serotonin (5-HT) reuptake inhibitor (SSRI), used in the treatment of obsessive-compulsive disorder.

S4113

Desvenlafaxine

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

S4064

Escitalopram Oxalate

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

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).

S3140

Milnacipran HCl

Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively.

S1642

Methyldopa

Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.

S8183

Pimavanserin

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

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.

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.

Catalog No. Information Product Use Citations Product Validations
S2459

Clozapine

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

2015, 43(7):1147-53

S2493

Olanzapine

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

2014, 15(19):8107-13

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.

S4694New

Alosetron Hydrochloride

Alosetron Hydrochloride is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.

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.

S1243

Agomelatine

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

S3005

Paroxetine HCl

Paroxetine HCl is an antidepressant drug of the SSRI type.

S1869

Dapoxetine HCl

Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.

S1615

Risperidone

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

S1444

Ziprasidone HCl

Ziprasidone HCl is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.

S2663

WAY-100635 Maleate

WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.

2014, 4:7270

S1483

Iloperidone

Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.

S2112

Blonanserin

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

S2849

SB269970 HCl

SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.

2015, 5:8060

S1345

Granisetron HCl

Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.

S2016

Mirtazapine

Mirtazapine is an adrenergic and seroton receptor antagonist, used to treat depression.

S2894

SB742457

SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.

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.

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.

S1390

Ondansetron HCl

Ondansetron is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.

S4053

Sertraline HCl

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

S3024

Lamotrigine

Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.

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.

S1898

Tropisetron HCl

Tropisetron HCl is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

S1394

Pizotifen Malate

Pizotifen Malate is a benzocycloheptane based agent used for recurrent migraine headaches.

S2106

Azasetron HCl

Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy.

S4249

Flopropione

Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.

S4086

Loxapine Succinate

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

S1996

Ondansetron

Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.

S2856

SB 271046 hydrochloride

SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes.

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.

S3050

Palonosetron HCl

Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.

S2865

VUF 10166

VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.

S2346

Puerarin

Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.

2015, 10.1021/cb5009487

S2582

Trazodone HCl

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

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.

S2669

LY310762 HCl

LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.

Catalog No. Information Product Use Citations Product Validations
S1436

Tianeptine sodium

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

2014, 4:e411

S1432

Sumatriptan Succinate

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

S2875

Prucalopride

Prucalopride is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.

2016, 28(8):1241-51

S1975

Aripiprazole

Aripiprazole is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.

S1488

Naratriptan HCl

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

S1607

Rizatriptan Benzoate

Rizatriptan Benzoate is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.

S1649

Zolmitriptan

Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.

S1385

Mosapride Citrate

Mosapride Citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

S4109

Lorcaserin HCl

Lorcaserin HCl is a selective full agonist of human 5-HT2C receptor with Ki of 15 nM.

S3180

Eletriptan HBr

Eletriptan is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.

S4247

Prucalopride Succinate

Prucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively.

S2096

Almotriptan Malate

Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.

S2852

BRL-54443

BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.

S4256

Buspirone HCl

Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.

S2025

Urapidil HCl

Urapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively.

S4244

Serotonin HCl

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

Catalog No. Information Product Use Citations Product Validations
S1283

Asenapine maleate

Asenapine maleate 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.

S4259

Vilazodone HCl

Vilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.

Catalog No. Information Product Use Citations Product Validations
S3196

Azacyclonol

Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

Tags: 5-HT receptor drugs | Serotonin receptor drugs | 5-HT receptor agonist and antagonist drugs | Serotonin receptor antagonist drugs | Serotonin receptor agonist drugs | 5-HT3 receptor antagonist drugs | 5-HT receptor agonist and antagonist clinical trial | 5-HT receptor agonist and antagonist ic50 | 5-HT receptor agonist and antagonist review