5-HT Receptor

5-HT Receptor Inhibitors | Agonists | Antagonists | Modulators (61)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2459 Clozapine Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
  • Drug Metab Dispos, 2015, 10.1124/dmd.114.062653
S2493 Olanzapine Olanzapine is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
  • Asian Pac J Cancer Prev, 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.
S1333 Fluoxetine HCl Fluoxetine is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.
  • Georgia State University, 2014, Chaquettea Felton
  • G3 (Bethesda), 2014, 4(6):1081-9
S1436 Tianeptine sodium Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.
  • Transl Psychiatry, 2014, 4:e411
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.
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.
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.
S1432 Sumatriptan Succinate Sumatriptan Succinate is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
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.
S1869 Dapoxetine HCl Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor.
S3005 Paroxetine HCl Paroxetine HCl is an antidepressant drug of the SSRI type.
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-HT1A receptor agonist with pIC50 of 8.87, exhibits >100-fold selectivity against other 5-HT receptor subtypes and major neurotransmitter receptors.
  • Sci Rep, 2014, 4:7270
S1483 Iloperidone Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.
S1975 Aripiprazole Aripiprazole is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.
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.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
S1488 Naratriptan Naratriptan is a triptan agent that is used for the treatment of migraine headaches.
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.
S1607 Rizatriptan Benzoate Rizatriptan Benzoate is a 5-HT1 agonist triptan drug for the treatment of migraine headaches.
S1649 Zolmitriptan Zolmitriptan is a selective serotonin receptor agonist.
S1345 Granisetron HCl Granisetron HCl is a serotonin 5-HT3 receptor antagonist.
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.
S1385 Mosapride Citrate Mosapride Citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S1336 Fluvoxamine maleate Fluvoxamine maleate is a selective serotonin (5-HT) reuptake inhibitor (SSRI).
S2016 Mirtazapine Mirtazapine is an adrenergic and seroton receptor antagonist, used to treat depression.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
  • Sci Rep, 2015, 5:8060
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.
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.
S4109 Lorcaserin HCl Lorcaserin HCl is a selective full agonist of human 5-HT2C receptor with Ki of 15 nM.
S1390 Ondansetron HCl Ondansetron HCl is a serotonin 5-HT3 receptor antagonist.
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.
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.
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.
S4053 Sertraline HCl Sertraline HCl is a 5-HT antagonist with Ki of 13 nM.
S4113 Desvenlafaxine Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1898 Tropisetron HCl Tropisetron HCl is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
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.
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).
  • J Pharmacol Exp Ther, 2014, 349(3):402-7
  • Am J Physiol Renal Physiol, 2013, 305(12):F1663-8
S4064 Escitalopram Oxalate Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.
S2856 SB271046 SB271046 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.
S1996 Ondansetron Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.
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.
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.
S4086 Loxapine Succinate Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
S4247 Prucalopride Succinate Prucalopride is a selective, high affinity 5-HT4 receptor agonist, inhibiting human 5-HT(4a) and 5-HT(4b) receptor with Ki value of 2.5 nM and 8 nM, respectively.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
S2669 LY310762 LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.
S2582 Trazodone HCl Trazodone HCl is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
S4244 Serotonin HCl Serotonin HCl is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.
S4256 Buspirone HCl Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
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.
S3050 Palonosetron HCl Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.
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.
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.
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.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
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.
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All 5-HT Receptor Products

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S2459 Clozapine <1 mg/mL 65 mg/mL 32 mg/mL
S2493 Olanzapine <1 mg/mL 63 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
S1436 Tianeptine sodium 91 mg/mL 91 mg/mL 91 mg/mL
S1245 Latrepirdine <1 mg/mL 24 mg/mL 13 mg/mL
S2698 RS-127445 <1 mg/mL 56 mg/mL 8 mg/mL
S1243 Agomelatine <1 mg/mL 49 mg/mL 49 mg/mL
S1283 Asenapine <1 mg/mL 80 mg/mL <1 mg/mL
S1432 Sumatriptan Succinate 83 mg/mL 83 mg/mL <1 mg/mL
S1441 Venlafaxine 55.5 mg/mL 55.5 mg/mL 55.5 mg/mL
S2875 Prucalopride <1 mg/mL 60 mg/mL 38 mg/mL
S1869 Dapoxetine HCl 68 mg/mL 68 mg/mL 68 mg/mL
S3005 Paroxetine HCl 10 mg/mL 73 mg/mL 35 mg/mL
S1615 Risperidone <1 mg/mL 3 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
S2691 BMY 7378 92 mg/mL 92 mg/mL 20 mg/mL
S2112 Blonanserin <1 mg/mL <1 mg/mL <1 mg/mL
S1488 Naratriptan 22 mg/mL 74 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
S1345 Granisetron HCl 70 mg/mL 1 mg/mL 1 mg/mL
S2677 BRL-15572 <1 mg/mL 96 mg/mL 40 mg/mL
S1385 Mosapride Citrate <1 mg/mL 90 mg/mL <1 mg/mL
S1336 Fluvoxamine maleate <1 mg/mL 87 mg/mL 87 mg/mL
S2016 Mirtazapine <1 mg/mL 53 mg/mL 53 mg/mL
S2849 SB269970 HCl <1 mg/mL 11 mg/mL <1 mg/mL
S2894 SB742457 <1 mg/mL 78 mg/mL 2 mg/mL
S8010 PRX-08066 Maleic acid 104 mg/mL 104 mg/mL 98 mg/mL
S4109 Lorcaserin HCl 46 mg/mL 46 mg/mL 46 mg/mL
S1390 Ondansetron HCl 24 mg/mL 66 mg/mL 10 mg/mL
S2541 Clomipramine HCl 70 mg/mL 70 mg/mL 70 mg/mL
S3180 Eletriptan HBr <1 mg/mL 93 mg/mL <1 mg/mL
S3024 Lamotrigine <1 mg/mL 10 mg/mL 3 mg/mL
S4053 Sertraline HCl <1 mg/mL 69 mg/mL 15 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
S2106 Azasetron HCl 3 mg/mL <1 mg/mL <1 mg/mL
S2084 Duloxetine HCl <1 mg/mL 67 mg/mL <1 mg/mL
S4064 Escitalopram Oxalate 25 mg/mL 83 mg/mL <1 mg/mL
S2856 SB271046 <1 mg/mL 40 mg/mL <1 mg/mL
S1996 Ondansetron <1 mg/mL 0.1 mg/mL <1 mg/mL
S3183 Amitriptyline HCl 15 mg/mL 63 mg/mL 63 mg/mL
S2096 Almotriptan Malate <1 mg/mL 94 mg/mL 53 mg/mL
S4086 Loxapine Succinate <1 mg/mL 89 mg/mL 2 mg/mL
S4247 Prucalopride Succinate 97 mg/mL 97 mg/mL <1 mg/mL
S4259 Vilazodone HCl <1 mg/mL 96 mg/mL <1 mg/mL
S2669 LY310762 <1 mg/mL 0.4 mg/mL <1 mg/mL
S2582 Trazodone HCl <1 mg/mL 1 mg/mL <1 mg/mL
S4244 Serotonin HCl 43 mg/mL 43 mg/mL 2 mg/mL
S4256 Buspirone HCl 84 mg/mL 84 mg/mL 36 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
S3175 Atomoxetine HCl 2 mg/mL 58 mg/mL 37 mg/mL
S2025 Urapidil HCl 85 mg/mL 24 mg/mL 1 mg/mL
S2865 VUF 10166 <1 mg/mL 21 mg/mL 61 mg/mL
S4112 Desvenlafaxine Succinate <1 mg/mL 80 mg/mL <1 mg/mL
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
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