GPCR / G Protein

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  1. SB 258585 HCl

    Catalog No. A14026
    5-HT6 serotonin receptor antagonist
    SB 258585 hydrochloride has been found to be a selective and potent SR-6 antagonist. This compound displays more than a 160-fold selectivity over other serotonin receptor subtypes. Learn More
  2. Granisetron

    Catalog No. A15096
    5-HT3 antagonist
    Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. Learn More
  3. LY 344864

    Catalog No. A15148
    5HT1F agonist
    LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor. Learn More
  4. WAY-100635 maleate salt

    Catalog No. A15282
    5HT1A antagonist
    WAY-100635 maleate is a potent and selective 5-hydroxytryptamine1A antagonist with an IC50 of 0.95 - 0.12 nM for 5-HT. Learn More
  5. Piboserod

    Catalog No. A15542
    5-HT4 receptor antagonist
    Piboserod is a selective 5-HT(4) receptor antagonist. Learn More
  6. Ricasetron

    Catalog No. A15499
    5-HT3 receptor antagonist
    Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor. Learn More
  7. LY278584

    Catalog No. A15500
    5-HT3 antagonist
    LY278584 is a potent and selective antagonist of 5-HT3 receptors. LY278584 is a useful ligand for studying the localization of 5-HT3 receptors in rat brain Learn More
  8. Lerisetron

    Catalog No. A15501
    5HT3 receptor antagonist
    Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. Learn More
  9. SB271046 HCl

    Catalog No. A15438
    5-HT Receptor Antagonist
    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. Learn More
  10. Pimavanserin (ACP-103)

    Catalog No. A14434
    5-HT2A receptor agonist
    Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay. Learn More
  11. Ketanserin tartrate

    Catalog No. A13664
    5HT2A antagonist
    Ketanserin tartrate is a salt of Ketanserin. Ketanserin is reported to have a high affinity for multiple G protein-coupled receptors, such as serotonin receptors. Learn More
  12. WAY 181187

    Catalog No. A14163
    5-HT6 agonist
    WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM. Learn More
  13. GSK163090

    Catalog No. A15838
    5-HT1A/B/D receptor antagonist
    GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively. Learn More
  14. Mosapride citrate

    Catalog No. A10607
    5-HT4-receptor agonist
    Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist. Learn More
  15. Tianeptine sodium

    Catalog No. A10931
    5-HT Receptor agonist
    Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE) in vitro and in vivo. Learn More
  16. Agomelatine

    Catalog No. A10048
    5-HT Receptor antagonist
    Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist. Learn More
  17. LY310762

    Catalog No. A11106
    5-HT Receptor antagonist
    LY310762 is a 5-HT1D-preferring receptor antagonist (EC50 = 31 nM). Learn More
  18. 5-Hydroxytryptophan (5-HTP) is a naturally occurring amino acid and chemical precursor as well as a metabolic intermediate in the biosynthesis of the neurotransmitters serotonin and melatonin from tryptophan. Learn More
  19. RS-127445

    Catalog No. A11165
    5-HT2B receptor antagonist

    RS-127445 is a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x selectivity over the closely related 5-HT2A and 5-HT2C receptors.

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  20. BRL-15572

    Catalog No. A11178
    5-HT1D receptor antagonist

    BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.

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  21. WAY-100635

    Catalog No. A11182
    5HT1A antagonist

    WAY-100635 was originally believed to act as a selective 5-HT1A receptor antagonist, but subsequent research showed that it also acts as potent full agonist at the D4 receptor.

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  22. BMY 7378

    Catalog No. A11208
    5-HT1A agonist
    BMY 7378 is a 5-HT1A partial agonist and high affinity α1D adrenoceptor antagonist. Learn More
  23. Naftopidil 2HCl

    Catalog No. A10619
    5-HT1A and α1-adrenergic receptor antagonist
    Naftopidil 2HCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively. Learn More
  24. Puerarin (Kakonein)

    Catalog No. A10759
    5-HT2C receptor antagonist
    Puerarin is one of several known isoflavones. Puerarin is a 5-HT2C receptor and benzodiazepine site antagonist. Puerarin is being investigated as a self-microemulsifying drug delivery system. Learn More
  25. Risperidone (Risperdal)

    Catalog No. A10797
    Risperidone(Risperdal) is an atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in children with autism. Learn More
  26. Tropisetron (ICS 205930)

    Catalog No. A11226
    5-HT3 antagonist
    Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy. Learn More
  27. Vilazodone

    Catalog No. A11116
    Serotonin reuptake inhibitor
    Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%). Learn More
  28. Duloxetine

    Catalog No. A11705
    Duloxetine is a serotonin-norepinephrine reuptake inhibitor (SNRI). It is effective for major depressive disorder and generalized anxiety disorder (GAD). Learn More
  29. Prucalopride

    Catalog No. A11771
    5-HT Receptor agonist
    Prucalopride is a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements. Learn More
  30. Alosetron

    Catalog No. A11310
    5-HT3 antagonist
    Alosetron is a 5-HT3 antagonist that an antagonist action on the 5-HT3 receptors of the enteric nervous system of the gastrointestinal tract. Learn More
  31. Naratriptan

    Catalog No. A10624
    5-HT1 receptor
    Naratriptan is a selective 5-HT1 receptor subtype agonist. Learn More
  32. SB269970 HCl

    Catalog No. A11925
    5-HT7 receptor antagonist
    SB269970 is a potent and selective 5-HT7 receptor antagonist. Learn More
  33. Ondansetron (Zofran)

    Catalog No. A11701
    Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic (to treat nausea and vomiting). Ondansetron reduces the activity of the vagus nerve, which deactivates the vomiting center in the medulla oblongata, and also blocks serotonin receptors in the chemoreceptor trigger zone. Learn More
  34. Mirtazapine

    Catalog No. A11702
    Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA) . Structurally, mirtazapine can also be classified as a tetracyclic antidepressant (TeCA). Learn More
  35. Trazodone HCl

    Catalog No. A11703
    Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor (SARI) class. It is a phenylpiperazine compound. Trazodone also has anti-anxiety (anxiolytic) and sleep-inducing (hypnotic) effects. Learn More
  36. Urapidil hydrochloride

    Catalog No. A11704
    Urapidil hydrochloride is an α1-adrenoceptor antagonist, 5-HT1A serotonin receptor partial agonist and anti-hypertensive. Learn More
  37. Duloxetine HCl

    Catalog No. A11717
    Duloxetine Hydrochloride is a dual serotonin and norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of stress urinary incontinence, as well as depression. Learn More
  38. Tegaserod maleate

    Catalog No. A11743
    Tegaserod functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist. Learn More
  39. Asenapine maleate

    Catalog No. A10091
    H1 antagonist
    Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors. Learn More
  40. Clomipramine HCl

    Catalog No. A10231
    5-HT Receptor agonist
    Clomipramine is a blocker of the following transporters:Serotonin transporter (SERT) (Ki = 0.14 nM),Norepinephrine transporter (NET) (Ki = 54 nM),Dopamine transporter (DAT) (Ki = 3,020 nM),Glycine transporter (GlyT/LeuT). Learn More
  41. Dapoxetine hydrochloride

    Catalog No. A10287
    Dapoxetine works by inhibiting serotonin transporter, increasing serotonins action at the post synaptic cleft, and as a consequence promoting ejaculatory delay. Learn More
  42. Citalopram Hydrobromide

    Catalog No. A10222
    Citalopram is a selective inhibitor of ST (5-hydroxytryptamine/serotonin transporter) and therefore is a potent and selective serotonin reuptake inhibitor. Learn More
  43. Ketanserin (Vulketan Gel)

    Catalog No. A10497
    5-HT2A serotonin receptor antagonist
    Ketanserin (Vulketan Gel) is specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A. Learn More
  44. Granisetron Hydrochloride

    Catalog No. A10437
    5-HT3 receptor antagonist
    Granisetron HCl is a serotonin 5-HT3 receptor antagonist Learn More
  45. Almotriptan malate (Axert)

    Catalog No. A11799
    5-HT Receptor agonist
    Almotriptan malate (Axert) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. Learn More
  46. Aripiprazole (Abilify)

    Catalog No. A11801
    5-HT1A receptor agonist
    Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. Learn More
  47. Mianserin hydrochloride

    Catalog No. A10588
    5-HT2/5-HT1 antagonist
    Mianserin hydrochloride is a 5-HT2/5-HT1 antagonist. Has moderate affinity for 5-ht6 Non-selective 5-HT2 receptor antagonist. Has moderate affinity for 5-HT6. Antidepressant. Learn More
  48. Lamotrigine

    Catalog No. A11873
    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. Learn More
  49. Eletriptan hydrobromide

    Catalog No. A11418
    5-HT1B/1D receptor agonist
    Eletriptan hydrobromide is a selective SR-1B/SR-1D agonist. Learn More
  50. 5-HT Receptor modulator
    Lu-AA21004 is an oral multimodal serotonergic agent, inhibits 5-HT(1A), 5-HT(1B), 5-HT(3A), 5-HT(7) and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Learn More

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