GPCR / G Protein

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  1. SB 258585 HCl

    Catalog No. A14026
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    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
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    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
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    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
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    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
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    5-HT4 receptor antagonist
    Piboserod is a selective 5-HT(4) receptor antagonist. Learn More
  6. Ricasetron

    Catalog No. A15499
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    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
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    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
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    5HT3 receptor antagonist
    Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity. Learn More
  9. SB271046

    Catalog No. A15438
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    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
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    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
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    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
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    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
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    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. Flopropione

    Catalog No. A16550
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    5-HT1A receptor antagonist/COMT inhibitor
    Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. Learn More
  15. MHP 133

    Catalog No. A20058
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    AChE /M1/M2/5HT4/I2 inhibitor
    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors. Learn More
  16. CP-809101

    Catalog No. A12481
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    5-HT2C receptor agonist
    CP-809101 is a potent and selective 5-HT2C receptor agonist with pEC50 of 9.96/7.19/6.81 for human 5-HT2C/5-HT2B/5-HT2A receptors respectively. Learn More
  17. Donitriptan

    Catalog No. A13145
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    5-HT1B/1D receptors agonist
    Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively. Learn More
  18. Deramciclane

    Catalog No. A13011
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    5-HT2A and 5-HT2C receptors antagonist
    Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist. Learn More
  19. YM348

    Catalog No. A12290
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    5-HT2C receptor agonist
    YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM). Learn More
  20. AP521

    Catalog No. A12280
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    human 5-HT1A receptor agonist
    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM. Learn More
  21. lumateperone Tosylate

    Catalog No. A12279
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    5-HT2A receptor antagonist
    Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). Learn More
  22. 5-HT4 antagonist 1

    Catalog No. A12268
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    5-HT4 receptor antagonist
    5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6. Learn More
  23. PRX933 hydrochloride

    Catalog No. A12261
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    5-HT2c receptor agonist
    PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1. Learn More
  24. Ziprasidone hydrochloride monohydrate

    Catalog No. A11008
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    5-HT (serotonin) and dopamine receptor antagonist
    Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. Learn More
  25. Pancopride

    Catalog No. A12967
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    5-HT3 receptor antagonist
    Pancopride is a new potent and selective 5-HT3 receptor antagonist. Learn More
  26. Lesopitron dihydrochloride

    Catalog No. A12950
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    5-HT1A receptor agonist
    Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. Learn More
  27. SB 271046 Hydrochloride

    Catalog No. A11573
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    5-HT6 receptor antagonist
    SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9. Learn More
  28. WAY-100635 Maleate

    Catalog No. A16787
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    5-HT1A receptor antagonist
    WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. Learn More
  29. Ziprasidone hydrochloride

    Catalog No. A16790
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    5-HT (serotonin)/dopamine receptor antagonist
    Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. Learn More
  30. Sarpogrelate hydrochloride

    Catalog No. A17295
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    5-HT2 antagonist
    Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Learn More
  31. RU 24969

    Catalog No. A20857
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    5-HT1A/5-HT1B receptors agonist
    RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors. Learn More
  32. Befiradol

    Catalog No. A21189
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    5-HT1A receptor agonist
    Befiradol (NLX-112) is a selective 5-HT1A receptor agonist. Learn More
  33. RS 127445

    Catalog No. A21256
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    5-HT2B receptor antagonist
    RS 127445 is a novel high affinity, selective 5-HT2B receptor antagonist with pKi of 9.5. Learn More
  34. Vortioxetine

    Catalog No. A21266
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    5-HT1A/5-HT1B/5-HT3A/5-HT7 receptor/SERT inhibitor
    Vortioxetine is a inhibitor of 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT, with Ki values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively. Learn More
  35. WAY 163909

    Catalog No. A21282
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    5-HT(2C) receptor agonist
    WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a Ki of 10.5??1.1 nM. Learn More
  36. SB 242084 Dihydrochloride

    Catalog No. A21349
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    5-HT2C receptor antagonist
    SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. Learn More
  37. Masupirdine mesylate

    Catalog No. A21409
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    5-HT6 receptor antagonist
    Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Learn More
  38. Nelotanserin

    Catalog No. A21506
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    5-HT2A inverse agonist
    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively. Learn More
  39. SB 242084

    Catalog No. A21715
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    5-HT2C receptor antagonist
    SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. Learn More
  40. LY 344864 S-enantiomer

    Catalog No. A21742
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    5-HT1F receptor agonist
    LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist. Learn More
  41. LY 344864 hydrochloride

    Catalog No. A21748
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    5-HT1F agonist
    LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM. Learn More
  42. Vilazodone D8

    Catalog No. A21876
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    SSR inhibitor / 5-HT1A receptor partial agonist
    Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist. Learn More
  43. SB-269970 hydrochloride

    Catalog No. A21889
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    5-HT7 receptor antagonist
    SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pKi of 8.3, exhibits >50-fold selectivity against other receptors. Learn More
  44. SB-224289 hydrochloride

    Catalog No. A21920
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    5-HT1B receptor antagonist
    SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect. Learn More
  45. Ritanserin

    Catalog No. A21976
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    5-HT2 receptor antagonist
    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors. Learn More
  46. Eplivanserin mixture

    Catalog No. A21987
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    serotonin reuptake inhibitor/5-HT2A receptor antagonist
    Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1. Learn More
  47. Ziprasidone D8

    Catalog No. A21989
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    5-HT / dopamine receptor antagonist
    Ziprasidone D8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. Learn More
  48. Aripiprazole (D8)

    Catalog No. A22004
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    human 5-HT1A receptor partial agonist
    Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. Learn More
  49. Mosapride citrate

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

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

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