5-HT Receptors

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  1. 5-HT Receptor antagonist

    Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist.
  2. 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.
  3. 5-HT3 receptor antagonist

    Granisetron HCl is a serotonin 5-HT3 receptor antagonist
  4. 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.
  5. 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.
  6. 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.
  7. 5-HT Receptors/D2 dopamine receptor antagonist

    Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
  8. 5-HT Receptors antagonist

    Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting, often following chemotherapy.
  9. 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.
  10. 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.
  11. 5-HT Receptor antagonist

    LY310762 is a 5-HT1D-preferring receptor antagonist (EC50 = 31 nM).
  12. 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.

  13. 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.

  14. 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.

  15. 5-HT3 antagonist

    Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy.
  16. Serotonin 5HT3-receptor antagonist

    Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  17. 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.
  18. 5-HT antagonist

    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.
  19. D2/5-HT2 receptor antagonist

    Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
  20. 5-HT/dopamine D2 antagonist

    Ocaperidone is an effective antipsychotic agent.
  21. 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).
  22. 5-HT1A receptor antagonist

    NAD 299 hydrochloride (Robalzotan) is a selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro).
  23. 5-HT Receptor antagonist

    Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner.
  24. 5-HT1A receptor antagonist

    NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor.
  25. 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.
  26. 5-HT2C serotonin receptor antagonist

    N-Desmethylclozapine is a potent and selective 5-HT2C serotonin receptor antagonist
  27. 5-HT4 Receptor Antagonist

    SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist.
  28. 5-HT3 receptor antagonist

    Tropanserin acts as a potent and selective 5-HT3 receptor antagonist.
  29. 5-HT6 receptor antagonist

    SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects.
  30. 5-HT2 receptor antagonist

    Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations.
  31. 5-HT3 receptor antagonist

    Tropisetron 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.
  32. 5HT3-receptor antagonist

    Alosetron is s Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  33. 5-HT1C receptor antagonist

    Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro.
  34. 5-HT3 antagonist

    Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  35. 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.
  36. 5-HT/dopamine receptor antagonist

    Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  37. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.
  38. serotonin/histamine2 antagonist

    Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
  39. 5-HT3 receptor antagonist

    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.
  40. 5-HT1A receptor antagonist/COMT inhibitor

    Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor.
  41. 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.
  42. 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.
  43. 5-HT6 receptor antagonist

    SB 399885 hydrochloride is a potent, brain penetrant, and orally active SR-6 antagonist. It displays > 200-fold selectivity for SR-6 over other serotonin receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human SR-6 receptors, respectively).
  44. 5-HT1F antagonist

    LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). CAS: 199673-74-0(LY 334370 hydrochloride); 182563-08-2 (LY 334370 Free Base)
  45. 5-HT2A receptor antagonist

    Volinanserin is a highly selective 5-HT2A receptor antagonist.
  46. 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.
  47. 5-HT3 receptor antagonist

    Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist.
  48. 5-HT3 receptor antagonist

    Dolasetron mesylate is a selective 5-HT3 receptor antagonist.
  49. 5-HT1A receptor antagonist

    Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
  50. Serotonergic receptor antagonist

    (Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1.

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