5-HT Receptors

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  1. 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.
  2. 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.
  3. 5-HT4 Receptor Antagonist

    SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist.
  4. 5-HT3 receptor antagonist

    Tropanserin acts as a potent and selective 5-HT3 receptor antagonist.
  5. 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.
  6. 5-HT6 receptor antagonist

    SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects.
  7. 5-HT6 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).

  8. 5-HT2 receptor antagonist

    Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations.
  9. 5-HT6 receptor antagonist

    LuAE58054 is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia.
  10. 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.
  11. 5-HT Receptor antagonist

    Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist.
  12. 5-HT3 receptor antagonist

    Granisetron HCl is a serotonin 5-HT3 receptor antagonist
  13. 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.
  14. 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.
  15. 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.
  16. 5-HT Receptors/D2 dopamine receptor antagonist

    Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
  17. 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.
  18. 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.
  19. 5-HT Receptor antagonist

    LY310762 is a 5-HT1D-preferring receptor antagonist (EC50 = 31 nM).
  20. 5-HT6R antagonist

    Lu AE58054 is a potent and selective 5-HT6 receptor antagonist.
  21. 5-HT3 receptor antagonist

    Pancopride is a new potent and selective 5-HT3 receptor antagonist.
  22. 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.
  23. 5-HT1B receptor agonist

    Eletriptan is a selective 5-hydroxytryptamine 1B/1D (5-HT1B) receptor agonist
  24. 5-HT1A receptor antagonist

    NAD 299 hydrochloride (Robalzotan) is a selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro).
  25. 5-HT2B receptor antagonist

    PRX-08066, a Novel 5-Hydroxytryptamine Receptor 2B Antagonist, reduced monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats.
  26. 5-HT Receptor antagonist

    Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner.
  27. 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.
  28. 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.
  29. 5-HT1B receptor antagonist

    SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
  30. 5-HT2 receptor antagonist

    Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM.
  31. 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.
  32. 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.
  33. 5-HT3 receptor antagonist

    5-HT3 antagonist-4i is a 5-HT3 receptor antagonist which modulates the serotonergic system.
  34. 5-HT7 receptor antagonist

    AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders.
  35. 5-HT4 receptor antagonist

    SB203186 is potent 5-HT4 receptor antagonist.
  36. 5-HT7 receptor antagonist

    JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
  37. 5-HT3 antagonist

    RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
  38. 5-HT1B receptor antagonist

    SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
  39. 5-HT2/sigma 2 receptor antagonist

    Roluperidone, also known as MIN-101, CYR-101, and MT-210, is a 5-HT2A and sigma 2 receptor antagonist potentially for the treatment of schizophrenia.
  40. 5-HT2B receptor antagonist

    RS 127445 is a novel high affinity, selective 5-HT2B receptor antagonist with pKi of 9.5.
  41. 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.
  42. 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).

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