5-HT Receptors

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  1. 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).
  2. 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.
  3. 5-HT6R antagonist

    Lu AE58054 is a potent and selective 5-HT6 receptor antagonist.
  4. 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.
  5. 5-HT1A receptor agonist

    Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
  6. 5-HT3 receptor antagonist

    Pancopride is a new potent and selective 5-HT3 receptor antagonist.
  7. 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.
  8. 5-HT1B receptor agonist

    Eletriptan is a selective 5-hydroxytryptamine 1B/1D (5-HT1B) receptor agonist
  9. 5-HT1A receptor antagonist

    NAD 299 hydrochloride (Robalzotan) is a selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro).
  10. 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.
  11. 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.
  12. 5-HT Receptor antagonist

    Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner.
  13. 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.
  14. norepinephrine (NE) transporter inhibitor

    Atomoxetine hydrochloride is a competitive and specific inhibitor of SLC6A2 while demonstrating weak ST and DAT inhibition as studied in synaptosomes of rat hypothalamus.
  15. serotonin uptake inhibitor

    Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively).
  16. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  17. 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.
  18. 5-HT3 Receptor Modulator

    PU 02 is a negative allosteric modulator of 5-HT3 receptors.
  19. 5-HT2C serotonin receptor antagonist

    N-Desmethylclozapine is a potent and selective 5-HT2C serotonin receptor antagonist
  20. 5-HT4 Receptor Antagonist

    SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist.
  21. 5-HT3 receptor antagonist

    Tropanserin acts as a potent and selective 5-HT3 receptor antagonist.
  22. 5-HT1A/1B and 5-HT2C agonist

    RU 24969 hemisuccinate is a potent 5-HT1A/1B and moderate 5-HT2C agonist that may also release 5-HT.
  23. Flibanserin is a new drug being investigated for the prevention of HSDD in woman.
  24. norepinephrine reuptake inhibitor

    Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor
  25. Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
  26. 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.
  27. Bifeprunox Mesylate is an antipsychotic compound through activation of the serotonin 5-hydroxytryptamine (5-HT)1A receptor.
  28. 5-HT6 receptor antagonist

    SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects.
  29. 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).
  30. 5-HT6 agonist

    WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM.
  31. 5-HT2 receptor antagonist

    Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations.
  32. 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.
  33. 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.
  34. serotonin/NE reuptake inhibitor

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  35. 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.
  36. 5HT3-receptor antagonist

    Alosetron is s Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  37. adrenergic receptor/5-HT receptor inhibitor

    Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  38. 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.
  39. 5-HT3 antagonist

    Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  40. 5HT1F agonist

    LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
  41. Quetiapine is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.
  42. 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.
  43. 5-HT/dopamine receptor antagonist

    Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  44. 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.
  45. serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  46. 5-HT3 receptor antagonist

    Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.
  47. 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
  48. 5HT3 receptor antagonist

    Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity.
  49. NA reuptake inhibitor

    MCI-225 is a selective NA reuptake inhibitor with 5-HT3 receptor antagonism.
  50. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.

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