5-HT Receptors

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  1. 5-HT3 Receptor Modulator

    PU 02 is a negative allosteric modulator of 5-HT3 receptors.
  2. 5-HT2C serotonin receptor antagonist

    N-Desmethylclozapine is a potent and selective 5-HT2C serotonin receptor antagonist
  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-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.
  6. Flibanserin is a new drug being investigated for the prevention of HSDD in woman.
  7. 5-HT6 receptor antagonist

    SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects.
  8. 5-HT6 agonist

    WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM.
  9. 5-HT2 receptor antagonist

    Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations.
  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-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.
  12. 5HT3-receptor antagonist

    Alosetron is s Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  13. 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.
  14. 5-HT3 antagonist

    Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  15. 5HT1F agonist

    LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
  16. Quetiapine is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.
  17. 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.
  18. 5-HT/dopamine receptor antagonist

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

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  20. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.
  21. 5-HT1E/5-HT1F receptor agonist

    BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
  22. 5-HT3 receptor inhibitor

    Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β.
  23. 5HT(1A) receptor agonist

    Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
  24. Serotonin2A Receptor Inverse Agonist

    Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson?€?s disease.
  25. serotonin/histamine2 antagonist

    Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
  26. 5-HT1A receptor agonist/serotonin reuptake inhibitor

    YL0919, a novel antidepressant candidate with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells were 1.78??0.34 nM and 1.93??0.18 nM respectively.
  27. Amitriptyline inhibits serotonin receptor, norepinephrine receptor, 5-HT4, 5-HT2 and sigma 1 receptor with IC50 of 3.45 nM, 13.3 nM, 7.31 nM, 235 nM and 287 nM, respectively.
  28. 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.
  29. Serotonin reuptake inhibitor

    Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.
  30. 5-HT1A receptor antagonist/COMT inhibitor

    Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor.
  31. Serotonin is a monoamine neurotransmitter that is biochemically derived from tryptophan and produced in serotonergic neurons in the central nervous system and in enterochromaffin cells in the gastrointestinal tract.
  32. 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.
  33. 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.
  34. 5-HT7 receptor agonist

    LP-211 is a a selective agonist of the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor.
  35. 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).
  36. 5-HT1F receptor agonist

    LY 344864 racemate is a 5-HT1F receptor agonist.
  37. 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)
  38. 5-HT2A receptor antagonist

    Volinanserin is a highly selective 5-HT2A receptor antagonist.
  39. 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.
  40. Harmine, also known as telepathine, is a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds. It occurs in a number of different plants, most notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi (also known as "yage" or "ayahuasca"). Harmine reversibly inhibits monoamine oxidase A (MAO-A), an enzyme which breaks down monoamines, making it a RIMA. Harmine selectively binds to MAO-A but does not inhibit the variant MAO-B.
  41. 5-HT3 receptor antagonist

    Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist.
  42. 5-HT2 receptors inhibitor

    Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test.
  43. 5-HT3 receptor antagonist

    Dolasetron mesylate is a selective 5-HT3 receptor antagonist.
  44. Serotonin receptors agonist

    Dihydroergotamine Mesylate, also known as DHE or Migranal, is an ergot alkaloid used to treat migraines. It has similar actions to the triptans, acting as an agonist to the serotonin receptors and causing vasoconstriction of the intracranial blood vessels, but also interacts centrally with dopamine and adrenergic receptors.
  45. 5-HT1A receptor antagonist

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

    (Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1.
  47. 5-HT receptor antagonist

    Pizotifen is a serotonin antagonist which acts mainly at the 5-HT1, 5-HT2A, and 5HT2C receptors with some antihistamine activity.
  48. 5-HT receptor /dopamine receptors antagonist

    Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
  49. Levomepromazine, also known as methotrimeprazine, is a phenothiazine neuroleptic drug. Levomepromazine is used for the treatment of psychosis, particularly those of schizophrenia, and manic phases of bipolar disorder.
  50. 5-HT1A receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone.

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