5-HT Receptors

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  1. 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.
  2. SEP-363856, also known as SEP-856, is an orally active and CNS active psychotropic agent.
  3. 5-HT2A receptor antagonist

    Volinanserin is a highly selective 5-HT2A receptor antagonist.
  4. 5-HT1A receptor agonist

    Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  5. 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.
  6. 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.
  7. 5-HT1B/1D receptor agonist

    Eletriptan hydrobromide is a selective SR-1B/SR-1D agonist.
  8. 5-HT Receptor agonist

    Almotriptan malate (Axert) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.
  9. 5-HT2C serotonin receptor antagonist

    N-Desmethylclozapine is a potent and selective 5-HT2C serotonin receptor antagonist
  10. 5-HT Receptor agonist

    Prucalopride is a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements.
  11. 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.

  12. Risperidone(Risperdal) is an atypical antipsychotic used to treat schizophrenia (including adolescent schizophrenia), schizoaffective disorder, the mixed and manic states associated with bipolar disorder, and irritability in children with autism.
  13. Serotonin reuptake inhibitor

    Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.
  14. 5HT(1A) receptor agonist

    Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
  15. Duloxetine is a serotonin-norepinephrine reuptake inhibitor (SNRI). It is effective for major depressive disorder and generalized anxiety disorder (GAD).
  16. 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.
  17. 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.

  18. 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.
  19. 5-HT6R antagonist

    Lu AE58054 is a potent and selective 5-HT6 receptor antagonist.
  20. 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.
  21. 5-HT1A receptor agonist

    Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
  22. 5-HT3 receptor antagonist

    Pancopride is a new potent and selective 5-HT3 receptor antagonist.
  23. 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.
  24. 5-HT1B receptor agonist

    Eletriptan is a selective 5-hydroxytryptamine 1B/1D (5-HT1B) receptor agonist
  25. 5-HT1A receptor antagonist

    NAD 299 hydrochloride (Robalzotan) is a selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro).
  26. 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.
  27. 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.
  28. 5-HT Receptor antagonist

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

  30. 5-HT1A agonist

    BMY 7378 is a 5-HT1A partial agonist and high affinity α1D adrenoceptor antagonist.
  31. 5-HT3 antagonist

    Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy.
  32. 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.
  33. 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.
  34. Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
  35. 5-HT6 receptor antagonist

    SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
  36. serotonin transporter (SER) inhibitor

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  37. Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic (to treat nausea and vomiting). Ondansetron reduces the activity of the vagus nerve, which deactivates the vomiting center in the medulla oblongata, and also blocks serotonin receptors in the chemoreceptor trigger zone.
  38. Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA) . Structurally, mirtazapine can also be classified as a tetracyclic antidepressant (TeCA).
  39. Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor (SARI) class. It is a phenylpiperazine compound. Trazodone also has anti-anxiety (anxiolytic) and sleep-inducing (hypnotic) effects.
  40. Urapidil hydrochloride is an α1-adrenoceptor antagonist, 5-HT1A serotonin receptor partial agonist and anti-hypertensive.
  41. Duloxetine Hydrochloride is a dual serotonin and norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of stress urinary incontinence, as well as depression.
  42. 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.
  43. D2/5-HT2 receptor antagonist

    Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
  44. Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
  45. 5-HT7 receptor antagonist

    SB269970 is a potent and selective 5-HT7 receptor antagonist.
  46. 5-HT/dopamine D2 antagonist

    Ocaperidone is an effective antipsychotic agent.
  47. 5-HT2c receptor agonist

    PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1.
  48. 5-HT4 receptor antagonist

    5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6.
  49. 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).
  50. human 5-HT1A receptor agonist

    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.

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