5-HT Receptors

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  1. NA reuptake inhibitor

    MCI-225 is a selective NA reuptake inhibitor with 5-HT3 receptor antagonism.
  2. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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).
  8. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  9. 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.
  10. 5-HT3 Receptor Modulator

    PU 02 is a negative allosteric modulator of 5-HT3 receptors.
  11. 5-HT4 Receptor Antagonist

    SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist.
  12. 5-HT3 receptor antagonist

    Tropanserin acts as a potent and selective 5-HT3 receptor antagonist.
  13. 5-HT1A/1B and 5-HT2C agonist

    RU 24969 succinate is a potent 5-HT1A/1B and moderate 5-HT2C agonist that may also release 5-HT.

  14. Flibanserin is a new drug being investigated for the prevention of HSDD in woman.
  15. norepinephrine reuptake inhibitor

    Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor
  16. 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).
  17. 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.
  18. Bifeprunox Mesylate is an antipsychotic compound through activation of the serotonin 5-hydroxytryptamine (5-HT)1A receptor.
  19. 5-HT6 receptor antagonist

    SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects.
  20. 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).

  21. 5-HT6 agonist

    WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM.
  22. 5-HT2 receptor antagonist

    Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations.
  23. 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.
  24. 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.
  25. serotonin/NE reuptake inhibitor

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  26. 5-Hydroxytryptophan (5-HTP) is a naturally occurring amino acid and chemical precursor as well as a metabolic intermediate in the biosynthesis of the neurotransmitters serotonin and melatonin from tryptophan.
  27. 5-HT Receptor antagonist

    Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist.
  28. Citalopram is a selective inhibitor of ST (5-hydroxytryptamine/serotonin transporter) and therefore is a potent and selective serotonin reuptake inhibitor.
  29. 5-HT Receptor agonist

    Clomipramine is a blocker of the following transporters:Serotonin transporter (SERT) (Ki = 0.14 nM),Norepinephrine transporter (NET) (Ki = 54 nM),Dopamine transporter (DAT) (Ki = 3,020 nM),Glycine transporter (GlyT/LeuT).
  30. Dapoxetine works by inhibiting serotonin transporter, increasing serotonins action at the post synaptic cleft, and as a consequence promoting ejaculatory delay.
  31. 5-HT3 receptor antagonist

    Granisetron HCl is a serotonin 5-HT3 receptor antagonist
  32. 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.
  33. 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.
  34. 5-HT4-receptor agonist

    Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist.
  35. 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.
  36. 5-HT1 receptor

    Naratriptan is a selective 5-HT1 receptor subtype agonist.
  37. 5-HT Receptors/D2 dopamine receptor antagonist

    Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
  38. 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.
  39. 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.
  40. 5-HT Receptor antagonist

    LY310762 is a 5-HT1D-preferring receptor antagonist (EC50 = 31 nM).
  41. Serotonin reuptake inhibitor

    Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 0.5 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60-70%).
  42. 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.
  43. 5-HT2/D1/D2 Antagonist

    Olanzapine-d3 is a deuterated form of olanzapine, targeting multiple receptors, including serotonin receptors 5-HT2A, 5-HT2C, and dopamine receptors D1 to D4. This selective and orally active monoaminergic antagonist exhibits high affinity binding with Ki values ranging from 4 to 57 nM for relevant targets. It is primarily utilized in research related to psychopharmacology and the treatment of schizophrenia and bipolar disorder, enabling detailed pharmacokinetic studies and investigation of receptor interactions.
  44. 5-HT2 Receptor Antagonist

    Cyproheptadine is a selective antagonist of the 5-HT2A receptor, exhibiting both antidepressant and antiserotonergic properties. In addition to its central nervous system effects, Cyproheptadine demonstrates antiplatelet and thromboprotective activities. This compound is valuable for research applications focused on thromboembolic disorders, contributing to the understanding of related vascular conditions.
  45. 5-HT1B/1D Agonist

    Zolmitriptan is a selective partial agonist of the 5-HT1B and 5-HT1D receptors, demonstrating high affinity with Ki values of 5.01 nM and 0.63 nM, respectively. It effectively crosses the blood-brain barrier, making it a valuable tool in migraine research. This compound is primarily utilized for studying the pathophysiology of migraines and developing targeted therapeutic interventions.
  46. 5-HT3 Receptor Antagonist

    Alosetron (Z)-2-butenedioate is a potent and selective antagonist of the serotonin 5-HT3 receptor. This compound is primarily utilized in research related to irritable bowel syndrome (IBS), demonstrating efficacy in blocking fast 5HT3-mediated depolarization in guinea pig myenteric and submucosal neurons, with an IC50 of approximately 55 nM. Additionally, Alosetron has been shown to reduce the visceral nociceptive response to rectal distension in both conscious and anesthetized canine models, indicating its potential for anti-inflammatory applications.
  47. 5-HT3 Antagonist

    Palonosetron is a selective 5-HT3 antagonist that effectively prevents acute, delayed, and overall chemotherapy-induced nausea and vomiting. In addition to its primary application in oncology, Palonosetron demonstrates moderate activity against flaviviruses and exhibits potent antiviral effects against Zika virus in mammalian cells. Furthermore, this compound has been associated with antidepressant properties, making it a valuable tool for diverse research applications in both oncology and virology.
  48. 5-HT3 Antagonist

    Palonosetron hydrochloride is a selective 5-HT3 receptor antagonist that primarily functions to prevent acute and delayed nausea and vomiting associated with chemotherapy. Beyond its primary application, Palonosetron hydrochloride demonstrates moderate activity against flaviviruses, including potent efficacy against the Zika virus in mammalian cells. Additionally, this compound has been associated with antidepressant effects, expanding its potential therapeutic applications in neurological research.
  49. 5-HT2C Receptor Agonist

    CP-809101 hydrochloride is a highly selective agonist of the 5-HT2C receptor, exhibiting pEC50 values of 9.96 for the human 5-HT2C receptor, along with lower activity at 5-HT2B and 5-HT2A receptors. This compound has been shown to inhibit conditioned avoidance responses in rodent models and effectively antagonizes PCP- and d-amphetamine-induced hyperactivity. Additionally, CP-809101 hydrochloride demonstrates potential in reducing food and nicotine dependence, making it a valuable tool for research in psychopharmacology and addiction studies.
  50. 5-HT Receptor Modulator

    Lurasidone Hydrochloride is a potent antagonist of both dopamine D2 and 5-HT7 receptors, exhibiting IC50 values of 1.68 nM and 0.495 nM, respectively. Additionally, it acts as a partial agonist at the 5-HT1A receptor with an IC50 of 6.75 nM. This compound is utilized in research focused on neuropharmacology and the treatment of psychiatric disorders, such as schizophrenia and bipolar disorder. Its selective modulation of serotonin and dopamine receptors makes it a valuable tool for investigating neurochemical pathways and therapeutic interventions.

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