5-HT Receptors

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Product Name
Application
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  1. 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%).
  2. Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
  3. 5-HT6 receptor antagonist

    SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
  4. 5-HT7 receptor antagonist

    SB269970 is a potent and selective 5-HT7 receptor antagonist.
  5. 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.
  6. 5-HT1B receptor agonist

    Eletriptan is a selective 5-hydroxytryptamine 1B/1D (5-HT1B) receptor agonist
  7. 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.
  8. 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).
  9. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  10. 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.
  11. Bifeprunox Mesylate is an antipsychotic compound through activation of the serotonin 5-hydroxytryptamine (5-HT)1A receptor.
  12. 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).
  13. 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.
  14. serotonin/NE reuptake inhibitor

    Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor.
  15. 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.
  16. 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.
  17. 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.
  18. 5-HT3 receptor antagonist

    Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.
  19. 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
  20. 5HT3 receptor antagonist

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

    MCI-225 is a selective NA reuptake inhibitor with 5-HT3 receptor antagonism.
  22. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.
  23. 5-HT1A/B/D receptor antagonist

    GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.
  24. 5HT(1A) receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
  25. 5-HT(2A) receptor agonist

    Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis.
  26. 5-HT3 receptor antagonist

    Dolasetron is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness.
  27. 5-HT6 receptor antagonist

    NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist with an IC50 of 7.2 nM, which also has a great binding affinity with Ki of 0.2 nM.
  28. 5-HT2A/α1-adrenergic receptor antagonist

    Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
  29. 5-HT3 partial agonist

    Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
  30. 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.
  31. 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).
  32. 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.
  33. SEP-363856, also known as SEP-856, is an orally active and CNS active psychotropic agent.

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