5-HT Receptors

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  1. 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).
  2. 5-HT4-receptor agonist

    Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist.
  3. 5-HT1 receptor

    Naratriptan is a selective 5-HT1 receptor subtype agonist.
  4. 5-HT Receptor agonist

    Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE) in vitro and in vivo.
  5. 5-HT1A agonist

    BMY 7378 is a 5-HT1A partial agonist and high affinity α1D adrenoceptor antagonist.
  6. 5-HT1B/1D receptor agonist

    Eletriptan hydrobromide is a selective SR-1B/SR-1D agonist.
  7. 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.
  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-HT1A receptor agonist

    Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  10. human 5-HT1A receptor agonist

    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
  11. 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.
  12. 5-HT6 agonist

    WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM.
  13. 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.
  14. 5HT1F agonist

    LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
  15. 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.
  16. 5HT(1A) receptor agonist

    Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.
  17. 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.
  18. 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.
  19. 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.
  20. 5-HT1F receptor agonist

    LY 344864 racemate is a 5-HT1F receptor agonist.
  21. 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.
  22. 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.
  23. 5-HT agonist

    8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
  24. 5-HT3 receptor selective agonist

    Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
  25. 5-HT1A/5-HT1B receptors agonist

    RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors.
  26. 5-HT1A/5-HT1B/5-HT1C agonist

    Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.
  27. 5-HT2A inverse agonist

    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
  28. 5-HT4 receptor partial agonist

    PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.
  29. 5-HT receptor agonist

    MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively).

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