5-HT Receptors

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  1. Serotonergic receptor antagonist

    (Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 5HT(1A) receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
  9. serotonin/histamine2 antagonist

    Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
  10. 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.
  11. 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.
  12. 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.
  13. 5-HT1A receptor antagonist/COMT inhibitor

    Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor.
  14. 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.
  15. 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.
  16. 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.
  17. 5-HT6 receptor antagonist

    SB 399885 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).

  18. 5-HT6R antagonist

    AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
  19. combined Ca2+/5-HT2 antagonist

    Nexopamil racemate is the racemate of Nexopamil. Nexopamil is a combined Ca2+/5-HT2 antagonist on thrombus formation in vivo and on platelet aggregation in vitro.
  20. 5-HT2 receptor antagonist

    Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
  21. 5-HT6 agonist

    EMDT oxalate is a selective 5-HT6 agonist, and has antidepressant effects.
  22. 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.
  23. 5-HT1B/1D receptors agonist

    Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK?293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
  24. 5-HT4 receptor antagonist

    Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
  25. SERT inhibitor

    DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
  26. 5-HT1B receptor antagonist

    AR-A 2 is a selective 5-HT1B receptor antagonist.
  27. AChE /M1/M2/5HT4/I2 inhibitor

    MHP 133 is a drug with multiple CNS targets, and inhibits acetylcholinesterase (AChE) with Ki of 69 μM; also active against muscarinic M1 and M2 receptors, serotonin 5HT4 receptors, and imidazole I2 receptors.
  28. 5-HT7 receptor agonist

    5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC50 of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders.
  29. 5-HT3 /5-HT4 receptor dual antagonist

    FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist.
  30. serotonin 5-HT2 antagonist

    Irindalone is a novel serotonin 5-HT2 antagonist.
  31. 5-HT6 receptor antagonist

    Masupirdine free base (SUVN-502 free base) 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-HT2A/α1-adrenergic receptor antagonist

    Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
  33. 5-HT2A/dopamine D2 antagonist

    Abaperidone is a potent antagonist of 5-HT2A?receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
  34. 5-HT1A modulator

    5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
  35. 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).
  36. 5-HT1 receptor modulator

    NEO 376 is a selective modulator of 5-HT1 receptor, GABA receptor and dopamine receptor, with anti-psychotic actively.
  37. 5-HT2C receptor-selective agonist

    Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
  38. triple reuptake inhibitor/5-HT2A/5-HT2C/5-HT3/α1A-adrenergic receptor antagonis

    Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist.
  39. 5HT3-receptor antagonist

    Alosetron is s Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.
  40. 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.
  41. 5-HT3 antagonist

    Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  42. 5HT1F agonist

    LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
  43. Quetiapine is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.
  44. 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.
  45. 5-HT/dopamine receptor antagonist

    Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  46. 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.
  47. serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  48. 5-HT3 receptor antagonist

    Ricasetron is a drug which acts as a selective antagonist at the serotonin 5-HT3 receptor.
  49. 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
  50. 5HT3 receptor antagonist

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

Items 51-100 of 899

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