5-HT Receptors

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  1. 5HT3 receptor antagonist

    Lerisetron is a serotonin type 3 (5-HT3) receptor antagonist with antiemetic activity.
  2. 5-HT4 receptor antagonist

    Piboserod is a selective 5-HT(4) receptor antagonist.
  3. 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.
  4. serotonin/histamine2 antagonist

    Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
  5. 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.
  6. 5-HT1A receptor antagonist/COMT inhibitor

    Flopropione is a 5-HT1A receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor.
  7. 5-HT1A receptor antagonist

    WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM.
  8. 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.
  9. 5-HT6 receptor 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).
  10. 5-HT1F antagonist

    LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). CAS: 199673-74-0(LY 334370 hydrochloride); 182563-08-2 (LY 334370 Free Base)
  11. 5-HT2A receptor antagonist

    Volinanserin is a highly selective 5-HT2A receptor antagonist.
  12. 5-HT2 antagonist

    Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD.
  13. 5-HT3 receptor antagonist

    Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist.
  14. 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.
  15. 5-HT3 receptor antagonist

    Dolasetron mesylate is a selective 5-HT3 receptor antagonist.
  16. 5-HT1A receptor antagonist

    Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
  17. Serotonergic receptor antagonist

    (Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1.
  18. 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.
  19. 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.
  20. 5-HT6R antagonist

    AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
  21. 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.
  22. 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).
  23. 5-HT1B receptor antagonist

    AR-A 2 is a selective 5-HT1B receptor antagonist.
  24. 5-HT3 /5-HT4 receptor dual antagonist

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

    Irindalone is a novel serotonin 5-HT2 antagonist.
  26. 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).
  27. 5-HT2A/α1-adrenergic receptor antagonist

    Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
  28. 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.
  29. 5-HT7 receptor antagonist

    JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
  30. 5-HT3 antagonist

    RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
  31. 5-HT1B receptor antagonist

    SB-616234A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
  32. 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.
  33. 5-HT2B receptor antagonist

    RS 127445 is a novel high affinity, selective 5-HT2B receptor antagonist with pKi of 9.5.
  34. 5-HT2C receptor antagonist

    SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
  35. 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).
  36. 5-HT2C receptor antagonist

    SB 242084 is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.
  37. 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.
  38. 5-HT1B receptor antagonist

    SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
  39. 5-HT2 receptor antagonist

    Eplivanserin is a potent, selective and orally available 5-HT2 receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM.
  40. 5-HT2 receptor antagonist

    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
  41. serotonin reuptake inhibitor/5-HT2A receptor antagonist

    Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1.
  42. 5-HT / dopamine receptor antagonist

    Ziprasidone D8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  43. 5-HT3 receptor antagonist

    5-HT3 antagonist-4i is a 5-HT3 receptor antagonist which modulates the serotonergic system.
  44. 5-HT7 receptor antagonist

    AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders.
  45. 5-HT4 receptor antagonist

    SB203186 is potent 5-HT4 receptor antagonist.

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