5-ht6

5-HT6/7 antagonist 1 is a dual 5-HT6/7/2A and D2 receptor antagonist used in the study of dementia and Alzheimer's disease.

5HT6-ligand-1 is an orally active ligand of 5-HT6 receptor (Ki = 1.43 nM).

NPS ALX Compound 4a hydrochloride(1:1) is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM.

EMDT oxalate, a selective 5-HT6 agonist, exhibits antidepressant effects.

Masupirdine free base (SUVN-502 free base) is an orally available 5-HT6 receptor antagonist that crosses the blood-brain barrier, with a Ki value of 2.04 nM for the human 5-HT6 receptor. It is potent and selective, inhibiting multiple targets, and can be used in the study of neurological disorders such as Alzheimer's disease.

Masupirdine mesylate (SUVN-502 mesylate) is a selective 5-HT6 receptor antagonist that crosses the blood-brain barrier and is utilized in the study of neurological disorders such as Alzheimer's disease and dementia.

E6801 is a novel selective 5-HT6 receptor agonist with a wide range of biological activities.E6801 can be used in the study of dementia, Parkinson's disease, depression, obesity epilepsy, anxiety, and many other diseases.

AVN 322 free base is an orally available, selective and potent 5-HT6R antagonist for the study of neuropathic system disorders such as Alzheimer's disease (AD) and schizophrenia.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Chlorprothixene (Truxal) is a typical antipsychotic drug of the thioxanthene class, which was the first of the series to be synthesized.

Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM).

Cerlapirdine (PF-05212365) is a selective, potent, full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine is already in clinical development for the treatment of cognitive disorders related to Alzheimer's disease and schizophrenia. It works by acting as a selective 5-HT6 receptor antagonist.

Intepirdine (GSK-742457) is a highly selective 5-HT6 receptor antagonist, used in trials studying the treatment of Alzheimer's Disease.

SB 258585 is a selective 5-HT6 receptor antagonist.SB 258585 has a high affinity for individual receptor populations in cell lines with human recombinant 5-HT6 receptors.SB 258585 can be used to label both recombinant and natural 5-HT6 receptors, and can be used to assay cognitive enhancement and antipsychotic activity.

ST1936 (ST 1936 oxalate) is a selective and highly potent 5-HT6 receptor agonist that inhibits human 5-HT6, 5-HT7 and 5-HT2B receptors by fully activating cloned human 5-HT6 receptors. body to stimulate cAMP, Ca2+, ERK1/2 and Fyn kinase.

SB 271046 hydrochloride (SB 271046A) is selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.35, 6.55, 6.27 at 5-HT6, 5-HT1A, 5-HT1D and D3, and 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. It increases extracellular aspartate and glutamate in the frontal cortex and exhibits anticonvulsant activity (EC50: 0.16 μM).

AVN-49 is a potent and selective 5-HT6R Antagonist (Ki: 91 pM).

5-HT6 inverse agonist 1 (Compound 33) is an antagonist of the 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. This compound can inhibit 5-HT6R-mediated Cdk5 and mTOR signaling pathways and reduce tactile allodynia induced by spinal nerve ligation (SNL) in rat models.

5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors, exhibiting K i values of 2 nM and 11 nM for the respective receptors, holding promise for research in neurological and psychiatric disorders [1].

Compound 42, a 5-HT6/5-HT2A receptor ligand-2, serves as a dual antagonist for the 5-HT6 and 5-HT2A receptors with Ki values of 25 nM and 32 nM, respectively. This brain-penetrant compound exhibits pro-cognitive properties [1].

5-HT6/5-HT2AR antagonist-1 is a potent dual antagonist for the 5-HT6 and 5-HT2A receptors, demonstrating high efficacy with K_i values of 11 nM and 39 nM, respectively [1].

Compound 19, a 5-HT6 agonist with an affinity (K i : 5 nM), exhibits antidepressant-like effects and enhances cognitive function while also inhibiting platelet aggregation. It demonstrates high metabolic stability [1].

5-HT6R antagonist 6 (Compound PP15) exhibits high affinity and selectivity for the 5-HT6R receptor, with a Ki of 42 nM. It demonstrates weak antiproliferative activity on tumor cells and low toxicity toward normal cells. 5-HT6R antagonist 6 is applicable in tumor research.