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.

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].

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

5HT6-ligand-2 (compound 15) is a potent 5-HT6 inhibitor with Ki values of 3.4 nM for 5-HT6 and 15 nM for SERT, demonstrating neuroprotective properties. It holds potential for research in dementia.

5-HT5AR/5-HT6R ligand-1 (Compound PP10) is a ligand for serotonin receptors, exhibiting high affinity for the 5-HT5A and 5-HT6 receptors with Ki values of 59 nM and 96 nM, respectively. It possesses some antiproliferative activity against tumor cells and can be utilized in cancer research.

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.

5-HT6R antagonist 3 (compound 15) is an effective and selective 5-HT6R antagonist capable of crossing the blood-brain barrier. It exhibits Ki values of 14 nM for 5-HT6, 3533 nM for 5-HT1A, 35 nM for 5-HT2A, and 1449 nM for 5-HT7. This compound demonstrates anxiolytic-like effects and possesses neuroprotective and cognitive-enhancing properties, indicating potential for Alzheimer's disease research.

5-HT6R antagonist 4 (compound 30) is a neutral antagonist of the 5-HT6 receptor, exhibiting a Ki value of 1 nM.

Compound 29 is a 5-HT6R antagonist that acts by inhibiting the 5-HT6 receptor.

5-HT1AR/5-HT6R ligand-1 (Compound PP13) functions as a ligand for the 5-HT receptor, demonstrating high affinity for 5-HT1AR, 5-HT6R, and 5-HT7R with Ki values of 19, 69, and 198 nM, respectively. In HEK293 cells, it inhibits cAMP production with EC50 values of 1535, 488, and 53 nM for these receptors. Additionally, 5-HT1AR/5-HT6R ligand-1 exhibits antiproliferative effects on several cancer cell lines, including 1321N1, U87MG, MCF7, and AsPC-1, with IC50 values of 9.6, 13.6, 19.3, and 14.6 μM, respectively. The compound also shows antagonistic activity towards the dopamine receptor D2R, with a Ki of 1903 nM.

5-HT6R/MAO-B modulator 1 is an antagonist of 5-HT6R (at Gs signaling) and an irreversible inhibitor of MAO-B that exhibits glial protective activity and induces scopolamine-induced memory deficits.

Compound 8 (5-HT6R antagonist 1), a 5-HT6R antagonist (K i : 5 nM), not only demonstrates inhibition of platelet aggregation and excellent metabolic stability but also reverses MK-801-induced memory impairments in rats, suggesting its utility in Alzheimer's disease (AD) research [1].

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.

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.

Rilapine (Rilapinum) is an antipsychotic compound that shows high affinity for 5-HT6 receptors and can be used to study neurological disorders.

AVN-322 is an orally active and specific 5-HT6R antagonist for the study of CNS disorders such as impaired memory and schizophrenia.

Landipirdine (RO-5025181) is a selective 5-HT6R antagonist for the study of central nervous system disorders such as 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.