5-ht6 receptor

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].

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 is a potent and selective antagonist of the 5-HT6 receptor with an IC50 of 7.2 nM.

NPS ALX Compound 4a dihydrochloride is a potent and selective antagonist of the 5-HT6 receptor with an IC50 of 7.2 nM.

SB-399885 hydrochloride is an antagonist of 5-HT6 receptor.

SB 243213 is an orally available and selective 5-HT2C receptor antagonist.SB 243213 has anxiolytic and antidepressant activity and is used in schizophrenia and movement disorders.

Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist that acts on D2 (Ki: 0.56 nM), D3 (Ki: 0.43 nM), and 5-HT2A (Ki: 0.6 nM) receptors, and also binds Alpha-1A adrenergic receptors. It can induce apoptosis, inhibit cancer cell proliferation, and is used to study psychiatric disorders, cancer, and inflammation.

Sarizotan 2HCl is an hERG channel inhibitor and 5-hydroxytryptamine 5-HT1A receptor agonist with potential antidepressant effects for the study of Parkinsonian movement disorders.

Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

Olanzapine (LY170053) is an atypical antipsychotic that is used currently in the treatment of schizophrenia and bipolar illness.

(E)-3,4,5-Trimethoxycinnamic acid (O-Methylsinapic acid) is a natural compound derived from the roots and rhizomes of Notopterygium incisum.

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).

SAX-187 (SAX-187) has high-affinity binding at the human 5-HT6 receptor.

PRX-07034 hydrochloride is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 hydrochloride is both a potent (Ki = 4-8 nM) and highly selective 5-HT(6) receptor antagonist (≥100-fold selectivity for the 5-HT(6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D(3) (Ki = 71 nM) and 5-HT(1B) (Ki = 260 nM) receptors.

Indophagolin is a potent, indoline-containing autophagy inhibitor with an IC50 of 140 nM, and it antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40, and 3.49 μM, respectively.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

Blonanserin (AD-5423) is an atypical antipsychotic approved in Japan in January, 2008. Relative to many other antipsychotics, blonanserin has an improved tolerability profile, lacking side effects such as extrapyramidal symptoms, excessive sedation, or hypotension.

Blonanserin is an antagonist of dopamine-D2 and serotonin-S2.

SB 243213 hydrochloride is an orally active, selective, high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor (pKi of 9.37 and pKb of 9.8), with an improved anxiolytic profile and potential for treating schizophrenia and motor disorders.

SB 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor.

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.