htrα

GC 14 is a selective thyroid hormone receptor antagonist with IC50 values of 200 nM for hTRα and 35 nM for hTRβ.

HTR2A antagonist 1 (Compound 15f) is an HTR2A antagonist with an IC50 of 42.79 nM. It induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells by activating the p53/p21/caspase 3 signaling pathway. HTR2A antagonist 1 exhibits good liver microsomal stability and is useful for colorectal cancer research.

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist with weak α1 adrenoceptor blocking activity.

Mavatrep (JNJ-39439335) is a selective antagonist of TRPV1 with Ki of 6.5 nM and can be used for studies about inflammatory pain.

Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Tabernanthalog (TBG) is a 5-HT2A agonist. In rodents,Tabernanthalog has been found to promote structural neuroplasticity, reduce alcohol-seeking and heroin-seeking behavior, and produce antidepressant effects.

TREM2 agonist-2 (I-192) is an orally active and potent agonist of myeloid triggered receptor 2 (TREM2) for neurodegenerative disease research.

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

QF0301B is a potent α1-adrenergic receptor antagonist with inhibitory effects on α2-adrenergic receptors, 5-HT2A and histamine H1 receptors.

5-HT3 antagonist 3 (Compound 15b) is a high-affinity 5-HT3 receptor antagonist that binds to 5-HT3 receptors in rat brain cortical membranes (Ki: 0.25 nM).

5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

5-HT7 agonist 1 (4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole) is a selective agonist of 5-HT7 (IC50 = 222.93 nM). 5-HT7 agonist 1 can be used in studies about CNS disorders.

Adoprazine (SLV313) is a potential atypical antipsychotic bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties.

Agomelatine (L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2), and Agomelatine (S-20098). L(+)-Tartaric acid also functions as a selective 5-HT2C receptor antagonist (pKis: 6.4 and 6.2 at native porcine and cloned human 5-HT2C receptors), actively supporting research into melatonergic signaling pathways, receptor-mediated regulation, and novel psychiatric therapeutics by enabling precise modulation of circadian and serotonergic systems in cellular models to improve neuropharmacological understanding and experimental reproducibility across neuroscientific and clinical translational studies.

Befiradol (NLX-112) is an agonist of 5-HT1A receptor.

5-HT2A antagonist 1 is a 5-HT2A receptor blocker that may be useful in treating gastrointestinal and circulatory disorders.

cis-Urocanic acid ((E)-Urocanic acid) is a 5-HT2A receptor agonist (Kd: 4.6 nM). It is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists.

Donitriptan is a 5-HT receptor agonist with pKis of 9.4 and 9.3 for 5-HT1B and 5-HT1D, respectively.

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

IrindaloneIrindalone is a potent serotonin (5-HT2) antagonist.

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.