Schizophrenia

Flucindole is an orally active dopamine receptor inhibitor (IC₅₀ = 240 nM) that also exhibits affinity for S₂ receptors. Flucindole inhibits amphetamine-induced stereotyped behaviors in rats, and increases the levels of dopamine metabolites in the striatum of rats and mice. Flucindole can be used in the research of psychosis.

(Rac)-Ulotaront hydrochloride ((Rac)-SEP-363856 hydrochloride) is the racemate of Ulotaront hydrochloride (HY-136109). Ulotaront hydrochloride, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. Ulotaront has the potential for the treatment of schizophrenia.

SSR103800 is an orally active and selective glycine transporter-1 (GlyT1) inhibitor with an IC₅₀ of 2 nM for hGlyT1. SSR103800 elevates synaptic glycine levels by blocking GlyT1, thereby indirectly enhancing glutamate-NMDA receptor function. SSR103800 can be used for research on schizophrenia and depression.

M1/M4 muscarinic agonist 4 is a dual-site muscarinic acetylcholine receptor ligand with potent agonistic activity at M1/M4 muscarinic acetylcholine receptors. M1/M4 muscarinic agonist 4 activates M1R to induce phosphorylation of ERK1/2, and activates M4R to induce GαoB protein activation as well as ERK1/2 phosphorylation. M1/M4 muscarinic agonist 4 exhibits higher binding affinity for M4R than for other muscarinic receptors, while its binding affinity for the W435A mutant M4R is reduced. M1/M4 muscarinic agonist 4 can be used in the research of schizophrenia.

RBI257 is a selective dopamine D4R antagonist with a pK_i of 8.42 for the hD4.4 receptor. RBI257 acts as a competitive antagonist at the hD4.4 receptor, blocking dopamine-stimulated G protein activation and GIRK current activation. RBI257 can be used for research on hypertension and schizophrenia.

Methoxymethyl-MTEP is a selective, high-affinity mGluR5 antagonist. Methoxymethyl-MTEP can serve as a radiotracer ligand, readily entering the brain and providing mGluR5-specific signal in gray matter regions. Methoxymethyl-MTEP exhibits a K_d = 20 nM as measured by saturation binding assays in rat brain cell membranes, and an IC₅₀ = 30 nM in competitive binding assays. Methoxymethyl-MTEP can be used for research on diseases related to the glutamatergic nervous system, such as excitotoxicity and schizophrenia.

Norzotepine is the major human metabolite of Zotepine (HY-103093) and also a NET inhibitor (human IC₅₀ = 4.2 nM). Norzotepine exerts antipsychotic-like and antidepressant-like effects by inhibiting Norepinephrine (HY-13715) reuptake and blocking dopamine D₂ (Dopamine D₂), histamine H₁ (Histamine H₁), and 5-HT₂ receptors. Norzotepine can be used for research on schizophrenia.

trans-Flupentixol (trans-Flupenthixol) is an isomer of the orally active cis-flupenthixol (HY-184837) and Flupenthixol (HY-15856A) that modulates NMDA receptor subunits. trans-Flupentixol regulates the mRNA expression levels of NMDAR1 and NMDAR2A-D. trans-Flupentixol is used in schizophrenia-related research.

5-HT5A antagonist 1 is a 5-HT5A receptor antagonist. 5-HT5A antagonist 1 acts by blocking 5-HT5A-mediated serotonin signaling. 5-HT5A antagonist 1 can be used in research related to schizophrenia.

Vabicaserin (SCA-136 free base) is a brain-penetrant, orally active, and selective 5-HT_2C receptor agonist (K_i = 3 nM; EC₅₀ = 8 nM). Vabicaserin specifically activates Gq-coupled 5-HT_2C receptors to promote calcium mobilization, thereby selectively reducing dopamine release in the mesolimbic system without affecting the nigrostriatal pathway. Vabicaserin is an antagonist of 5-HT_2A/5-HT_2B receptors. Vabicaserin can be used for research on schizophrenia, obesity, chronic pain, and neurodegenerative diseases (such as Machado-Joseph disease).

M4R ligand-1 is a M4R ligand. M4R ligand-1 binds to the extracellular vestibular allosteric site of M4R. M4R ligand-1 can be used for the research of schizophrenia.

Dibenzepine-d₃ is the deuterated-labeled Dibenzepine (HY-12391). Dibenzepine is a blood-brain barrier permeable ligand of the histamine H1 receptor (Histamine H1 Receptor), with a K_i value of 0.02 μM. Dibenzepine exhibits varying degrees of affinity for multiple serotonin receptors and dopamine receptors. Dibenzepine can be used in research related to depression, schizophrenia, dementia, and non-specific agitation.

Dibenzepine hydrochloride is a blood-brain barrier permeable ligand of the histamine H1 receptor (Histamine H1 Receptor), with a K_i value of 0.02 μM. Dibenzepine hydrochloride exhibits varying degrees of affinity for multiple serotonin receptors and dopamine receptors. Dibenzepine hydrochloride can be used in research related to depression, schizophrenia, dementia, and non-specific agitation.

(D-Tyr11)-Neurotensin is an agonist of neurotensin receptor (Neurotensin Receptor) and an inhibitor of glutamatergic neurotransmission. Activation of NTR1 in the VTA by (D-Tyr11)-Neurotensin enhances glutamatergic inputs to non-dopaminergic neurons, mediating reward and dopamine efflux; meanwhile, activation of NTR2 reduces glutamatergic excitatory postsynaptic currents (EPSC) in dopaminergic neurons. (D-Tyr11)-Neurotensin can be used in studies related to schizophrenia.

BRD3290 is a GluA3-preferring AMPA receptor positive allosteric modulator with brain exposure in Mus musculus (mice) following peripheral administration. BRD3290 preferentially potentiates GluA3-containing AMPA receptors over GluA1/2-containing AMPA receptors. BRD3290 increases cerebellar cGMP levels in Mus musculus (mice). BRD3290 does not induce convulsions, alter motor function, or improve novel object recognition task performance in Mus musculus (mice) at tested doses. BRD3290 can be used for the research of schizophrenia.

HTL-9936 is an orally active partial agonist of muscarinic M1 receptor. HTL-9936 has an EC₅₀ of 32 nM for human M1 receptor and an EC₅₀ of 224 nM for human M4 receptor. HTL-9936 activates Gq/11 coupling, promotes inositol phosphate accumulation, ERK1/2 phosphorylation, β-arrestin recruitment and receptor internalization. HTL-9936 can be used in the research of Alzheimer's disease and schizophrenia.

NS-6740 hydrochloride is a silent agonist of α7 nicotinic acetylcholine receptor (α7 nAChR) with an IC₅₀ of 3 nM. NS-6740 hydrochloride reduces LPS-induced TNF-α release and regulates the cholinergic anti-inflammatory pathway. NS-6740 hydrochloride exerts anti-inflammatory effects. NS-6740 hydrochloride reduces long-term potentiation in hippocampal brain slices. NS-6740 hydrochloride can be used in research related to neuroinflammation and schizophrenia.

Methyl-2-bromo-LSD is a blood-brain barrier-penetrant serotonin 5-HT₂ receptor ligand and PET imaging agent that binds 5-HT₂ receptors with high affinity and achieves selective labeling of cortical regions. Methyl-2-bromo-LSD is useful for research on Alzheimer's disease, depression, schizophrenia, and anxiety disorders.

25N-N1-Nap is a blood-brain barrier-permeable, selective, β-arrestin2-biased 5-HT_2A receptor (5-HT_2AR) agonist. 25N-N1-Nap reduces Gq efficacy while preserving β-arrestin2 efficacy. 25N-N1-Nap does not induce hallucinogen-like behavioral responses, blocks hyperactivity induced by hallucinogens and psychostimulants, and induces rapid tolerance to hallucinogen-like responses. 25N-N1-Nap can be used for research on schizophrenia-related hyperactivity.

SYA16263 is a dopamine D₂ receptor (D₂R) and serotonin 1A receptor (5-HT_1AR) ligand, with K_i values of 1.24 nM and 0.67 nM for D₂R and 5-HT_1AR, respectively. SYA16263 stabilizes the inactive conformation of D₂R and 5-HT_1AR via interactions with specific amino acid residues in their orthosteric binding pockets, thereby blocking downstream signal transduction. SYA16263 can be used in research related to schizophrenia and psychosis.