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.

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.

UK-78282 is a K_V1.3 channel inhibitor with an IC₅₀ value of 0.20 μM and a K_d of 0.39 μM. UK-78282 also inhibits the Kv1.4 Potassium Channel. UK-78282 blocks KV1.3 in a use-dependent manner and inhibits human T lymphocyte activation by regulating the cell cycle. UK-78282 can be used in research related to mental disorders, such as depression and schizophrenia.

5-HT2AR ligand-2 is a serotonin 2A receptor (5-HT_2AR) ligand with a K_i value of 11.4 nM. 5-HT2AR ligand-2 stabilizes the inactive conformation of receptors by interacting with specific amino acid residues in the orthosteric binding pockets of D₂R and 5-HT_2AR, thereby blocking downstream signal transduction. 5-HT2AR ligand-2 can be used in studies related to schizophrenia.

DR/5-HT7AR Ligand-1 is a ligand with a K_i value of 1.24 nM against human D2R, 5.78 nM against human D3R, 0.67 nM against human 5-HT1AR, and 19.9 nM against human 5-HT7AR. DR/5-HT7AR Ligand-1 can be used for the research of schizophrenia.

NMDAR modulator 3 is a subunit-selective NMDA receptor potentiator targeting NMDAR receptors containing NR2C/NR2D subunits. NMDAR modulator 3 can be used for the research of schizophrenia, parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, neurodegeneration.

VU6052959 (BI’7927) is an orally active, blood-brain barrier-penetrant mGlu3 modulator with an EC₅₀ of 36 nM in humans and 16 nM in rats. VU6052959 enhances recognition memory and reverses cognitive impairment in male rats. VU6052959 can be used in the research of schizophrenia.

NK3R antagonist-2 (Compound 45) is a small-molecule antagonist of tachykinin NK3R, with an IC₅₀ of 1100 nM and a K_i of 1800 nM. NK3R antagonist-2 can be used in the research of schizophrenia.

VU6066098 is a blood-brain barrier penetrant, orally active inhibitor of metabotropic glutamate receptor subtype 2 (mGlu2), with IC₅₀ values of 77 nM and 111 nM against human and rat targets, respectively. VU6066098 induces antidepressant-like activity, inhibits psychosis-like hyperlocomotion, enhances recognition memory and associative learning, and reverses cognitive deficits caused by blast-related traumatic brain injury. VU6066098 can be used in research on major depressive disorder, schizophrenia, Alzheimer's disease, and traumatic brain injury.

trans-(3R)-Rimcazole (trans-(3R)-BW 234U) is an antipsychotic agent. trans-(3R)-Rimcazole reduces drug-induced aggressive behavior in rats and exhibits antipsychotic activity. trans-(3R)-Rimcazole can be used for the research of psychosis.