Schizophrenia

Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine inhibits the membrane aggregation of NINJ1 and prevents plasma membrane rupture during cell death. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis.

Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a K_d of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca²⁺ flux.

Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with K_is of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM).

Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.

TP-10 is a selective PDE10A inhibitor with an IC₅₀ value of 0.8 nM. TP-10 shows an antioxidant activity with IC₅₀s of 31.72 and 16.04 μg/ml for DPPH and CUPRAC, respectively. TP-10 can be used for the research of neuropathy.

Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).

Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.

Piperacetazine is an orally active dopamine receptor antagonist and phenothiazine antipsychotic. Piperacetazine can directly bind to the PAX3::FOXO1 fusion protein and inhibit its transcriptional activity. Piperacetazine also exhibits antitumor activity with an IC₅₀ of 7.627 μM against PANC-1 cells. Piperacetazine can be used for the research of diseases such as schizophrenia and pancreatic cancer and other tumors.

Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication. Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

ZH8651 is an orally active TAAR1 agonist. ZH8651 activates the Gs and Gq signaling pathways. ZH8651 alleviates dizocilpine-induced hyperactivity, improves prepulse inhibition deficits, and attenuates cognitive impairment in mice. ZH8651 can be used for the research of schizophrenia.

Vabicaserin hydrochloride (SCA-136) is a brain-penetrant, orally active, and selective 5-HT_2C receptor agonist (K_i = 3 nM; EC₅₀ = 8 nM). Vabicaserin hydrochloride 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 hydrochloride is an antagonist of 5-HT_2A/5-HT_2B receptors. Vabicaserin hydrochloride can be used for research on schizophrenia, obesity, chronic pain, and neurodegenerative diseases (such as Machado-Joseph disease).

Pterin is a pteridine with antibacterial activity. Pterin binds to the Fe²⁺ active site via its carbonyl group, reducing the oxygen activation energy barrier in hydroxylases. Pterin participates in metabolic redox processes. Pterin can be used in research related to cancer, vitiligo, bacterial infections, phenylketonuria, Parkinson's disease, schizophrenia and depression.

Petunidin chloride is an anthocyanin and also a pentoside (PEN) synthesis inhibitor. Petunidin chloride directly inhibits the synthesis of PEN without degrading or sequestering already synthesized PEN. Petunidin chloride can be used in studies related to PEN accumulation and advanced glycation associated with schizophrenia.

GSK239512 is a blood-brain barrier-permeable, orally active H3 receptor antagonist, with a human pK_i ranging from <5.5 to 9.92 and a murine pK_i ranging from 9.44 to 9.83. GSK239512 modulates cholinergic and monoaminergic neurotransmission, blocks the inhibitory feedback of H3 receptors, and increases the release of pro-cognitive neurotransmitters. GSK239512 induces oligodendrocyte precursor cell differentiation and restores myelin gene expression at the cellular level. GSK239512 reverses Scopolamine (HY-N0296)-induced memory deficits and improves recognition memory in animal models. GSK239512 can be used in research related to Alzheimer's disease, chronic traumatic encephalopathy, relapsing-remitting multiple sclerosis, and schizophrenia.

SR 142948A is a blood-brain barrier-permeable, orally active, selective, non-peptide Neurotensin Receptor antagonist. SR 142948A exhibits an IC₅₀ of 4.0 nM at the NTS1 site. SR 142948A competitively antagonizes neurotensin-dependent neurotransmitter release and modulates neurotensin-related dopaminergic and serotonergic signaling, making it useful for research on neurobehavioral mechanisms associated with schizophrenia.

DQP-1105 is a potent and selective NMDA receptor antagonist. DQP-1105 inhibits NMDA receptors containing GluN2C and GluN2D with IC₅₀ values of 7.0 and 2.7 μM, respectively, and shows weaker inhibitory activity against receptors containing GluN2A or GluN2B. DQP-1105 exhibits higher affinity after the receptor binds glutamate, and inhibits high-frequency excitatory synaptic transmission by altering receptor gating kinetics or prolonging deactivation time. DQP-1105 can be used in research on epilepsy, depression, schizophrenia, and fragile X syndrome.

AA43279 is an orally effective, blood-brain barrier-penetrant Nav1.1 voltage-gated sodium channel activator with an EC₅₀ of 9.5 μM in HEK-293 cells. AA43279 inhibits fast inactivation and enhances sodium conductance. AA43279 can be used in research on schizophrenia and Dravet syndrome.

MK-212 monohydrochloride (CPP monohydrochloride) is an orally active, blood-brain barrier permeable agonist of 5-HT₁C, 5-HT₂ and 5-HT₁A receptors. MK-212 monohydrochloride induces hyperthermia, nausea, arousal, irritability and restlessness, inhibits the elevation of plasma cortisol and prolactin, and reduces feelings of calmness and overall positive affect. MK-212 monohydrochloride mediates anxiety-like behaviors and motor inhibition. MK-212 monohydrochloride is applicable to research related to schizophrenia and anxiety disorders.

5-Iodo-A-85380 dihydrochloride (5-I A-85380 dihydrochloride) is a blood-brain barrier-permeable selective ligand for α4β2 nicotinic acetylcholine receptors (nAChR). The K_i of 5-Iodo-A-85380 dihydrochloride binding to rat α4β2 nAChRs is 0.01 nM. 5-Iodo-A-85380 dihydrochloride activates receptor currents, elicits single-channel currents, and promotes calcium influx, dopamine release, and calcium-dependent neuroprotection, acting as a full agonist at high-sensitivity α4β2 and a partial agonist at low-sensitivity α4β2 and α6-containing nAChRs. 5-Iodo-A-85380 dihydrochloride can be used for research on glutamate-induced neurotoxicity, pain, Alzheimer's disease, Parkinson's disease, schizophrenia, and attention deficit hyperactivity disorder.

Olanzapine N-oxide is a phase I metabolite of Olanzapine (HY-14541). Olanzapine N-oxide serves as a substrate for reduction reactions and converts to Olanzapine in whole blood in vitro. Olanzapine is an antipsychotic compound widely used in research on schizophrenia and other psychotic disorders.