autism

LIT-001 improves social interaction in a mouse model of autism.It is the first nonpeptide oxytocin receptor agonist with EC50 of 55 nM and Ki of 226 nM.

Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

TAK-418 is a selective and orally active inhibitor of LSD1/KDM1A enzyme with an IC50 of 2.9 nM. TAK-418 unlocks abnormal epigenetic mechanisms and improves autism symptoms in models of neurodevelopmental disorders.

N-Methylsarcosine (Dimethylglycine) is used as an athletic performance enhancer and immunostimulant. It is also used in the treatment of autism, epilepsy and mitochondrial disease. It is also employed as a biomarker of protein degradation in chronic obstructive lung disease (COPD) patients. Further, it is used as a substrate to identify, differentiate and characterize amino acid methyltransferase. It plays an important role in the development of glycine-based ionic liquids and emulsifiers.

LIT-001 free base improves social interaction in a mouse model of autism. LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM).

3-Hydroxyhippuric acid is an acylglycine compound and inhibits kynureninase (Ki = 60 μM).3-Hydroxyhippuric acid shows significantly higher in vivo concentrations in the autism model group compared with the control group.It is also a characteristic biomarker of Clostridium and is positively correlated with Clostridium abundance.In addition, 3-hydroxyhippuric acid is one of the major metabolites of catechin diets and wine polyphenol diets.

Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors. It is used for the research of autism.

GSK3-IN-9 (0713) is a selective inhibitor of glycogen synthase kinase 3 (GSK3). It holds potential for research into fragile X syndrome, attention deficit hyperactivity disorder (ADHD), childhood epilepsy, intellectual disabilities, diabetes, acute myeloid leukemia (AML), autism, and mental disorders.

KTD-092, a DYRK1A inhibitor, exhibits an IC50 of 22 nM against human DYRK1A. It is applicable in research related to Down syndrome (DS), Alzheimer's disease (AD), autism spectrum disorder (ASD), diabetes, and other neurodegenerative diseases.

LSD1-IN-49 hydrochloride (Compound (±)1) is an irreversible inhibitor of LSD1/KDM1A with an IC50 of 29 nM for hLSD1. It acts by forming an adduct with flavin adenine dinucleotide (FAD) in the binding pocket of LSD1, leading to irreversible inhibition of LSD1's enzymatic activity. This compound is applicable for research related to schizophrenia, autism spectrum disorder, and Huntington's chorea.

5-(2-aminoethyl)-4-methyl-1,3-thiazol-2-amine dihydrochloride is a potent and selective antagonist of metabotropic glutamate receptor 5 (mGluR5). It has been shown to be effective in several neurological disorders, including fragile X syndrome, autism spectrum disorders, and addiction.

N,N-Dimethylglycine hydrochloride (N-Methylsarcosine hydrochloride) is a dietary supplement used to improve autism spectrum disorders.

ARN23746 (IAMA-6) is a selective NKCC1 inhibitor with neuroprotective activity, used in the research of brain diseases including drug-resistant epilepsy (such as temporal lobe epilepsy TLE, Dravet syndrome DrS), autism spectrum disorder ASD, and Down syndrome DoS.

Dityrosine, an oxidation product of protein formed through the intermolecular cross-linking of tyrosyl radicals from the reactive oxygen species (ROS) and tyrosine interaction, is associated with decreased hippocampal expression of NMDA receptor subunits Nr1, Nr2a, and Nr2b when administered intragastrically at 320 µg/kg per day, leading to memory impairments in mice as evidenced by their performance in a novel object recognition test. Additionally, it raises fasting blood glucose levels while reducing plasma insulin levels and the pancreatic expression of insulin synthesis-related genes Ins2, Pdx1, and MafA. Increased dityrosine levels have been positively linked to a range of diseases, including autism spectrum disorder, cataracts, Alzheimer's disease, Parkinson's disease, atherosclerosis, and cystic fibrosis.

Compound 4h, also known as 5-HT7R antagonist 2, is a selective inhibitor of the 5-HT7R that disrupts both G protein and β-arrestin signaling pathways. It exhibits a K_i value of 67 nM, with IC_50 values of 2.59 μM in cAMP assays and 39.57 μM in Tango tests. This antagonist is noted for its potential to mitigate repetitive behaviors associated with autism spectrum disorder (ASD) and to foster the restoration of neurogenesis impaired by ASD [1]. Pharmacokinetic analysis in ICR male mice following intravenous and intraperitoneal administration shows a T_max of 0.08 hours and 0.25 hours, a T_1/2 of 0.77 hours and 1.06 hours, and a C_max of 33.07 ng/mL and 156.44 ng/mL, respectively. The AUC_last was recorded at 28.31 ng·h/mL and 143.27 ng·h/mL, with a clearance rate (CL) of 41.61 L/h/kg for intravenous administration. The volume of distribution at steady state (V_ss) was 32.43 L/kg, the mean residence time (MRT) was 0.79 hours and 0.93 hours, and the bioavailability (F) was calculated at 50.60% [1].

3-Hydroxyphenylacetic acid-d6 is the deuterium-labeled version of 3-Hydroxyphenylacetic acid. 3-Hydroxyphenylacetic acid is an orally bioavailable flavonoid metabolite produced by gut microbiota, known for its antihypertensive activity. It can inhibit ferroptosis by upregulating GPX4 expression, thus improving spermatogenic dysfunction in aged mice. Furthermore, abnormal levels of 3-Hydroxyphenylacetic acid are closely associated with some conditions, such as [autism spectrum disorder].

3-Hydroxyhippuric acid-d4 is the deuterium-labeled analogue of 3-Hydroxyhippuric acid. This compound is an acyl glycine, known for its ability to inhibit kynureninase in dogs with a Ki value of 60 μM. Higher concentrations of 3-Hydroxyhippuric acid have been observed in the experimental group with autism compared to the control group. It serves as a biomarker for Clostridia, showing a positive correlation with its levels. Additionally, 3-Hydroxyhippuric acid is a primary metabolite of catechin and wine polyphenol diets.

The synthetic compound me4 Peptide, designed from the microexon me4 sequence of the neuronal CPEB4 protein, can inhibit the aggregation of CPEB4 and is applicable in research on autism spectrum disorder-related conditions.

me4 Peptide acetate is a synthetic peptide designed based on the microexon 4 (me4) sequence from the neuronal CPEB4 protein. It inhibits CPEB4 aggregation and may be used in research related to autism spectrum disorders and schizophrenia.

NHIP peptide is a 20-amino acid segment located within the cell nucleus. It is highly expressed in neuron-derived cells such as LUHMES cells. Additionally, NHIP peptide promotes the proliferation of 293T cells and regulates gene networks associated with neurodevelopment and autism spectrum disorders (ASD).