Central nervous system diseases

PDE9-IN-(S)-C33 ((S)-C33) is a potent and selective inhibitor of PDE9 (IC50 = 11 nM). PDE9-IN-(S)-C33 can be used for central nervous system diseases and diabetes research.

CPPHA, a positive allosteric modulator of glutamate receptors mGluR5 and mGluR1, is commonly used in development for central nervous system diseases.

Antipsychotic agent 54 is a benzoylpiperidine compound that can be used in the study of central nervous system diseases such as psychosis and cognitive impairment.

Gedocarnil(ZK 113315) may be used to study diseases of the central nervous system.

AGI-43192 is a potent methionine adenosine transferase 2A (MAT2A) inhibitor that penetrates the blood-brain barrier. AGI-43192 inhibits S-adenosine methionine (SAM) production metabolic enzyme and methionine adenosine transferase 2A (MAT2A), which has the potential to study the role of SAM regulation in the central nervous system (CNS) and the treatment of cancer diseases.

Substance P Receptor Antagonist 1 has potential applications in treating gastrointestinal disorders, inflammatory diseases, respiratory conditions, and central nervous system disorders.

Natalizumab is a recombinant humanized monoclonal antibody and a humanized monoclonal antibody inhibitor that selectively targets α4 integrin (CD49d). Natalizumab binds to the α4β1 heterodimer and blocks its interaction with vascular cell adhesion molecule 1. Natalizumab also prevents lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses, and is used in the study of relapsing-remitting multiple sclerosis and Crohn’s disease. Natalizumab possesses anti-inflammatory and immunomodulatory activity, inhibiting the adhesion, retention, and transendothelial migration of immune cells, and reducing the infiltration of inflammatory cells into the central nervous system or affected sites. Natalizumab is also being studied for autoimmune or inflammation-related diseases such as B-cell lymphoma and non-infectious uveitis.

SLF is a synthetic ligand for FKBP12, which increases Ca2+ efflux and protein synthesis to improve skeletal muscle function, and is used in the study of central nervous system diseases and cancer.

Toladryl is a derivative of Diphenhydramine that can cross the blood-brain barrier and exhibits oral activity, with antihistamine and anticholinergic properties. Its anticholinergic effects are approximately a tenth of those seen with Diphenhydramine, yet it offers 2-4 times the protection against lethal doses of histamine in guinea pigs. The side effects of Toladryl are fewer and milder compared to Diphenhydramine; however, at higher doses, it may cause symptoms such as insomnia, agitation, and disorientation related to the central nervous system. Toladryl is utilized in the research of allergic diseases.

UNC10099984A (Compound 6) is a functionally selective ligand for the dopamine D2 receptor, exhibiting a Ki value of 4.6 nM and an EC50 of 6.2 nM for β-arrestin. This compound is useful for research into central nervous system diseases related to the D2 receptor.

CDKI-IN-1 (Compound SNX12) is an inhibitor of cyclin-dependent kinase inhibitory protein (CDKI) and is applicable in research related to degenerative diseases of the central nervous system.

HDAC6-IN-52 (EX.1) is a potent HDAC6 inhibitor, achieving a 100% inhibition rate at a concentration of 10 μM. It plays a significant role in central nervous system disorders, including neurodegenerative diseases such as Alzheimer's disease and progressive supranuclear palsy.

NRMA-9 is an amide prodrug of small molecule nuclear receptor modulators. It shows high exposure levels in the brain, indicating good penetration of the blood-brain barrier (BBB). NRMA-9 is utilized in research related to central nervous system diseases associated with nuclear receptors, such as Alzheimer's and Parkinson's.

NRMA-I is an amide prodrug of a small molecule nuclear receptor modulator. It demonstrates high brain exposure, indicating effective blood-brain barrier (BBB) penetration. NRMA-I is useful for research into central nervous system diseases related to nuclear receptors, such as Alzheimer's and Parkinson's diseases.

Tau ligand-1 (Compound 75) is a ligand of aggregated tau protein that can penetrate the blood-brain barrier. In tissues affected by Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 shows high affinity for aggregated tau protein, with equilibrium dissociation constants (KD) ranging from 1 to 3.8 nM. It holds potential as a positron emission tomography (PET) tracer for imaging studies of tau-related diseases within the central nervous system.

CCR5-IN-1 (compound 3ad) is an allosteric, selective inhibitor of CCR5 with an IC50 of 1.09 μM. It is applicable in research related to cardiovascular, central nervous system, immune system, and infectious diseases.

OT-R agonist 1 TFA (compound 5) is an oxytocin receptor (OT-R) agonist with an EC50 value of 0.39 nM. It exhibits V1A antagonist activity, with an EC50 value of 2432 nM, and can be utilized in studies related to central nervous system diseases.

CSF1R-IN-18 (Compound 16t) is an aniline derivative that acts as an inhibitor of the colony stimulating factor 1 receptor (CSF1R). It is applicable in research related to cancer, central nervous system disorders, and bone diseases.

5-HT2A receptor agonist-10 (Compound (R)-I-121.HCl) acts as a 5-HT2A receptor agonist with IC50 values of 2192.39 nM for h5-HT2A and 33.57 nM for h5-HT1A. It is applicable in research related to psychiatric disorders, mental illnesses, and central nervous system diseases.

UVI3502 is a cannabinoid receptor 1 (CB1) antagonist with an IC50 value of 4641 nM for CB1 and approximately 16200 nM for CB2. It can inhibit Gi/o protein coupling induced by the agonist CP55,940. UVI3502 shows potential for research into diseases related to the endocannabinoid system in the central nervous system, such as cognitive impairments and neurodegenerative disorders.

5-HT2A receptor agonist-11 (Compound I-69) is a 5-HT2A receptor agonist with an EC50 of 22 nM, and is applicable in research on psychiatric disorders or central nervous system diseases.

H3R antagonist 6 (Compounds 3) (H3-2406) is a histamine receptor 3 (H3R) antagonist with an IC50 of 5.6 nM. The 18F-labeled version exhibits high radiochemical yield, molar activity, and moderate brain uptake, although it shows off-target binding with the Sigma-1 receptor. It serves as a radioligand for positron emission tomography (PET) imaging in the study of central nervous system (CNS) diseases.

H3R antagonist 7 (compounds 4) is a histamine subtype 3 receptor (H3R) antagonist with a Ki value of 3.15 nM. It can potentially be used as a PET radioligand in the study of central nervous system (CNS) diseases.

LMD-902 is an analog of LMD-009 and acts as a CCR8 agonist with an EC50 of 15 nM. It exhibits excellent binding affinity, which is reliant on crucial residues such as PheVI:16. LMD-902 can be utilized in research for inflammatory conditions like bronchial asthma and central nervous system diseases such as multiple sclerosis.