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.

hMAO-B-IN-5 is a potent reversible and selective human monoamine oxidase hMAO-B inhibitor (IC50:0.12μM). hMAO-B-IN-5 can cross the blood-brain barrier and can be used in the study of Parkinson's disease. It is a promising compound in the treatment and diagnosis of central nervous system diseases.

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

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.

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.

AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective positive modulator of Nav1.1 channels and also increases the activity of Nav1.2 and Nav1.5 channels while not affecting Nav1.4, Nav1.6, and Nav1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Nav1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al[1].

Zagociguat (CY6463) is a soluble guanylate cyclase stimulator with central nervous system penetrance, enhancing nitric oxide (NO) signaling and used in the study of neurological diseases.

PNU-282987 (free base) is a potent agonist of α7 nicotinic acetylcholine receptor (nAChR) with an EC50 of 154 nM and a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. It can be used for central and peripheral nervous system studies[1].

Laquinimod (ABR-215062) sodium is a carboxamide derivative administered orally that serves as a powerful immunomodulator, designed to prevent inflammation and neurodegeneration within the central nervous system. This compound effectively diminishes the activation of astrocytic NF-κB, offering protection against Cuprizone-induced demyelination. It shows promise for the treatment of both relapsing-remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS), in addition to its potential applications in the study of neurodegenerative diseases [1] [2] [3] [4].

AZ3391 is a quinoxaline derivative that is a potent inhibitor of PARP. AZ3391 has potential for the study of diseases and conditions occurring in central nervous system tissues (e.g., brain and spinal cord).

S1P receptor agonist 2 (compound 1) is a selective agonist of the S1P5 receptor, exhibiting higher selectivity than for S1P1 and or S1P3 receptors. It is useful in the endogenous SIP signaling system and for mitigating or preventing central nervous system (CNS) diseases, including neurodegenerative diseases.

mTOR inhibitor-12 (Compound 11), a selective, brain-penetrant mTOR inhibitor, exhibits no genotoxicity risk and is utilized in research pertaining to central nervous system (CNS) diseases [1].

BET-IN-24 (example 2) is a bromodomain and extra-terminal (BET) inhibitor used in studies of virology, heart failure, inflammation, central nervous system (CNS) diseases, and various cancers.