cns-active

ITI-214 is a picomolar PDE1 inhibitor with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters, and ion channels, exhibits potent PDE1 inhibitory activity (Ki = 58 pM).

AVN-322 is an orally active and specific 5-HT6R antagonist for the study of CNS disorders such as impaired memory and schizophrenia.

JNJ-26489112 is a CNS-active agent and inhibitor of voltage-gated Na+ channels and N-type Ca2+ channels with broad-spectrum anticonvulsant activity in rodents and can be used to study neurological disorders.

LY3372689 (Formulaic Ia) is an oral, highly selective, CNS-permeable O-GlcNAcase (OGA) inhibitor. LY3372689 exerts a neuroprotective effect by inhibiting OGA enzymatic activity, increasing the O-GlcNAc glycosylation level of tau protein, and thereby reducing abnormal tau phosphorylation and the formation of neurofibrillary tangles. LY3372689 can be used in research on tau-related diseases, including Alzheimer’s disease.

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity. It is used in relapsing-remitting multiple sclerosis, associated with modest reductions in CD4, CD8, and CD19 lymphocyte counts in cerebrospinal fluid.

Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

Ganciclovir (2'-Nor-2'-deoxyguanosine) is an ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

L-DOPA belongs to the category of dopamine precursors, serving as an orally active neurotransmitter metabolic precursor capable of crossing the blood-brain barrier and undergoing conversion to dopamine within the brain. The compound exhibits anti-hyperalgesic properties and finds application in Parkinson's disease research as well as in the induction of disease models.

Tryptamine hydrochloride is a monoamine alkaloid, metabolite of tryptophan and CNS active substance, agonist of 5-HT4 receptor, TAAR1 and AHR, with potential for blood-brain barrier permeability.

Uridine triacetate (RG 2133 triacetate) (Tri-O-acetyl uridine), an orally active prodrug of uridine, is efficiently absorbed in the gut and swiftly deacetylated in the circulation to release free uridine. It is utilized in the research of 5-fluorouracil (5-FU) and capecitabine toxicity, particularly targeting early-onset cardiac or central nervous system (CNS) complications.

Ganciclovir sodium (Cytovene IV sodium) is the sodium salt of Ganciclovir with antiviral activity, especially against cytomegalovirus (CMV) and herpes simplex virus type 1 (HSV-1).

AT-007 is an orally active CNS penetrant Aldose Reductase inhibitor for the treatment of Galactosemia (IC50: 100 pM). It reduces toxic galactitol levels and prevents disease complications in GALT deficiency rats.

DLK-IN-1 is a selective oral active inhibitor of bisleucine zipper kinase (DLK, MAP3K12) with Ki of 3 nM. DLK-IN-1 is active in the Alzheimer's disease model, retains excellent CNS permeability, and after multiple days of administration, its concentration

ICA-105665 (PF-04895162) is a potent and orally active opener of neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels. ICA-105665 had low cytotoxic potential in human hepatocytes but inhibited liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the central nervous system (CNS) and has antiseizure effects [1][2][3][4].

(Rac)-SEP-363856, the racemate of SEP-363856, is an orally active and CNS-active psychotropic agent with a unique profile.

SEP-363856 is an agent of orally active and CNS active psychotropic with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects, has the potential to treatment of schizophrenia.

SEP-363856 hydrochloride (SEP-856 hydrochloride) is an orally active, CNS-active psychotropic agent with a unique non-D2/5-HT2A mechanism of action, demonstrating antipsychotic-like effects and potential for schizophrenia treatment.

GLP-1R Antagonist 1 is an orally active, CNS penetrant and non-competitive glucagon-like peptide 1 receptor (GLP-1R) antagonist (IC50: 650 nM).

ONO-2920632 is an orally active and CNS-penetrant TREK channel activator with EC50 values of 0.3 µM for TREK-1 and 2.8 µM for TREK-2. It demonstrates selectivity for other K2P channels, showing over 91-fold selectivity against TASK1, TASK2, TASK3, TRAAK, TWIK2, and 31-fold selectivity against TRESK. ONO-2920632 exhibits analgesic effects and is used in the study of pain, migraine, and neurological disorders.

PF-06442609 is an orally active γ-secretase modulator with an IC50 value of 6 nM for Aβ42. It exhibits good CNS permeability.

5-HT2AR-IN-1 (Compound Ie) is an orally active inhibitor of the serotonin 2A receptor (5-HT2AR) with antidepressant effects. It reduces the expression of 5-HT2AR and levels of SERT protein. This compound holds potential for research in central nervous system (CNS) conditions, including depression and addiction-related disorders.

STAT3-IN-47 is an orally active STAT3 inhibitor. It exhibits broad-spectrum antitumor activity against HeLa, HepG2, U87, and LN229 cells. STAT3-IN-47 inhibits STAT3 activation in vitro. This compound is applicable for solid tumor research, particularly in studies of central nervous system (CNS) malignancies and hepatocellular carcinoma.

A-784168, a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1), acts on a ligand-gated nonselective cation channel pivotal in integrating pain stimuli including endogenous lipids, capsaicin, heat, and low pH. It demonstrates commendable central nervous system (CNS) penetration upon oral administration [1].

Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective, and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). It demonstrates potent efficacy against common activating EGFR mutations and the resistant T790M mutation. Rezivertinib hydrochloride efficiently penetrates the central nervous system (CNS) and exhibits antitumor activity in conditions such as non-small cell lung cancer (NSCLC).