Neurological Disease

Decanoic acid-d₅ is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.

BRD6688 is a selective HDAC inhibitor with IC₅₀ values of 21 nM and 100 nM for HDAC1 and HDAC2, respectively. BRD6688 induces histone H4K12 and H3K9 acetylation. BRD6688 decreases CK2-induced HDAC2 phosphorylation. BRD6688 induces macrophage M1 to M2 polarization and renal cell proliferation. BRD6688 is used in research on neurodegenerative diseases, acute kidney injury, pain, and anxiety disorders.

NB-3 is a nicotinamide adenine dinucleotide (NAD) hydrolase SARM1 inhibitor. NB-3 intercepts NAD hydrolysis and undergoes covalent conjugation with the reaction product adenosine diphosphate ribose (ADPR). The resulting small-molecule ADPR adducts are highly potent and confer compelling neuroprotection in neurological injury.

GSK1059865 is a potent orexin 1 receptor antagonist.

SP11 is a mitochondrial fission protein 1 (Fis1) inhibitor with an IC₅₀ of 9.4 μM. SP11 binds only to activated Fis1 by engaging Cys41. SP11 preserves mitochondrial integrity and function during oxidative stress, inhibits hydrogen peroxide-induced mitochondrial ROS production, mitochondrial fragmentation, and Drp1 mitochondrial translocation. SP11 can be used for the research of parkinson’s disease.

VUF-5574 is a selective antagonist of adenosine A³ receptor with a K_i of 4.03 nM for the recombinant human receptor.

2-Methyl-4-pentenoic Acid (2-Methylpent-4-enoic acid) is an organic acid that can be used as a precursor for synthesizing other compounds. Additionally, changes in the level of 2-Methyl-4-pentenoic Acid may be associated with the susceptibility to schizophrenia and type 2 diabetes.

Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a K_i of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model.

NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC₅₀ values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits.

p-Xylene bis(pyridinium bromide) (compound 21), a cationic charged quencher, is a week bisquaternary AChE and BChE inhibitor with IC₅₀s of 1540 μM and 529 μM, respectively.

S-22153 is a potent melatonin receptor antagonist with EC₅₀ values of 19 nM, 4.6 nM for hMT₁ and hMT₂ melatonin receptor, respectively. S-22153 has K_i values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT₁, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT₂. S-22153 is a specific ligand of MT₁ and MT₂ melatonin receptors subtypes.

Butabindide (UCL-1397) oxalate is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with K_i values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide oxalate inhibits TPP II to protect CCK-8 against inactivation.

Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal.

Tetrahydropalmatine (DL-Tetrahydropalmatine) hydrochloride possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.

(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABA_A/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT_2C and 5-HT_1A receptor, with IC₅₀ values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.

Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment.

NCGC 607 is a noninhibitory small-molecule chaperone of glucocerebrosidase (GCase). NCGC 607 can increase GCase activity, reduce α-synuclein levels, and decrease glycolipid levels. NCGC 607 can be used in the research of Gaucher disease and Parkinson's disease.

ITH12575, a CGP37157 derivative, is a potent and selective mNCX blocker. ITH12575 reduces Ca²⁺ influx through CALHM1 at low micromolar concentrations.

TLR7 agonist 3 (compound 2) is a TLR7 agonist and can be used for the stuy of cancers.

Dynorphin B (1-13) acts as an agonist on opioid κ-receptor.