cns

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

γ-Aminobutyric acid belongs to natural products and functions as an agonist of GABAA and GABAB receptors, possessing central sedative effects, cell permeability, and the ability to modulate neuronal excitability. This compound is used in neuroscience research and exhibits anxiolytic, anticonvulsant, and neuroprotective activities.

Proglumide (Binoside) is a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

BTRX-335140 (CYM-53093) is a potent and selective orally active κ-opioid receptor (KOR) antagonist with antagonistic activity against κOR, μOR, and δOR with IC50 values of 0.8, 110, and 6500 nM, respectively.

Caracemide (NSC-253272) inhibits the enzyme ribonucleotide reductase of Escherichia coli and can be utilized in anticancer studies.

(RS)-AMPA ((±)-AMPA) is a glutamate analog and an agonist of the effective and selective excitatory neurotransmitter L-glutamic acid.

SB-222200 is a selective, reversible, and competitive antagonist of the human NK-3 receptor(Ki=4.4 nM).

CYM5442 is an S1P agonist, targeting to Sphingosine.

XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1].

Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.

5J-4 is a potent a blocker of calcium release-activated calcium (CRAC) channel and store-operated calcium entry (SOCE). 5J-4 reduces the production of IL-17 and decreases the expression of RORα and RORγt.

MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3).

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.

AER-271 is an inhibitor of aquaporin-4.

ASP-2905 is a potent and selective inhibitor of potassium channel Kv12.2 encoded by the Kcnh3/BEC1 gene. It can cross the blood-brain barrier and has antipsychotic activities

2BAct is a novel eif2b activator, preventing neurological defects caused by a chronic integrated stress response

ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.

Lu AF27139 is an effective and selective antagonist of P2X7 receptor (IC50s of 12 and 2.4 nM for human and rat, Kis of 22, 54, and 13 nM for mouse, human, and rat, respectively). Lu AF27139 can be used in CNS diseases studies.

CNS-5161 hydrochloride (CNS 5161A) is a small molecule antagonist and an NMDA receptor antagonist that selectively and non-competitively blocks the action of glutamate, and can be used for research on neurological diseases.

CNS-5161 is a selective, non-competitive NMDA receptor antagonist that is able to displace [3H] MK-801 binding with a Ki of 1.8 nm. CNS-5161 inhibits NMDA receptor-mediated excitatory neurotransmission in both in vitro and in vivo experiments, thereby facilitating the study of neuroprotective mechanisms and related signaling pathways. CNS-5161 is commonly used in neuroscience research to assess excitotoxicity and neuronal survival in model systems, and can be employed in studies of the mechanisms underlying central nervous system disorders.

CNS-5788 is a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker

CNS-11, a compound that disaggregates tau fibrils, is utilized in Alzheimer's disease (AD) research [1].