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.

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.

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

CNS-5161 hydrochloride (CNS 5161A) is a new antagonist of NMDA ion-channel. It interacts with the NMDA receptor ion channel site to produce a noncompetitive blockade of the actions of glutamate.

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

CNS-5161 is an NMDA antagonist.

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

In the CNS, Kainic acid is an effective agonist at excitatory amino acid receptor subtypes.

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.

5-HT7 agonist 1 (4-[4-[(2-chlorophenyl)methyl]piperazin-1-yl]-1H-indole) is a selective agonist of 5-HT7 (IC50 = 222.93 nM). 5-HT7 agonist 1 can be used in studies about CNS disorders.

VU6012962 is an orally bioavailable negative allosteric modulator of CNS-penetrant metabotropic glutamate receptor 7(mGlu7; IC50: 347 nM).

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.

Besipirdine (HP 749 free base) is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic and cardiovascular activities.Besipirdine inhibits voltage-dependent sodium-potassium channels and inhibits biogenic amine uptake.Besipirdine reduces schedule-induced irritability and thirst and enhances cholinergic and adrenergic activity in the CNS in the rat. Besipirdine reduces schedule-induced thirst and enhances cholinergic and adrenergic neurotransmission in the central nervous system.

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

LRRK2-IN-7 is a selective, CNS permeable and potent LRRK2 kinase inhibitor (IC50: 0.9 nM) for the study of Parkinson's disease.

Anisperimus (LF 15-0195) is an immunosuppressant that enhances activation-induced T-cell death by promoting caspase-8 and caspase-10 activation at the DISC level, and prevents CNS autoimmunity by promoting the development of Foxp3-expressing regulatory CD4 T cells.

AGI-41998 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A) that penetrates the blood-brain barrier. It inhibits S-adenosylmethionine (SAM) metabolizing enzymes and MAT2A for the treatment of cancer and for studying the role of SAM regulation in the central nervous system (CNS).

Org 13011 has CNS activity and induces conditioned taste aversion by mediating 5-HT 1A receptors.

Aptiganel (CNS-1102) is a non-competitive NMDA antagonist, a peptide that may be used to study acute ischemic stroke.

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.

JNJ-54175446 (JNJ-5446) is a CNS-permeable and selective P2X7 receptor antagonist that attenuates the release of IL-1β IL-18 from microglia, and may be used in the study of depression.

BW-1370U87 is a reversible competitive monoamine oxidase-A inhibitor for the study of depression and other CNS disorders.

Sipatrigine (619C89) is an antiepileptic compound with neuroprotective activity through glutamate release, TREK ion channels, TRESK channels, sodium channels, and calcium channel inhibitors in the CNS, and can be used to study TRESK channels.

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.