central activity

TCS 1102 is an effective, dual orexin receptor antagonist (Ki: 0.2/3 nM for OX2/1 receptors).

CS-722 Free base is a synthetic central muscle relaxant exhibiting muscle relaxant effects and inhibition of spinal reflexes. In hippocampal cultures, CS-722 Free base may suppress spontaneous inhibitory and excitatory post-synaptic currents by inhibiting sodium and calcium currents.

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.

Picenadol (LY 150720) is a racemic mixture of N-methyl-4-phenylpiperidine derivatives with agonist-antagonist opioid properties.Picenadol has central analgesic activity.

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.

(Z)-Metanicotine 2HCl has analgesic activity and is used in the treatment of central system disorders.

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.

Oxcarbazepine (GP 47680) is an Anti-epileptic Agent. The physiologic effect of oxcarbazepine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer. The physiologic effect of lamotrigine is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Flunarizine dihydrochloride (R14950) is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. Flunarizine dihydrochloride (R14950) is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Pentylenetetrazol is a GABA(A) receptor antagonist, that displays activity as a central nervous system and respiratory stimulant.

Citalopram hydrobromide (XU-62-320) , a selective serotonin reuptake inhibitor (SSRI), selectively inhibits the CNS neuronal reuptake of serotonin, thereby potentiating serotonergic activity in the central nervous system (CNS). Citalopram hydrobromide is the orally bioavailable hydrobromide salt of the racemic bicyclic phthalene derivative citalopram with antidepressant activity. This agent has minimal effects on the CNS neuronal reuptake of norepinephrine (NE) and dopamine (DA).

Buclizine dihydrochloride (Buclina) is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine dihydrochloride binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine dihydrochloride exerts its anti-emetic effect by binding to and blocking the muscarinic and histamine receptors in the vomiting center of the central nervous system (CNS). This may prevent activation of the chemoreceptor trigger zone (CTZ) and may reduce nausea and vomiting.

Histamine dihydrochloride (Ceplene) is the dihydrochloride salt form of histamine, an endogenous metabolic product. Histamine is an organic nitrogen-containing compound with diverse biological activities. It acts as a potent stimulator of gastric acid secretion, a bronchial smooth muscle constrictor, and a vasodilator, as well as a neurotransmitter with central nervous system activity. It is commonly used to induce gastric ulcer models in research.

(-)-Agelastatin A is a member of the pyrrole-aminoimidazole marine alkaloid (PAI) family, capable of inhibiting β-catenin, GSK-3β, and osteopontin (OPN), exhibiting antiproliferative activity against various cancers such as leukaemia and breast cancer, and possessing a certain ability to penetrate the central nervous system (CNS).

RMC5127 is an orally available, mutation-selective RAS G12V inhibitor exhibiting central nervous system (CNS) and brain permeability. It suppresses the RAS pathway and induces apoptosis in KRAS G12V mutant cancer cells, demonstrating antitumour activity.

OPN-9652 is a potent and orally active covalent TEAD inhibitor, with a half-maximal inhibitory concentration (IC50) of 0.005 µM against TEAD in MSTO-211H cells, and it targets the central palmitate-binding pocket of TEAD. OPN-9652 can significantly reduce the activity of TEAD-dependent reporter genes and downregulate the expression levels of TEAD target genes (CTGF and CYR61). Notably, OPN-9652 can reverse the resistance of SOX10 knockout (SOX10 KO) resistant cells to the combination of BRAF inhibitor (BRAFi) and MAPK inhibitor (MAPKi), restoring their sensitivity to the drugs. In the xenograft mouse model of BRAF-mutant A375 cells, OPN-9652 can effectively delay the development of tumor drug resistance; specifically, this effect is manifested by a significant delay in the onset of tumor drug resistance after the combination of BRAFi and MEK inhibitor (MEKi) starting from the minimal residual disease (MRD) stage. At present, OPN-9652 can be used as a research tool for scientific research related to melanoma.

ABBV-706 is an antibody-drug conjugate (ADC) that targets the receptor tyrosine kinase SEZ6. After binding to the surface of tumor cells, it is internalized and releases a cytotoxic payload, thereby inducing tumor cell death. ABBV-706 is currently in clinical development and has demonstrated potential antitumor activity in solid tumors such as small cell lung cancer.

Triflupromazine is a dopamine receptor D1/D2 antagonist and LHDA inhibitor that suppresses dopamine activity in the central nervous system (CNS) and promotes LDHA-mediated AMBRA1 ubiquitination, used for treating mental disorders, sedation, and antiemesis.

Natalizumab is a recombinant humanized monoclonal antibody and a humanized monoclonal antibody inhibitor that selectively targets α4 integrin (CD49d). Natalizumab binds to the α4β1 heterodimer and blocks its interaction with vascular cell adhesion molecule 1. Natalizumab also prevents lymphocytes from entering the central nervous system, thereby preventing acute demyelinating relapses, and is used in the study of relapsing-remitting multiple sclerosis and Crohn’s disease. Natalizumab possesses anti-inflammatory and immunomodulatory activity, inhibiting the adhesion, retention, and transendothelial migration of immune cells, and reducing the infiltration of inflammatory cells into the central nervous system or affected sites. Natalizumab is also being studied for autoimmune or inflammation-related diseases such as B-cell lymphoma and non-infectious uveitis.

WAY-213613 hydrochloride is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC 50 of 85 nM. WAY-213613 hydrochloride inhibits EAAT1 and EAAT3 with IC50 values of 5 and 3.8 microM, respectively. WAY-213613 hydrochloride shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function and can be used for the research of central nervous system [1] [2].

MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM), and a radioligand competition binding assay (IC50 = 3.4 nM).