Neurological Disease

F-00217830 is an agonist ofDopamine D2 receptor. PF-00217830 inhibits of spontaneous locomotor activity and 2,5-dimethoxy-4-iodoamphetamine-induced head twitches in rats.

GSK3β-IN-3 is an ATP-competitive GSK-3β inhibitor (IC₅₀ = 0.90 μM). GSK3β-IN-3 can reduce the phosphorylation level of tau protein in the BR5706 strain and reduce the deposition of Aβ aggregates in the CL2006 strain, and can be used to research Alzheimer's disease (AD).

Azosulfamide has an anticonvulsant effect and can be used for research of epilepsy. Azosulfamide is active against recurrent tetanus.

NBI 35965 hydrochloride is a selective, orally active and brain-penetrant corticotropin-releasing factor receptor 1 (CRF1) antagonist with a K_i value of 4 nM and a pK_i value of 8.5. NBI 35965 hydrochloride does not inhibit CRF2. NBI 35965 hydrochloride reduces CRF or stress-induced adrenocorticotropic hormone (ACTH) production in vivo with pIC₅₀ values of 7.1 and 6.9, respectively. NBI 35965 hydrochloride shows anxiolytic effects.

Proxyfan Oxalate is a potent histamine H3 receptor antagonist with K_i values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan Oxalate is over 1000-fold more potent at H3 receptors than other histamine receptors.

SSR504734 free base is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC₅₀=18, 15, and 38 nM, respectively). SSR504734 free base shows anti-schizophrenia, anti-anxiety and anti-depression activities.

Mambalgin-3 is an acid-sensitive ion channel 1 (ASIC1) inhibitor. Mambalgin-3 can be used in the study of analgesia.

Fluoxetine-d₆ oxalate (LY-110140-d₆ oxalate) is the deuterium labeled Fluoxetine oxalate. Fluoxetine oxalate is a selective serotonin reuptake inhibitor (SSRI) class used for antidepressant research.

Ambenoxan is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.

(D-Arg2, Sar 4)-Dermorphin (1-4) is a tetrapeptide derivative of the peptide Dermorphin (HY-P0244) found in amphibian skin. (D-Arg2, Sar 4)-Dermorphin (1-4) has significant analgesic effects by binding to the μ-opioid receptor (MOR) in the body. (D-Arg2, Sar 4)-Dermorphin (1-4) can be used in the development of analgesic drugs.

S(−)-Cyanopindolol hemifumarate is an isomer of Cyanopindolol (HY-W795507). S(-)-Cyanopindolol hemifumarate is a 5-HT1A/1B serotonin receptor antagonist and a β3-adrenoceptor antagonist.

E-0747 is an antiarrhythmic drug that inhibits arrhythmias by inhibiting Na^[+] channels in cardiomyocytes.

Bleformin A is a potent BChE inhibitor with an IC₅₀ value of 5.2 μM. Bleformin A is a nature product that could be isolated from Bletilla striata. Bleformin A can be used for research of Alzheimer's disease (AD).

SUVN-507 is a 5-HT6 receptor antagonist. SUVN-507 can reverse cognitive impairments and enhance excitatory neural transmission while weakening inhibitory neural transmission. SUVN-507 can be used for the research of neurological disease, such as Alzheimer's disease.

Anemarrhena extract (Rhizoma anemarrhenae extract) is an extract of Anemarrhena rhizome that can be used for research on neurological diseases.

NLRP3-IN-74 (Compound 11) is an orally active NLRP3 inhibitor with an IC₅₀ value of 2.7 μM. NLRP3-IN-74 can inhibit the release of IL-1β, reducing the release level by approximately 90%, and does not inhibit the release of TNFα. NLRP3-IN-74 can be used in the research of related diseases such as atherosclerosis and Parkinson's disease.

Brasofensine (BMS-204756) sulfate is an oral active dopamine transporter antagonist and can be used for parkinson’s disease research.

BRF110 is an orally active, blood-brain barrier-penetrant Nurr1-RXRα heterodimer activator with an EC₅₀ of 0.9 μM in human systems. BRF110 increases the mRNA level of BDNF, upregulates the transcription of TH, AADC and GCH1 to elevate striatal dopamine levels. BRF110 exhibits neuroprotective activity against MPP⁺-induced cytotoxicity. BRF110 prevents dopaminergic neuron death, protects nerve cells from toxic damage, and improves motor coordination in mouse models. BRF110 can be used in research related to Parkinson's disease.

NMDA receptor antagonist 8 (Compound (R)-10a) is GluN2B subunit-selective NMDA Receptor antagonist, with an K_i of 265 nM and an IC₅₀ of 62 nM. NMDA receptor antagonist 8 can be used for research of neurodegenerative diseases.

β Amyloid(17-28) human is a β-amyloid peptide (Abeta), a lipid-induced amyloid core fragment. β Amyloid(17-28) human enhances aggregation of full-length β Amyloid40, producing toxic aggregates in Alzheimer's disease (AD).