Flo8 is a potent anti-inflammatory and antioxidant compound. Flo8 inhibits the release of intracellular reactive oxygen species (ROS) and nitric oxide (NO) and suppresses neuronal apoptotic by inhibiting inflammatory and apoptotic signaling pathways. Flo8 can be used for Parkinson's Disease (PD) research[1].
Simufilam (PTI-125) is a low toxicity, orally active filamin A (FLNA) activator. Simufilam preferentially binds altered FLNA and restores its native conformation, restores receptor and synaptic activities, reduces its a7nAChR/TLR4 associations and downstream pathologies. Simufilam can be used for the research of Alzheimer's disease[1].
Foscarbidopa (Carbidopa 4′-monophosphate) is a prodrug of Carbidopa, acts as a dopamine receptor agonist[1][2].
CP-409092 is a GABA(A) partial agonist, used for the treatment of anxiety.
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo[1][2].
Sodium Channel inhibitor 4 is a sodium channel inhibitor[1].
Casuarictin is a potent and competitive α-glucosidase inhibitor with an IC50 of 0.21 μg/mL. Casuarictin is a presenilin stabilization factor like protein (PSFL) protein inhibitor. Casuarictin can be used for Alzheimer's disease research[1].
α-Synuclein (61-95) (human) is the hydrophobic core region of α-synuclein, and induces neuronal cell death. α-Synuclein (61-95) (human) can be used for research of neurodegenerative diseases, including Alzheimer’s disease (AD) and Parkinson’s disease (PD)[1][2].
PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation[1][2][3].
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats[1][2].
Benserazide Hydrochloride is a peripherally-acting aromatic L-amino acid decarboxylase (AAAD) or DOPA decarboxylase inhibitor.Target: DOPA decarboxylaseBenserazide is commonly used for Parkinson's disease in combination with L-DOPA as a peripheral aromatic L-amino acid decarboxylase (AADC) inhibitor. Administration of 5, 10 and 50 mg/kg benserazide to 6-OHDA-lesioned rats showed an identical increase in exogenous L-DOPA-derived extracellular DA levels, the time to reach the peak DA levels were significantly prolonged by benserazide dose-dependently. The AADC activity in the denervated striatal tissues showed a significant decrease by 10 mg/kg and 50 mg/kg benserazide. These results suggest that benserazide reduces the central AADC activity in the striatum of rats with nigrostriatal denervation, which leads to changes in the metabolism of exogenous L-DOPA [1].
Ex26 (S1P1-IN-Ex26) is a potent and selective Sphingosine 1-phosphate receptor 1 (S1P1) antagonist (IC50=0.93 nM). Ex26 shows >3,000-fold selectivity for S1P1 over other Sphingosine 1-phosphate receptors. Ex26 can be used in experimental autoimmune encephalomyelitis reseach[1].
Fabomotizole (CM346) is an anxiolytic drug; produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions.IC50 value:Target: anxiolytic agent Afobazole's mechanism of action remains poorly defined however, with GABAergic, NGF and BDNF release promoting, MT1 receptor antagonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Afobazole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors. Afobazole has found little clinical use outside of Russia and has not been evaluated by the FDA.
PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study[1].
Pyridazinediones-derivative-1 has potential in treating neurodegenerative disorders. It shows an ED50 of 2.1 μM for inhibiting glutamate-induced contractions of isolated guineapig ileum.
Neritaloside could be isolated from nerium oleander. Neritaloside has central nervous system (CNS) depressant effect[1][2.
Icapamespib (PU-HZ151) is a potent HSP90 inhibitor with an EC50 of 5 nM. Icapamespib is able to cross blood-brain barrier[1].
IRL 1038 is an endothelin B receptor selective antagonist with a Ki of 6-11 nM[1].
Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant mGluR4 positive allosteric modulator (PAM) with an EC50 of 79 nM[1]. Antiparkinsonian effect[1].
Bilaid C, a tetrapeptide, can be isolated from the Australian estuarine isolate of Penicillium sp. MST-MF667. Bilaid C is also a potent and selective μ-Opioid Receptor (MOPr) agonist (Ki=210 nM, hMOPr)[1].
SV5 is a potent anti-Alzheimer agent. SV5 can significantly protect SHSY-5Y cells against Aβ1-42-induced death. SV5 shows moderate antioxidant and good neuroprotective activities. SV5 shows the high stability in human plasma and the best pharmacological profile[1].
Pirnabine is a cannabinoid receptor ligand. Pirnabine can be used for the research of glaucoma[1].
Glycine-13C is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
FG8119 is a novel benzodiazepine agonist extracted from patent US 4745112 A.
Gabapentin (Neurontin) is a pharmaceutical drug, specifically a GABA analog. It was originally developed to treat epilepsy, and currently is also used to relieve neuropathic pain.IC50 Value: 140 nM (α2δ subunit of calcium channel) [1]Target: Calcium Channelin vitro: Gabapentin, baclofen and CGP 44532 all reduced the electrically stimulated release of [3H]glutamic acid (IC50=20 microM, 0.8 microM and 2 microM, respectively). Gabapentin was without effect on the release of [3H]GABA, whilst baclofen (IC50=8 microM) and CGP 44532 (IC50=1 microM) inhibited [3H]GABA release [2]. A large inhibition of calcium currents by gabapentin was observed in pyramidal neocortical cells (up to 34%). Significantly, the gabapentin-mediated inhibition of calcium currents saturated at particularly low concentrations (around 10 microM), at least in neocortical neurons (IC50 about 4 microM) [3].in vivo: Gabapentin produced an anti-allodynic effect over the 7-day period, reducing the expression of pro-inflammatory cytokines but increasing the expression of IL-10 (TNF-α, 316.0 ± 69.7 pg/mL vs 88.8 ± 24.4 pg/mL; IL-1β, 1,212.9 ± 104.5 vs 577.4 ± 97.1 pg/mL; IL-6, 254.0 ± 64.8 pg/mL vs 125.5 ± 44.1 pg/mL; IL-10, 532.1 ± 78.7 pg/mL vs 918.9 ± 63.1 pg/mL). The suppressive effect of gabapentin on pro-inflammatory cytokine expression was partially blocked by the anti-IL-10 antibody [4].Toxicity: No new safety signals or adverse event trends relating to GEn exposure were identified [5].Clinical trial: N/A
cis-Indatraline (cis-Lu 19-005) hydrochloride is an active compound. cis-Indatraline (cis-Lu 19-005) hydrochloride can be used for the research of neurodegenerative diseases[1].
R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research [1].
Novel Activator of Satellite Cell Proliferation and Enhance Repair of Damaged Muscle