YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease[1].
Carbidopa is an inhibitor of DOPA decarboxylase, which is used in parkinson disease.Target: DOPA decarboxylaseCarbidopa (CD), a competitive inhibitor of aromatic l-amino acid decarboxylase that does not cross the blood-brain barrier, is routinely administered with levodopa (LD) to patients with Parkinson disease (PD) to reduce the peripheral decarboxylation of LD to dopamine [1]. CD premedication improves 11C-5-HTP PET image quality and facilitates detection of NET lesions. Because of the similarity of metabolic pathways, this method could probably be applied to improve PET imaging using other tracers like 18F-DOPA and 11C-DOPA [2]. Carbidopa (100 microM) decreased growth of (but did not kill) SK-N-SH neuroblastoma and A204 rhabdomyosarcoma cells and did not affect proliferation of DU 145 prostate, MCF7 breast, or NCI-H460 large cell lung carcinoma lines. sublethal doses of carbidopa produced additive cytotoxic effects in carcinoid cells in combination with etoposide and cytotoxic synergy in SCLC cells when coincubated with topotecan [3].
AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (Kd=15.4 μM). AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis. AKOS-22 protects against mitochondrial dysfunction[1].
CBiPES hydrochloride is a mGlu2 receptor positive allosteric modulator (EC50: 92.8 nM). CBiPES hydrochloride attenuates stress-induced hyperthermia and PCP-induced hyperlocomotor activity. CBiPES hydrochloride can be used for research of neurological disease[1][2].
Thioproperazine (RP 7843) is an orally active antipsychotic agent with calming, antiemetic activity. Thioproperazine is effective in promoting the release of dopamine in rat striatum. Thioproperazine can be used in studies of schizophrenia and bipolar disorder[1].
(+)-Erinacin A is an anticancer compound that can be isolated from the mushroom Hericium erinaceum. (+)-Erinacin A has the capacity to trigger cancer cell death dependent on the production of reactive oxygen species (ROS). (+)-Erinacin A has anticancer and neuroprotective activity[1].
Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS)[1][2][3].
ZLc-002 is a selective small-molecule inhibitor of nNOS-Capon coupling. ZLc-002 suppresses inflammatory nociception and chemotherapy-induced neuropathic pain. ZLc-002 can be used for the research of anxiety disorder and inflammation[1][2][3].
PM226 is a selective cannabinoid CB2R agonist (Ki (CB2)=13 nM; EC50 (CB2)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo[1].
pep2-EVKI (YNVYGIEEVKI) is an inhibitor peptide that selectively blocks PICK1 interactions, caused the opposite effects on synaptic AMPAR function to PICK1 expression[1].
WAY 629 hydrochloride is a potent and selective 5-HT2C agonist with EC50s of 426, 260000 nM for 5-HT2C and 5-HT2A, respectively. WAY 629 hydrochloride decreases feeding behavior[1][2].
CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents[1].
Levoxadrol is an active enantiomer of dexoxadrol[1].
Gluten Exorphin A5 is a fragment from wheat gluten with neuroprotective effects. Gluten Exorphin A5 produces various effects not only in the peripheral nervous systems but also in the central nervous system[1].
Irisolidone is a major isoflavone found in Pueraria lobata flowers. Irisolidone exhibits potent hepatoprotective activity. Irisolidone shows the high efficacy for volume-regulated anion channels (VRAC) blockade[1][2][3].
CB1 antagonist 2 is caimabinoid 1 (CB1) antagonist extracted from patent WO2016184310A1, compound 3, inhibits CB1 in vivo with an IC50 of 25.5 nM[1].
SIRT2-IN-10 (Compound 12) is a potent SIRT2 inhibitor with an IC50 of 1.3 μM. SIRT2-IN-10 can be used for the research of cancer and neurodegenerative disease[1].
BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptor Ki values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent[1].
L-Ascorbic acid is an effective reducing agent and donor antioxidant.
ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively[1].
β-Amyloid Protein Precursor 770 (135-155) is a peptide of amyloid precursor protein isoform (APP 770). APP 770 produces Aβ40/42[1].
Pramipexole-d5 (dihydrochloride) is deuterium labeled Pramipexole (dihydrochloride). Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS)[1][2][3].
Menthol is a natural analgesic compound. Menthol could cause a feeling of coolness due to stimulation of ‘cold’ receptors by inhibiting Ca++ currents of neuronal membranes[1].
D-erythro-Sphingosine (Erythrosphingosine) hydrochloride is a specific TRPM3 activator. D-erythro-Sphingosine also induces retinoblastoma protein dephosphorylation[1][2].
Oxotremorine M iodide is a potent and selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms[1].
Atropine sulfate monohydrate is a competitive muscarinic acetylcholine receptor antagonist.Target: mAChRAtropine is a naturally occurring tropane alkaloid extracted from deadly nightshade (Atropa belladonna), Jimson weed (Datura stramonium), mandrake (Mandragora officinarum) and other plants of the family Solanaceae. Atropine is a competitive antagonist of the muscarinic acetylcholine receptors (acetylcholine being the main neurotransmitter used by the parasympathetic nervous system). Atropine dilates the pupils, increases heart rate, and reduces salivation and other secretions [1].
PF-CBP1 is a highly selective inhibitor of the CREB binding protein bromodomain[1].
Tavapadon (PF 6649751, PF-06649751) is an orally available dopamine D1 receptor partial agonist for treatment of Parkinson's disease. Parkinson Disease Discontinued
Miglustat(OGT918) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).Target: OthersMiglustat is an inhibitor of the ceramide-specific glycosyltransferase, which catalyzes the first step of glycosphingolipid biosynthesis and is currently approved for the oral treatment of type 1 GD [1]. Consumption of a standard high-fat breakfast within 30 minutes before administration of miglustat significantly reduced peak exposure but did not significantly affect the extent of systemic exposure to miglustat. The peak plasma concentration (C(max)) decreased by 36% on average following administration with food. Area under the plasma concentration-time curve (AUC(0-infinity)) showed a modest (14%) decrease with food, but the 90% confidence interval was within the acceptance limit of 80% to 125%. The median (min-max) time to C(max) (t(max)) was prolonged from 2.5 (1.0-4.0) hours in the fasted state to 4.5 (1.5-8.0) hours in the fed state, whereas the apparent terminal half-life was approximately 8 hours and not affected by food [2].
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.