Tat-NR2B9c is a 20-aa peptide, which acts as a postsynaptic density-95 (PSD-95) inhibitor, with an EC50 of 6.7 nM for PSD-95d2 (PSD-95 PDZ domain 2), and 670 nM for PSD-95d1; Tat-NR2B9c also reduces NMDA-induced p38 activation, and possesses neuroprotective efficacy.
MSX-2 is A2A adenosine receptor antagonist, with Ki of 5 nM in human that plays an important role in Parkinson's disease[1][2].
(-)-Eseroline fumarate is a metabolic of Physostigmine (HY-N6608), an AChE inhibitor. (-)-Eseroline fumarate elicits a leakage of lactic acid dehydrogenase (LDH) from cancer cells. (-)-Eseroline fumarate also induces the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, thus induce cell death. (-)-Eseroline fumarate inhibits the electrically evoked twitches of the mouse vas deferens and of the guinea-pig ileum[1][2].
Atenolol is a selective β1 receptor antagonist.Target: Adrenergic ReceptorAtenolol is a cardioselective beta-adrenergic blocker possessing properties and potency similar to propranolol, but without a negative inotropic effect [1, 2].
Dimethyl malonate is a competitive inhibitor of succinate dehydrogenase (SDH). Dimethyl malonate is able to cross the blood-brain barrier and hydrolyse to malonate. Dimethyl malonate reduces neuronal apoptosis[1].
BI-1408 is a potent γ secretase modulator with an IC50 of 0.04 μM for Aβ42[1].
Bis-ANS dipotassium is a fluorescent probe of hydrophobic protein. Bis-ANS binds to tubulin with a Kd of 2 μM[1]. Bis-ANS dipotassium is a potent biphasic modulator of protein liquid-liquid phase separation (LLPS). Bis-ANS dipotassium promotes LLPS at low concentrations but suppresses LLPS at high concentrations[2].
BPN14770 is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3 (two different dimeric forms of PDE4D), respectively[1].
Ipsapirone (TVX Q 7821), an anxiolytic compound and a 5-HT1A partial agonist, also exhibits 5-HT1A antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function[1][2].
Opioid receptor modulator 1 is a opioid receptor modulator extracted from patent WO2014072809A2, Compound RA11 in EXAMPLE 7.
Fluoroclebopride binds reversibly to dopamine receptors. 18F labeled fluoroclebopride has been used as a probe for studying D2/D3 receptor availability via PET in various monkey models[1][2].
Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and high affinity histamine H3 receptor antagonist (rat Ki=0.47 nM)[1][2][3][4][5].
SA72 is a highly selective fatty acid amide hydrolase (FAAH) inhibitor.
J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors[1].
Palvanil is a capsaicin analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects[1][2].
VU0155041 is a potent, selective and mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site[1].
Becampanel (AMP397) is the first competitive AMPA antagonist and an antiepileptic agent.
Citalopram hydrobromide is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) class. It has US FDA approval to treat major depression.
Procion Blue HB (Reactive Blue 2) is a purinergic antagonist.
Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats[1][2].
Pralidoxime iodide is a reactivator of acetylcholinesterase (AChE). Pralidoxime iodide reactivates nerve agent, which inhibits AChE via direct nucleophilic attack by the oxime moiety on the phosphorus center of the bound nerve agent. Pralidoxime iodide is an antidote for organophosphate poisoning[1][2].
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].
MUN57694 is 26S proteasome inhibitor. MUN57694 was reported in WO 2006128196. This product has not formal name. For the convenience of scientific communication, we named it by combining its Inchi key (3 letters from the first letter of each section) with the last 5 digits of its CAS number or its molecule weight if its CAS number is not available
Felbamate-d5 is the deuterium labeled Felbamate[1]. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA)[2][3].
Tau Peptide (45-73) (Exon 2/Insert 1 Domain) is aTau fragment.
Fluphenazine decanoate is a long-acting phenothiazine neuroleptic that used to treat schizophrenia. Fluphenazine decanoate is also a high and continuous dopamine D2 receptor blocker[1][2][3].
Paraxanthine, a caffeine metabolite, provides protection against Dopaminergic cell death via stimulation of Ryanodine Receptor Channels.
Picrotoxin is a noncompetitive antagonist of GABAA receptor.
AR-C102222 hydrochloride is a potent, competitive, orally active and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 37 nM[1]. AR-C102222 hydrochloride has antinociception and anti-inflammatory activities[2].
Ulinastatin (Uristatin) is a trypsin and serine protease inhibitor. Ulinastatin is the main protein binding inhibitor of various trypsin, chymotrypsin, and various pancreatic proteases. Ulinastatin shows neuroprotective, anti-inflammatory, anti-apoptotic, anti-oxidant effects[1][2].