Risdiplam is an orally administered, centrally and peripherally distributed SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels.
GSK-3β inhibitor 11 (compound 21) is a glycogen synthase kinase-3β (GSK-3β) inhibitor (IC50=10.02 μM). GSK-3β inhibitor 11 can be used in neurodegenerative disease research[1].
AChE-IN-23 (compound 3h) is an acetylcholinesterase (AChE) inhibitor with an IC50 value of 48.3 μM[1].
Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM[1].
DSP-2230 is a selective Nav1.7/Nav1.8 blocker[1][2].
Picroside IV is an iridoid glycoside found in the underground parts of Picrorhiza scrophulariiflora. Picroside IV is a derivative of Catalpol (HY-N0820)[1]. Catalpol has neuroprotective, hypoglycemic, anti-inflammatory, anti-cancer, anti-spasmodic, anti-oxidant effects and anti-HBV effects[2].
RXFP3/4 agonist 2 is a potent, nonpeptide dual RXFP3/4 agonist (EC50=3.1 and 2.7 nM). RXFP3/4 agonist 2 also potently promotes interactions between RXFP3 and β-arrestin-2 with EC50 values in the range of 10-22 nM[1].
Hypaphorine is an indole alkaloid isolated from Pisolithus tinctorius, and with neurological and glucose-lowering effects in rodents[1].
BChE-IN-17 (compound 6n) is a potent and selective BChE inhibitor with IC50s of 10.5 nM and 32.5 nM for eqBChE and hBChE, respectively. BChE-IN-17 shows over 1000-fold selectivity to BChE against AChE. BChE-IN-17 shows low neurotoxicity and moderate neuroprotective effects[1].
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo. IC50 value: 2.6 nMTarget: NK-1 receptorIn vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4 nM, whereas the compound's affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC(50) values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13+/-2 and 27+/-2 nM in gerbil midbrain and rat striatum, respectively. In vivo, using the hind foot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity following oral administration (ID(50)=0.23 mg/kg; 2 h pretreatment), supporting a central activity of NKP608. NKP608 may prove a useful anxiolytic compound.
(R)-CR8 trihydrochloride (CR8 trihydrochloride), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect[1][2].
Nelonicline (ABT-126) is a selective neuronal nicotinic receptor agonist.
Trimipramine N-oxide is an active metabolite of the tricyclic antidepressant trimipramine. Trimipramine N-oxide inhibits the human monoamine transporters for noradrenaline (hNAT), serotonin (hSERT), dopamine (hDAT) and the human organic cation transporters (hOCT1 and hOCT2) with IC50s of 11.7, 3.59, 9.4, 9.35 and 27.4 nM, respectively. Trimipramine N-oxide can be used for the research of depression and anxiety[1].
Valbenazine is a prodrug of the (+)-α isomer of tetrabenazine for tardive syndrome therapy, and inhibits VMAT2 function.
ATX inhibitor 10 is a potent inhibitor of ATX. ATX inhibitor 10 is s nitrogen-containing heterocyclic compound. ATX plays a role in causing pathological conditions including fibrosis, arthritis, neurodegeneration, neuropathic pain, and cancer. ATX inhibitor 10 has the potential for the research of ATX related diseases (extracted from patent WO2021115375A1, compound 35)[1].
Tetrahydropalmatine, an active component isolated from corydalis, acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
(S)-(-)-5-Fluorowillardiine Hcl is a potent and specific AMPAR agonist.
Setiptiline-d3 (Org-8282-d3) is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].
Polyphyllin H, the major active component isolated from Rhizoma Paridis (named chonglou in Chinese), have been widely used in traditional Chinese medicinal preparations to treat inflammation, fracture and convulsion[1].
BChE-IN-13 (Compound 17c) is an orally active, potent and selective Butyrylcholinesterase (BChE) inhibitor with IC50s of 0.22 and 0.016 μM for eqBChE and hBChE, respectively. BChE-IN-13 can improve memory and cognitive impairments, and be used in Alzheimer’s disease (AD) research[1].
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice[1][2].
JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms[1].
HDAC-IN-58 is a HDAC inhibitor. HDAC-IN-58 has HDAC6-specific inhibition activity with an IC50 value of 2.06 nM. HDAC-IN-58 can be used for the research of chronic diseases, including neurodegenerative and psychiatric conditions[1].
Lys-Bradykinin, a kind of kallidin and bradykinin receptor ligand, can be generated by kininogen protein through enzymatic cleavage by the protease kallikrein. Lys-Bradykinin, also a vasodilator, can widen blood vessels and increase blood flow. Lys-Bradykinin involves in vascular regulation, inflammation and pain sensation[1].
NLRP3-IN-13 (Compound C77 in reference patent) is a selective and potent NLRP3 inhibitor (IC50: 2.1 μM). NLRP3-IN-13 inhibits NLRP3 andNLRC4 inflammasomes, and inhibits NLRP3-mediated IL-1β production. NLRP3-IN-13 also inhibits NLRP3 ATPase activity. NLRP3-IN-13 can be used in the research of neuroinflammatory disorders[1].
Theophyllol (theophylline sodium acetate) can alter calcium levels in subcellular fractions of rat brain cortex[1].
Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic drug of the benzamide class.
Ciproxifan maleate(FUB-359 maleate) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.IC50 value: Target: H3 receptorIn vitro, Ciproxifan behaved as a competitive antagonist at the H3 autoreceptor controlling 3H histamine release from synaptosomes and displayed similar Ki values (0.5-1.9 nM) at the H3 receptor controlling the electrically-induced contraction of guinea pig ileum or at the brain H3 receptor labeled with 125I-iodoproxyfan. This appears to be an orally bioavailable, extremely selective and potent H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders.
Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice [1].