L6H21, a derivative of chalcone, is an orally active and potent MD-2 (myeloid differentiation factor 2) inhibitor. L6H21 inhibits TLR4-NF-κB signaling and NLRP3 inflammasome activation in macrophages. L6H21 inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells. L6H21 effectively inhibits EtOH + LPS-induced hepatic fat accumulation and liver injury. L6H21 shows neuroprotective effect in a model of prediabetes[1][2].
Dimethocaine is a local anesthetic with reported stimulant properties most similar to cocaine.
Bombesin is a tetradecapeptide originally isolated from frog skin; plays an important role in the release of gastrin and the activation of G-protein receptors.
CGRP antagonist 4 is an antagonist of calcitonin gene-related peptide (CGRP) receptor. CGRP antagonist 4 shows the highest affinity for CGRP receptors in the human brain. CGRP antagonist 4 can be used to study the binding properties of non-peptide calcitonin gene-related peptide (CGRP) receptor antagonist (gepants) in rat, pig and human menes [1].
Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory[1][2].
Propiomazine is an orally active antihistamine agent with sedative effects. Propiomazine can be used in the research of insomnia[1][2].
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect[1][2].
Endokinin C is a peptide component of endokinin. Endokinin C works as a neurotransmitter or modulator in the pain system. Pretreatment with endokinin C prevents induction of scratching behavior and thermal hyperalgesia of endokinin A/B in mice[1].
IDRA 21 is a positive and orally active modulator of the AMPA receptor. IDRA 21 facilitates excitatory neurotransmission via GluR1/2 receptors. IDRA 21 has the potential for the research of cognitive/memory disorders, including those associated with aging[1].
Zonisamide-d4 (AD 810-d4) is the deuterium labeled Zonisamide. Zonisamide (AD 810) is an inhibitor of zinc enzyme carbonic anhydrase (CA), with Kis of 35.2 nM and 20.6 nM for human mitochondrial isozyme hCA II and hCA V, respectively. Zonisamide has antiepileptic activity. Zonisamide can be used for the rsearch for epilepsy, seizures and Parkinson's disease[1][2].
Aha1/Hsp90-IN-1 (Compound 17) is an Aha1/Hsp90 complex inhibitor. Aha1/Hsp90-IN-1 disrupts Aha1/Hsp90 interactions with an IC50 of 3.32 μM. Aha1/Hsp90-IN-1 inhibits tau aggregation[1].
SR7826 is a potent and selective LIM kinase (LIMK) inhibitor with IC50 of 43 nM, displays >100-fold selectivity over ROCK1 and ROCK2, as well as JNK kinases (>400-fold); inhibits only Limk1 and STK16 with >80% inhibition at 1 uM in a panel of 61 kinases; potently inhibits cofilin phosphorylation in A7r5, PC-3, and CEM-SS T cells (IC50 <1 uM), suppresses migration and invasion of PC-3 cells in vitro.
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype[1][2].
(Asp37)-Amyloid β-Protein (1-42) is the G37D mutant of wild-type Amyloid-beta (1-42) peptide[1].
Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington's disease (HD)[1][2][3][4].
Biotin-Substance P is the biotin tagged Substance P. Substance P (Neurokinin P) is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS. The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R)[1].
Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. IC50 Value: 1.7 nM (Mu-type opioid receptor) [1]in vitro: The dissociation rate of alvimopan from the micro opioid receptor (t(1/2)=30--44 min) was comparable to that of the long acting partial agonist buprenorphine (t(1/2)=44 min), but was slower than those of the antagonists naloxone (t(1/2)=0.82 min) and N-methylnaltrexone (t(1/2)=0.46 min) [2].in vivo: Alvimopan did not significantly accelerate GI-3 compared with placebo [6 mg: hazard ratio (HR) = 1.20, p = 0.080; 12 mg: HR = 1.24, p = 0.038). However, after adjustment for significant covariates (sex/surgical duration), benefits were significant for both doses (6 mg: HR = 1.24, p = 0.037; 12 mg: HR = 1.26, p = 0.028). Alvimopan also significantly accelerated time to GI-2 (6 mg: HR = 1.37, p = 0.008; 12 mg: HR = 1.33, p = 0.018) and DCO (6 mg: HR = 1.31, p = 0.008; 12 mg: HR = 1.28, p = 0.015) [3]. Alvimopan (1 and 3 mg/kg) significantly reversed this delayed GI transit when administered 45 min prior to surgery. However, the effects of alvimopan were less pronounced when administered following surgery [4].Toxicity:The most common treatment-emergent adverse events across all treatment groups were nausea, vomiting, and hypotension; the incidence of nausea and vomiting was reduced by 53 percent in thealvimopan 12-mg group [5].Clinical trial: Intercostal Nerve Block With Liposome Bupivacaine in Subjects Undergoing Posterolateral Thoracotomy. Phase 3
Uridine 5′-diphosphoglucose-13C disodium is the 13C labeled Uridine 5′-diphosphoglucose disodium salt. Uridine 5′-diphosphoglucose disodium salt (UDP-D-Glucose disodium salt) is the precursor of glucose-containing oligosaccharides, polysaccharides, glycop
CB1 antagonist 1 is an antagonist of CB1 receptor, used in the research of metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, gastrointestinal disorders, and cardiovascular conditions.
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons[1].
(S)-(+)-O-Desmethyl Venlafaxine is a S-enantiomer of O-Desmethyl Venlafaxine. O-Desmethyl Venlafaxine is an active metabolite of Venlafaxine[1]. Venlafaxine (HY-B0196) is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class[2].
Withanolide A, isolated from the indian herbal drug Ashwagandha (root of Withania somnifera), could regenerate neurites and reconstruct synapses in severely damaged neurons[1].
TCS 2210 (compound 1) is a neuronal differentiation inducer in mesenchymal stem cells (MSCs). TCS 2210 increases expression of the neuronal markers β-III tubulin and neuron-specific enolase (NSE)[1].
Inflachromene (ICM) is a microglial inhibitor with anti-inflammatory effects, directly binds high mobility group protein 1 (HMGB1) and HMGB2 and reduces their cytoplasmic accumulation in microglial cells; blocks the sequential processes of cytoplasmic localization and extracellular release of HMGBs by perturbing its post-translational modification; effectively downregulates proinflammatory functions of HMGB and reduces neuronal damage in vivo.
Isograndifoliol is a selective inhibitor of butyrylcholinesterase (BChE) with an IC50 value of 0.9 μM. And Isograndifoliol moderately inhibits acetylcholinesterase (AChE) with an IC50 value of 342.9 μM. Isograndifoliol also has vasorelaxant effect and anti-tumor effect. Isograndifoliol can be used for research against dementia caused by neurodegenerative diseases[1][2][3].
Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect[1][2][3].
(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders[1].
Pitavastatin (NK-104) sodium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin sodium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin sodium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin sodium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects[1][2][3][8].
Paroxetine maleate is a potent and selective inhibitor of SSRI. Paroxetine maleate is used in generalized anxiety disorder, post traumatic stress disorder, premenstrual dysphoric disorder and chronic headache research[1].